Search Result
Results for "
Competitive
" in MedChemExpress (MCE) Product Catalog:
2113
Inhibitors & Agonists
15
Biochemical Assay Reagents
140
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-147167
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- HY-120182
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- HY-18732C
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Tilarginine hydrochloride; Methylarginine hydrochloride
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NO Synthase
Endogenous Metabolite
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Cardiovascular Disease
Cancer
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L-NMMA (Tilarginine) hydrochloride competitively antagonizes L-arginine, and thus inhibits production of nitric oxide (NO). L-NMMA hydrochloride is utilized as NO synthase antagonist in experimental settings .
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-
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- HY-18732
-
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Tilarginine; Methylarginine
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NO Synthase
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Others
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L-NMMA (Tilarginine; Methylarginine) competitively antagonizes L-arginine, and thus inhibits production of nitric oxide (NO). L-NMMA is utilized as NO synthase antagonist in experimental settings .
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- HY-P3786
-
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PKA
PKC
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Cancer
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H-Arg-Gly-Tyr-Ala-Leu-Gly-OH is a competitive and CAMP dependent protein kinase inhibitor .
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- HY-118177
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-
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- HY-136344
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Drug Metabolite
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Others
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Simvastatin Acyl-β-D-glucuronide is a metabolite of Simvastatin. Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM .
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- HY-115273
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P2Y Receptor
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Others
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MRS-2179 is a selective and competitive antagonist for P2Y1 receptor, with KB of 0.177 μM .
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- HY-136345
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Drug Metabolite
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Others
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(Rac)-3′-Hydroxy simvastatin is a metabolite of Simvastatin. Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM .
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- HY-136347
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-
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- HY-19593
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Fungal
Antibiotic
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Infection
|
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Nikkomycin Z, a nucleoside-peptide, is a selective competitive chitin synthesis inhibitor. Nikkomycin Z has antifungal effects and acts as a competitive analogue of the chitin synthase substrate UDP-N-acetylglucosamine .
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- HY-P1292
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PKG
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Cancer
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PKG inhibitor peptide is an ATP-competitive inhibitor of cGMP-dependent protein kinase (PKG), with a Ki of 86 μM .
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- HY-120239
-
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5-HT Receptor
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Neurological Disease
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Ro 63-0563 is a potent, competitive and selective 5-HT6 receptor antagonist with pKi values ??of 7.83 and 7.91 for rat and human 5-HT6 receptors, respectively. Ro 63-0563 has no affinity for other receptors .
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- HY-107704
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-
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- HY-129250
-
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Histamine Receptor
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Neurological Disease
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AZD5213 is a selective and competitive human H3 receptor antagonist with a pKi value of 9.3 for hH3R. AZD5213 can be used for the research of sleep and cognitive regulation .
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- HY-105375
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Cytochrome P450
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Cancer
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FR 901537 is a potent and competitive aromatase inhibitor. FR 901537, a novel naphthol derivative, has the potential for breast cancer research .
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- HY-19361
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-
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- HY-18732B
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- HY-10450S
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BMS-512148-d5
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SGLT
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Metabolic Disease
Cancer
|
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Dapagliflozin-d5 is a deuterium labeled Dapagliflozin. Dapagliflozin is a competitive SGLT2 inhibitor[1].
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- HY-161411
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Glucosidase
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Metabolic Disease
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α-Glucosidase-IN-60 (Compound 5k) exhibits a competitive inhibitory efficacy against α-Glucosidase, with IC50 of 10.8 μM .
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- HY-136347R
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HMG-CoA Reductase (HMGCR)
Drug Metabolite
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Cardiovascular Disease
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3α-Hydroxy pravastatin (sodium) (Standard) is the analytical standard of 3α-Hydroxy pravastatin (sodium). This product is intended for research and analytical applications. 3α-Hydroxy pravastatin sodium is the major metabolite of Pravastatin. Pravastatin is a competitive HMG-CoA reductase inhibitor .
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- HY-114923
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DNA-PK
PI3K
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Cancer
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SU-11752 is an inhibitor for DNA-dependent protein kinase (DNA-PK) with an IC50 of 0.13 μM. SU-11752 inhibits PI3K p110γ kinase with IC50 of 1.1 μM. SU-11752 binds competitively for ATP-site in DNA-PK, results in inhibition of intracellular DNA double-strand break repair and increases the sensitivity of cells to radiotherapy .
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- HY-146318
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-
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- HY-147879
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- HY-109079A
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DWP14012 hydrochloride; Fexuprazan hydrochloride
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Proton Pump
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Metabolic Disease
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Abeprazan hydrochloride (DWP14012 hydrochloride) is a potassium-competitive acid blocker. Abeprazan hydrochloride inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan hydrochloride is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases .
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- HY-109079
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DWP14012; Fexuprazan
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Proton Pump
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Metabolic Disease
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Abeprazan (DWP14012) is a potassium-competitive acid blocker. Abeprazan inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases .
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- HY-N2689
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(R)-6′,7′-DHB
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Cytochrome P450
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Cancer
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(R)-6',7'-Dihydroxybergamottin ((R)-6′,7′-DHB) is a competitive inhibitor of human and rat CYP1A1 activity with Kis of 55 μM and 1.72 μM, respectively. (R)-6',7'-Dihydroxybergamottin has the potential for cancer research .
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- HY-120491
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Others
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Cardiovascular Disease
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L 722151 is a competitive inhibitor for factor XIIIa with Ki of 49 µM. L 722151 accelerates tissue plasminogen activator-catalyzed clot dissolution, and exhibits antithrombotic efficacy .
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- HY-161299
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Parasite
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Infection
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LAPTc-IN-1 (compound 4) is a competitive inhibitor targeting acidic M17 leucinopeptidase (LAPTc) with Ki=0.27 μM. LAPTc-IN-1 is a potential antagonist of the parasite Trypanosoma cruzi .
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- HY-B1582A
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Aldadiene potassium; SC-14266
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Mineralocorticoid Receptor
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Cardiovascular Disease
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Canrenoate (Aldadiene) potassium, a proagent that releases canrenone, is a potent, competitive mineralocorticoid receptor (aldosterone receptor) antagonist. Potassium canrenoate, as a diuretic, is used for the research of hypertension .
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- HY-139145
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Trimethylopropane phosphate
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GABA Receptor
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Neurological Disease
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Etbicyphat (Trimethylopropane phosphate) is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors .
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- HY-149527
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-
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- HY-114991
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HPPD
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Others
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Leptospermone is a competitive, reversible inhibitor for p-Hydroxyphenylpyruvate dioxygenase (HPPD), with an IC50 of 12.1 μM. Leptospermone exhibits herbicidal activity for its bleaching effect .
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- HY-149528
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Monoamine Oxidase
Cholinesterase (ChE)
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Cancer
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MAO-B-IN-24 (compound 11h) is a selective, reversible, competitive inhibitor of MAO-B (IC50: 1.60 μM). MAO-B-IN-24 also inhibited MAO-A (22.42 μM); at 10 μM concentration, it also reduced AChE and BChE activities to 54.58% and 88.43% .
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- HY-119409
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-
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- HY-A0252
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- HY-116854
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GCGR
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Metabolic Disease
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NNC 92-1687 is a non-peptide competitive human glucagon receptor antagonist (IC50=20 μM; Ki=9.1 μM). NNC 92-1687 can be used in the research of type 2 diabetes .
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- HY-162711
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Others
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Cancer
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Methylbiocin is an ATP competitive inhibitor for human CMG helicase with an IC50 of 59 µM. Methylbiocin exhibits potential in cancer research .
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- HY-P1294
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CRFR
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Neurological Disease
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α-Helical CRF(9-41) is a competitive CRF2 receptor antagonist with KB of ~100 nM. α-Helical CRF(9-41) is also a partial agonist of CRF1 receptor with an EC50 of 140 nM .
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- HY-12031
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MEK
Autophagy
Mitophagy
Influenza Virus
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Cancer
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U0126 (U0126-EtOH) is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor .
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- HY-100782
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2-APH; 2-Amino-7-phosphonoheptanoic acid
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iGluR
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Neurological Disease
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DL-AP7 is a competitive NMDA antagonist and an anticonvulsant. DL-AP7 blocks the NMDA-induced convulsions and impairs learning performance in a passive avoidance task in mice .
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- HY-19316
-
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O6-(Cyclohexylmethyl)guanine
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CDK
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Cancer
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NU2058 (O6-(Cyclohexylmethyl)guanine) is a potent, competitive and guanine-based CDK inhibitor with IC50s of 17 μM and 26 μM for CDK2 and CDK1. NU2058 has anti-cancer activity.
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- HY-P1294A
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CRFR
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Neurological Disease
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α-Helical CRF(9-41) TFA is a competitive CRF2 receptor antagonist with KB of ~100 nM. α-Helical CRF(9-41) TFA is also a partial agonist of CRF1 receptor with an EC50 of 140 nM .
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- HY-123480
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5-HT Receptor
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Neurological Disease
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EGIS-7625 is a selective and competitive 5-HT2B inhibitor with pKi values of 9.0, 6.2, 7.7 for 5-HT2B, 5-HT2A, 5-HT2C, respective. EGIS-7625 partially attenuates m-chlorophenylpiperazine-induced hypomotility and hypophagia .
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- HY-N2554
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Ostenol
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Monoamine Oxidase
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Neurological Disease
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Osthenol (Ostenol), a prenylated coumarin isolated from the dried roots of Angelica pubescens, is selective, reversible, and competitive human monoamine oxidase-A (hMAO-A) inhibitor (Ki=0.26 µM). Osthenol potently inhibits recombinant hMAO-A with an IC50 of 0.74 µM and shows a high selectivity index for hMAO-A versus hMAO-B .
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- HY-119016
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SK1-I
1 Publications Verification
BML-258
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SphK
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Cancer
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SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM . SK1-I shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I enhances autophagy and has antitumor activity .
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- HY-119016A
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BML-258 hydrochloride
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SphK
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Cancer
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SK1-I hydrochloride (BML-258 hydrochloride), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM . SK1-I hydrochloride shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I hydrochloride enhances autophagy and has antitumor activity .
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- HY-122203A
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mAChR
Cholinesterase (ChE)
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Neurological Disease
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PCS1055 is a selective and competitive antagonist for muscarinic M4 receptor with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 is also an inhibitor for AChE with IC50 of 22 nM and 120 nM for electric eel and human AChE, respectively .
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- HY-151591
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Phosphatase
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Metabolic Disease
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SPAA-52 is an orally active, competitive and reversible low-molecular-weight protein tyrosine phosphatase (LMW-PTP) inhibitor (IC50=4 nM, Ki=1.2 nM). SPAA-52 can be used in diabete research .
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- HY-B0334
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CP45899
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Bacterial
Antibiotic
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Infection
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Sulbactam (CP45899) is a competitive, irreversible beta-lactamase inhibitor. Sulbactam shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex .
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- HY-B0334A
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CP45899 sodium
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Bacterial
Antibiotic
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Infection
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Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex .
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- HY-A0252R
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Adrenergic Receptor
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Inflammation/Immunology
Cancer
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Bupranolol (Standard) is the analytical standard of Bupranolol. This product is intended for research and analytical applications. Bupranolol is an orally active, competitive and non-selective β-adrenoceptor antagonist without intrinsic sympathomimetic activity .
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- HY-117043
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Deubiquitinase
SARS-CoV
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Infection
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GRL0617 is a selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLpro), with an IC50 of 0.6 μM and a Ki value of 0.49 μM. GRL0617 also inhibits SARS-CoV with an EC50 of 14.5 μM. GRL0617 can be used for the research of severe acute respiratory syndrome .
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- HY-P0222
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PKA
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Others
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PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor .
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- HY-112468
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CDK
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Cancer
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PNU112455A hydrochloride is an ATP-competitive CDK2 and CDK5 inhibitor. PNU112455A hydrochloride binds to the ATP site of CDK2 and CDK5 with Kms of 3.6 and 3.2 μM, respectively .
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- HY-P0222A
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PKA
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Others
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PKI(5-24) TFA is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) TFA corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor .
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- HY-W013754
-
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Others
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Others
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S-Hexylglutathione is an S-substituted glutathione in which the hydrogen of the thiol has been replaced by a hexyl group. S-Hexylglutathione is also an competitive inhibitor against glutathione-S-transferase. S-Hexylglutathione can be used as an affinity chromatographic ligand for glutathione-S-transferase and glutathione peroxidase .
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- HY-100414
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BYK61359
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Proton Pump
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Metabolic Disease
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Soraprazan (BYK61359) is a selective, reversible K-competitive inhibitor of the H,K-ATPase (Ki=6.4 nM), with an IC50 of 0.19 μM in gastric glands. Soraprazan binds to the H,K-ATPase with a Kd of 28.27 nM. Soraprazan shows immediate inhibition of acid secretion and is more than 2000-fold selective for H,K-ATPase over Na,K- and Ca-ATPases .
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- HY-113468A
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3-Methoxy-L-tyrosine; 3-O-Methyl-L-DOPA
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Dopamine Receptor
Endogenous Metabolite
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Neurological Disease
|
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3-O-Methyldopa (3-Methoxy-L-tyrosine) is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine .
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- HY-134246
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5'-dTuMP
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Others
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Others
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7-CH-5'-dAMP (5'-dTuMP) is an adenylate derivative that acts as a potential substrate, competitive inhibitor, or modulator of enzymes that interact with 2-deoxyadenosine-5-monophosphate .
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- HY-B0437AS
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MJ 1999-d6 hydrochloride
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Adrenergic Receptor
Potassium Channel
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Cardiovascular Disease
Endocrinology
|
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Sotalol-d6 (hydrochloride) is a deuterium labeled Sotalol hydrochloride. Sotalol hydrochloride is an orally active, non-selective competitive β-adrenergic receptor blocker. Sotalol hydrochloride is a potent antiarrhythmic agent that can be used for the research of pediatric arrhythmias. Sotalol hydrochloride blocks β-receptors, and potassium KCNH2 channels[1][2].
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- HY-110154
-
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Histone Demethylase
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Cancer
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NSC636819 is a competitive and selective inhibitor of KDM4A/KDM4B. KDM4A/KDM4B are potential progression factors for prostate cancer. NSC636819 has the potential for the research of cancer diseases, especially prostate cancer .
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- HY-14806
-
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MP-513
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Dipeptidyl Peptidase
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Metabolic Disease
|
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Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM .
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- HY-162485
-
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Dengue virus
Virus Protease
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Infection
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DV-B-120 is a competitive inhibitor for dengue virus (DENV) with IC50s of 5.35, 7.39, 10.49 and 8.58 μM, for DENV-1, DENV-2, DENV-3 and DENV-4, respectively, by inhibiting NS2B-NS3 protease. DV-B-120 exhibits antiviral activity through inhibition of DENV replication .
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- HY-13452
-
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ML282
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Ras
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Inflammation/Immunology
|
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CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with a Ki of 13 nM.
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- HY-10195
-
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LY333531
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PKC
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Metabolic Disease
|
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Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin inhibits PKC beta II with an IC50 of 5.9 nM .
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- HY-15067
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DNQX
5 Publications Verification
FG 9041
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iGluR
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Cancer
|
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DNQX (FG 9041), a quinoxaline derivative, is a selective, potent competitive non-NMDA glutamate receptor antagonist (IC50s = 0.5, 2 and 40 μM for AMPA, kainate and NMDA receptors, respectively) .
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- HY-155374
-
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Phosphatase
Apoptosis
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Cancer
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PP5-IN-1 (Compound P053) is a competitive inhibitor of Serine/threonine protein phosphatase-5 (PP5) that binds to its catalytic domain and causes apoptosis in renal cancer .
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- HY-10195A
-
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LY333531 mesylate
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PKC
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Cardiovascular Disease
Metabolic Disease
|
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Ruboxistaurin (LY333531) mesylate is an orally active, selective and ATP competitive PKCβ inhibitor with IC50 values of 4.7 and 5.9 nM for PKCβI and PKCβII, respectively. Ruboxistaurin mesylate can be used for the research of eye disorders, heart failure and diabetes .
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- HY-B0334R
-
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Bacterial
Antibiotic
|
Infection
|
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Sulbactam (Standard) is the analytical standard of Sulbactam. This product is intended for research and analytical applications. Sulbactam (CP45899) is a competitive, irreversible beta-lactamase inhibitor. Sulbactam shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex .
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- HY-B0334AR
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Bacterial
Antibiotic
|
Infection
|
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Sulbactam (sodium) (Standard) is the analytical standard of Sulbactam (sodium). This product is intended for research and analytical applications. Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex .
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- HY-103233
-
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FG 9041 disodium salt
|
iGluR
|
Cancer
|
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DNQX (FG 9041) disodium salt, a quinoxaline derivative, is a selective, potent competitive non-NMDA glutamate receptor antagonist (IC50s = 0.5, 2 and 40 μM for AMPA, kainate and NMDA receptors, respectively) .
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- HY-19435A
-
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iGluR
Cytochrome P450
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Neurological Disease
|
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GYKI-47261 dihydrochloride is a competitive, orally active, and selective AMPA receptor antagonist with an IC50 of 2.5 μM. GYKI-47261 has broad spectrum anticonvulsive activity and neuroprotective effects. GYKI-47261 dihydrochloride is also a potent inducer of CYP2E1 .
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- HY-19435
-
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iGluR
Cytochrome P450
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Neurological Disease
|
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GYKI-47261 is a competitive, orally active, and selective AMPA receptor antagonist with an IC50 of 2.5 μM. GYKI-47261 has broad spectrum anticonvulsive activity and neuroprotective effects. GYKI-47261 is also a potent inducer of CYP2E1 .
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- HY-126946
-
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Fungal
|
Infection
|
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Nikkomycin pseudo-J is a tripeptide derivative of the nikkomycin class found in Streptomyces tendae, which has antifungal and antiinsect activities. Nikkomycin pseudo-J exerts its biological activity by competitively inhibiting chitin synthetase of fungi and insects .
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- HY-124366
-
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Others
|
Infection
Cancer
|
|
Slingshot inhibitor D3 is a potent, selective, reversible and competitive inhibitor of Slingshot. The IC50 value for Slingshot 1 is 3 μM and the Ki value for Slingshot 2 is 3.9 μM. Slingshot inhibitor D3 has similar inhibitory activities toward both Slingshot 1 and Slingshot 2 .
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- HY-129278
-
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Parasite
|
Infection
Cardiovascular Disease
Neurological Disease
|
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Lunarine is an alkaloid, which can be isolated from the seeds of kale (Lunaria annua). Lunarine lowers the blood pressure, stimulates small intestinal motility, inhibits spontaneous contractions of uterus and nervous system, and exhibits an acute toxicity with LD50 of 62.3 mg/kg in dogs and rabbits. Lunarine exhibits antiparasitic activity through a competitive inhibition of protozoan oxidoreductase trypanothione reductase (TryR) with Ki of 304 μM .
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- HY-132309
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BRD0639
1 Publications Verification
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Histone Methyltransferase
|
Cancer
|
|
BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities .
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- HY-162642
-
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Bcl-2 Family
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Cancer
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Bfl-1-IN-3 (Compound 56) is a selective, competitive inhibitor for Bfl-1 on BID binding site with Ki of 105 nM. Bfl-1-IN-3 inhibits the proliferation of cell pfeiffer and MV4-11, with IC50 of 6.92 μM and 12.6 μM. Bfl-1-IN-3 induces apoptosis in pfeiffer cells. Bfl-1-IN-3 overcomes Venetoclax (HY-15531) resistance at the cellular level, and shows synergistically enhanced anti-tumor activity with Venetoclax .
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- HY-149929
-
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Beta-lactamase
Bacterial
|
Infection
|
|
EBL-3183, an indole-2-carboxylate, is a potent metallo-β-lactamase (MBL) inhibitor. EBL-3183 is reversibly binding, non-covalent, competitive NDM-1 inhibitor with a pIC50 of 7.7 .
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- HY-14806R
-
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Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Teneligliptin (Standard) is the analytical standard of Teneligliptin. This product is intended for research and analytical applications. Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM .
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-
- HY-168079
-
|
|
GSK-3
Tau Protein
|
Neurological Disease
Inflammation/Immunology
|
|
GSK-3β inhibitor 21 (compound 44) is an ATP-competitive GSK-3β inhibitor (IC50=6.06 μM) with anti-amyloid aggregation and tau phosphorylation inhibitory activities. GSK-3β inhibitor 21 can be used in the study of Alzheimer's disease .
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-
- HY-101964
-
|
|
SHP2
Phosphatase
|
Cancer
|
|
SPI-112 is a potent, selective and competitive SHP2 (PTPN11) inhibitor with IC50s of 1 μM, 18.3 μM and 14.5 μM for SHP2, protein tyrosine phosphatase (PTP) and PTP1B, respectively .
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-
- HY-P1299
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 is a potent, selective, and competitive antagonist of the NOP receptor, with a pKi of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 shows antidepressant-like effect .
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-
- HY-100606
-
|
(-)-Pindolol; (S)-(-)-Pindolol; S-Pindolol
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
l-Pindolol ((-)-pindolol) is a reversible, competitive and orally active 5-HT1A/1B antagonist. l-Pindolol is a partial β-adrenoceptor agonist. l-Pindolol can be used for the research of neurological disease .
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-
- HY-127024
-
|
|
Thyroid Hormone Receptor
|
Metabolic Disease
|
|
Thyroid hormone receptor antagonist (1-850) is a competitive, selective and high-affinity thyroid hormone receptor (TR) antagonist with an IC50 of 1.5 μM for antagonizing the effect of T3 on TR. Thyroid hormone receptor antagonist (1-850) blocks T3-mediated interaction of TRα and TRβ with nuclear receptor coactivator. Thyroid hormone receptor antagonist (1-850) has no effect on the activity of RARα .
|
-
- HY-117058
-
|
(6S)-DDATHF
|
Antifolate
|
Cancer
|
|
LY243246 ((6S)-DDATHF), the 6S diastereomer of DDATHF, is a potent competitive inhibitor of 5’-phosphoribosylglycinamide formyltransferase (GAR transformylase). 6R- and 6S-diastereomers of DDATHF are remarkably similar and equiactive antimetabolites inhibitory to de novo purine synthesis .
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-
- HY-113906A
-
|
|
GHSR
|
Inflammation/Immunology
|
|
(αR,8aS)-GSK1614343 (compound 18a, d2) is a cyclized ghrelin antagonist with an pIC50 value of 8.4. (αR,8aS)-GSK1614343 shows a competitive antagonism of hGHSR1a with a mean pKb value of 8.06 .
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-
- HY-19012
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
N-1518 is an α and β adrenergic receptor blocker that has competitive antagonism against β1 and α1 receptors, but does not show selectivity for β1 receptors, but shows about 20-fold selectivity for α1 receptors. N-1518 has vasodilatory effects and can be used in the research field of hypertension treatment .
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-
- HY-N6057
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Obtusin, isolated from Cassia obtusifolia Linn seed, is a highly selective and competitive human monoamine oxidase-A (hMAO-A) inhibitor with an IC50 of 11.12 μM and a Ki of 6.15 μM. Obtusin plays a preventive role in neurodegenerative diseases, especially anxiety and depression .
|
-
- HY-134280
-
|
Nicotinamide 8-Br-hypoxanthine dinucleotide
|
Others
|
Others
|
|
8-Br-NHD+ (Nicotinamide 8-Br-hypoxanthine dinucleotide) is a derivative of NAD+ (nicotinamide adenine dinucleotide) that acts as a potential substrate, competitive inhibitor or modulator of enzymes that interact with β-NAD+. 8-Br-NHD+ can be used to synthesize a cyclic ADP nucleotide (cADPR) analog .
|
-
- HY-N7536
-
|
|
TRP Channel
|
Others
|
|
Voacangine is an antagonist for TRPV1 and TRPM8 but as an agonist for TRPA1 (EC50=8 μM). Voacangine competitively blockes capsaicin binding to TRPV1 (IC50=50 μM). Voacangine competitively inhibits the binding of menthol to TRPM8 (IC50=9 μM) and it shows noncompetitive inhibition against icilin (IC50=7 μM). Voacangine selectively abrogates chemical agonist-induced TRPM8 activation and did not affect cold-induced activation. Voacangine is an alkaloid isolated from the root bark of Voacanga africana .
|
-
- HY-P1299A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect .
|
-
- HY-123517
-
|
|
Enterovirus
|
Infection
|
|
DC07090 dihydrochloride is a low toxicity, potent, reversible and competitive non-peptidyl human enterovirus 71 3C protease inhibitor with an IC50 and a Ki value for 21.72 μM and 23.29 μM. DC07090 dihydrochloride could also inhibit coxsackievirus A16 (CVA16) replication with an EC50 value of 27.76 μM .
|
-
- HY-125625
-
|
|
Renin
|
Cardiovascular Disease
|
|
ES 6864 is an orally active, competitive inhibitor for human renin, with an IC50 of 6.9 nM and a Ki of 7.3 nM. ES 6864 exhibits high species-specific and enzyme-specific properties. ES 6864 exhibits metabolic stability in rat tissue homogenates. ES 6864 reduces blood pressure in rats and sodium-depleted awake marmosets .
|
-
- HY-138568
-
|
|
MAP4K
|
Inflammation/Immunology
|
|
HPK1-IN-3 is a potent and selective ATP-competitive hematopoietic progenitor kinase 1 (HPK1; MAP4K1) inhibitor with an IC50 of 0.25 nM. HPK1-IN-3 has IL-2 cellular potency with an EC50 of 108 nM in human peripheral blood mononuclear cells (PBMCs) .
|
-
- HY-133130
-
|
|
MAGL
|
Neurological Disease
|
|
JNJ-42226314 is a competitive, highly selective and reversible non-covalent monoacylglycerol lipase (MAGL) inhibitor. JNJ-42226314 demonstrates dose-dependent enhancement of the major endocannabinoid 2-arachidonoylglycerol (2-AG) as well as efficacy in models of neuropathic and inflammatory pain .
|
-
- HY-158417
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
KSI-6666 is an orally active, competitive antagonist for sphingosine 1-phosphate receptor 1 (S1PR1), with an IC50 of 6.4 nM. KSI-6666 exhibits anti-inflammatory efficacy in autoimmune encephalomyelitis model and T cell transfer colitis model .
|
-
- HY-148207
-
|
|
Amino Acid Derivatives
|
Metabolic Disease
|
|
S-Benzylglutathione is a competitive glutathionase inhibitor. S-Benzylglutathione is converted to the corresponding cysteine derivatives by rat kidney microsomes. S-Benzylglutathione can be used for the research of metabolic breakdown of glutathione by the glutathionase system .
|
-
- HY-116621
-
|
|
DNA-PK
|
Cancer
|
|
NU-7163 is an ATP-competitive DNA-PK inhibitor (IC50=0.19 μM; Ki=24 nM). NU-7163 enhances the cytotoxicity of ionizing radiation against the HeLa human tumor cell line in vitro .
|
-
- HY-115570
-
|
GW108X
|
Kinesin
ULK
Autophagy
|
Cancer
|
|
GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK .
|
-
- HY-107670
-
|
DHβE hydrobromide
|
nAChR
|
Neurological Disease
|
|
Dihydro-β-erythroidine (DHβE) hydrobromide is a potent, orally active, and competitive antagonist of neuronal nAChRs. Dihydro-β-erythroidine hydrobromide shows selectivity for α4β4 and α4β2 nAChRs, with IC50s of 0.19 and 0.37 μM, respectively. Antidepressant-like activities .
|
-
- HY-164388
-
|
|
Caspase
Apoptosis
Autophagy
Necroptosis
|
Cardiovascular Disease
Cancer
|
|
Z-VAD is a competitive, irreversible pan-caspase inhibitor. Z-VAD inhibits all 10 caspases, except for caspase-2 which is only weakly inhibited. Z-VAD decreases radiation-induced apoptosis. Z-VAD induces both autophagy and necrosis in irradiated MDA-MB-231 and H460 mouse xenografts. Z-VAD with radiation produces a significant tumor growth delay and shows dramatic antiangiogenic effect in cancer xenograft .
|
-
- HY-402410
-
|
|
TET Protein
|
Cancer
|
|
TETi76 is an orally active TET family inhibitor with IC50 values ??of 1.5, 9.4 and 8.8 μM for TET1, TET2 and TET3, respectively. TETi76 competitively binds to the active site of TET enzymes, reduces cytosine hydroxymethylation and restricts clonal growth of TET2 mutants in vitro and in vivo, but does not affect the growth of normal hematopoietic precursor cells. TETi76 can be used for leukemia research .
|
-
- HY-11007
-
GNF-2
2 Publications Verification
|
Bcr-Abl
SARS-CoV
|
Cancer
|
|
GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
|
-
- HY-101308
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
MRS2179 tetrasodium is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors . MRS2179 tetrasodium inhibits platelet aggregation .
|
-
- HY-101308A
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
MRS2179 tetrasodium hydrate is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium hydrate is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors . MRS2179 tetrasodium hydrate inhibits platelet aggregation .
|
-
- HY-123171
-
|
|
Others
|
Metabolic Disease
|
|
ASP8497 is a competitive dipeptidyl peptidase IV (DPP-IV) inhibitor that reduces blood glucose levels and increases plasma active GLP-1 and insulin levels without causing hypoglycemia in fasted normal mice. ASP8497 can be utilized for antihyperglycemic research .
|
-
- HY-129944
-
|
|
Phospholipase
|
Inflammation/Immunology
|
|
MJ33-OH is a metabolite of MJ33. MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6 .
|
-
- HY-14806S
-
|
MP-513 d8
|
Dipeptidyl Peptidase
|
Cardiovascular Disease
|
|
Teneligliptin-d8 is a deuterium labeled Teneligliptin (MP-513). Teneligliptin is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor[1].
|
-
- HY-P3245
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-P3245A
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 hydrochloride is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 hydrochloride antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 hydrochloride selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-129944A
-
|
|
Phospholipase
|
Inflammation/Immunology
|
|
MJ33-OH lithium is a metabolite of MJ33. MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6 .
|
-
- HY-148208
-
|
|
Amino Acid Derivatives
|
Metabolic Disease
|
|
S-(p-Nitrobenzyl)glutathione is a competitive glutathionase inhibitor. S-(p-Nitrobenzyl)glutathione is converted to the corresponding cysteine derivatives by rat kidney microsomes. S-(p-Nitrobenzyl)glutathione can be used for the research of metabolic breakdown of glutathione by the glutathionase system .
|
-
- HY-100834
-
|
5,7-DCKA
|
iGluR
|
Neurological Disease
|
|
5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid, a derivative of kynurenic acid, reduced NMDA-induced neuron injury in rat cortical cell cultures .
|
-
- HY-145860
-
|
|
Phosphoglycerate Dehydrogenase (PHGDH)
|
Cancer
|
|
PHGDH-IN-2 is a potent and NAD + competitive PHGDH inhibitor with an IC50 of 5.2 µM. PHGDH-IN-2 inhibits the serine synthetic pathway in MDA-MB-468 cells. PHGDH-IN-2 inhibits the growth of PHGDH-dependent cancer cells .
|
-
- HY-18953
-
|
|
mTOR
|
Cancer
|
|
mTOR inhibitor-23 (compound DHM25) is a selective, competitive, irreversible and covalent inhibitor of mTOR. mTOR inhibitor-23 has the mechanism of inhibition occurs mainly through its capacity to covalently interact with a nucleophilic amino acid inside the ATP pocket. mTOR inhibitor-23 exerts potent antitumor activity against triple-negative breast tumor cell lines .
|
-
- HY-129412
-
|
|
Renin
|
Cardiovascular Disease
|
|
A-74273 is an orally active peptide renin inhibitor (IC50=3.1 nM). A-74273 competitively binds to the active site of renin, preventing angiotensinogen from being converted to ANG-I, thereby reducing the level of angiotensin II. A-74273 can be used in the study of diseases such as hypertension .
|
-
- HY-123981
-
|
|
Phosphatase
|
Cancer
|
|
5MPN is a first-in-class, potent, orally active and selective 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4) inhibitor. 5MPN appears to be a competitive inhibitor of the F6P binding site (Ki=8.6 μM). 5MPN does not inhibit PFK-1 or PFKFB3. 5MPN targets the sugar metabolism of tumors and suppresses proliferation of multiple human cancer cell lines .
|
-
- HY-103282
-
|
|
Bombesin Receptor
|
Others
|
|
[D-Phe12]-Bombesin is a derivative of Bombesin (HY-P0195) and an antagonist for bombesin receptor with Ki of 4.7 μM. [D-Phe12]-Bombesin inhibits the Bombesin (HY-P0195)-induced amylase release, with IC50 of 4 μM .
|
-
![[D-Phe12]-Bombesin](//file.medchemexpress.eu/product_pic/hy-103282.gif)
- HY-B0919
-
|
CI-337; O-Diazoacetyl-L-serine; P-165
|
Bacterial
Antibiotic
DNA/RNA Synthesis
|
Infection
Cancer
|
|
Azazerine (CI-337) is a competitive inhibitor of glutamine amidotransferase. Azaserine is an antibiotic, it shows antibacterial activities. Azazerine shows anti-tumor activities and it may also act as a tumor inducer. Azazerine can be used for the research of cancer and infection .
|
-
- HY-N7433
-
|
Ethylidene-glucose
|
GLUT
Endogenous Metabolite
|
Metabolic Disease
|
|
4,6-O-ethylidene-α-D-glucose (Ethylidene-glucose), a glucose derivative, is a competitive exofacial binding-site inhibitor on glucose transporter 1 (GLUT1) with a Ki of 12 mM for wild-type 2-deoxy-D-glucose transport .
|
-
- HY-145462
-
|
|
Bacterial
|
Infection
|
|
N-cis-octadec-9Z-enoyl-L-Homoserine lactone is a potent inhibitor of AhyI. AhyI (expressing acylhomoserine lactone) is responsible for the biosynthesis of autoinducer-1 (AI-1), commonly referred to as a quorum sensing (QS) signaling molecule, which plays an essential role in bacterial communication. N-cis-octadec-9Z-enoyl-L-Homoserine lactone is a competitive inhibitor of AI-1 biosynthesis .
|
-
- HY-P10552
-
|
|
CXCR
|
Inflammation/Immunology
|
|
pCXCL8-1aa is an anti-inflammatory peptide. pCXCL8-1aa competitively inhibits the binding of CXCL8 to glycosaminoglycans such as heparin sulfate (HS) by binding with high affinity. This reduces the presentation of CXCL8 on the surface of vascular endothelial cells, thereby inhibiting neutrophil migration and inflammatory responses. pCXCL8-1aa can be used to study inflammatory diseases such as rheumatoid arthritis .
|
-
- HY-100501
-
|
MSC2363318A
|
Ribosomal S6 Kinase (RSK)
Akt
|
Cancer
|
|
M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity .
|
-
- HY-155280
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-60 (compound 5a) is an S-adenosylmethionine (SAM)-competitive and irreversible SARS-CoV-2 nsp16-nsp10 methyltransferase activity inhibitor with an IC50 of 9 μM and a Ki of 26 μM. SARS-CoV-2-IN-60 can specifically occupy a newly identified pocket adjacent to the SAM-binding site on nsp16. SARS-CoV-2-IN-60 has the potential for pan-coronavirus therapeutics .
|
-
- HY-152208
-
|
|
SHP2
|
Cancer
|
|
BPDA2 is a highly selective and competitive active site SHP2 inhibitor with IC50s of 92.0 nM, 33.39 μM, 40.71 μM for SHP2, SHP1, SHP1B, respectively. DBDA2 downregulates mitogenic and cell survival signaling and RTK expression. BPDA2 suppresses SHP2 mediated signaling and breast cancer cell phenotypes .
|
-
- HY-128129
-
|
|
Urea Transporter
|
Metabolic Disease
|
|
UT-B-IN-1 (UTBINH-14) is a reversible, competitive and selective urea transporter-B (UT-B) inhibitor with IC50 values of 10 and 25 nM for human and mouse UT-B, respectively. UT-B-IN-1 shows low toxicity and high selectivity for UT-B over UT-A isoforms. UT-B-IN-1 increases urine output and reduces urine osmolality of mice. UT-B-IN-1 can be used for diuretic mechanism research .
|
-
- HY-137955
-
|
|
P2Y Receptor
|
Cardiovascular Disease
Others
Neurological Disease
|
|
MRS 2211 sodium hydrate is a competitive P2Y13 receptor antagonist (pIC50= 5.97). MRS 2211 sodium hydrate is highly selective to the P2Y13 receptor, showing more than 20-fold selectivity compared to the P2Y1 and P2Y12 receptors. MRS 2211 sodium hydrate can be used to further investigate the role of the P2Y13 receptor in different physiological and pathological processes, such as its function in blood cells, the nervous system and the immune system .
|
-
- HY-149880
-
|
|
c-Met/HGFR
|
Cancer
|
|
c-Met-IN-18 is ATP competitive type-III c-MET inhibitor of WT and D1228V mutant c-MET. c-Met-IN-18 has inhibitory for WT/D1228V with an IC50 value of 0.013/0.20 e.c-Met-IN-18 can be used for the research of c-MET driven cancers . c-Met-IN-18 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-114858
-
|
|
Casein Kinase
|
Cancer
|
|
Epiblastin A is an ATP competitive casein kinase 1 (CK1) inhibitor with IC50s of 8.9, 0.5, and 4.7 µM for CK1α, CK1δ, and CK1 ɛ, respectively. Epiblastin A induces reprogramming of epiblast stem cells into embryonic stem cells by inhibition of CK1 .
|
-
- HY-155108B
-
|
|
Arginase
|
Cancer
|
|
OATD-02 hydrochloride is the hydrochloride salt form of OATD-02 (HY-155108). OATD-02 hydrochloride an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and Arginase2. OATD-02 hydrochloride is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 hydrochloride bolishes tumor immunosuppression induced by both arginases. OATD-02 hydrochloride can be used for melanoma study .
|
-
- HY-P3678
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Neuropeptide Y (18-36) (porcine) is a competitive neuropeptide Y (NPY) cardiac receptor antagonist. Neuropeptide Y (18-36) (porcine) inhibits the binding of I-NPY to cardiac ventricular membranes in a concentration-dependent manner with an IC50 value of 158 nM and an Ki value of 140 nM. Neuropeptide Y (18-36) (porcine) can be used for the research of congestive heart failure .
|
-
- HY-13404
-
|
INC280; INCB28060
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-112345
-
|
|
FGFR
PDGFR
EGFR
Src
|
Cancer
|
|
PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity .
|
-
- HY-13404B
-
|
INC280 hydrochloride; INCB-28060 hydrochloride
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Capmatinib (INC280; INCB28060) hydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib hydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib hydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib hydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-13404C
-
|
INC280 dihydrochloride hydrate; INCB-28060 dihydrochloride hydrate
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Capmatinib (INC280; INCB28060) dihydrochloride hydrate is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride hydrate can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride hydrate potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride hydrate is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-13404A
-
|
INC280 dihydrochloride; INCB28060 dihydrochloride
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Capmatinib (INC280; INCB28060) dihydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-160478
-
|
|
Bcr-Abl
|
Cancer
|
|
GNF-6 (Compound 14) inhibits the gatekeeper threonine residue mutation of BCR-ABL-T315I with IC50s of 0.25 μM, 0.09 μM and 0.590 μM for c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants, respectively. GNF-6, an ATP competitive inhibitor, disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), thereby locking the kinase in an inactive ‘DFG-out’ conformation .
|
-
- HY-126388
-
-
- HY-100924
-
|
|
GABA Receptor
|
Neurological Disease
|
|
β-CCB is a ligand for benzodiazepine receptor, which inhibits the binding of [ 3H]flunitrazepam and ethyl (3-[ 3H]carboline-3-carboxylate to benzodiazepine receptors, with Ki of 3-4 nM. β-CCB exhibits proconvulsant and anxiogenic effects .
|
-
- HY-13404R
-
|
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Capmatinib (Standard) is the analytical standard of Capmatinib. This product is intended for research and analytical applications. Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-15295
-
|
TAK-438
|
Proton Pump
|
Metabolic Disease
|
|
Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease .
|
-
- HY-100007A
-
|
TAK-438 hydrochloride
|
Proton Pump
Bacterial
|
Infection
Endocrinology
|
|
Vonoprazan hydrochloride, a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan hydrochloride inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan hydrochloride is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan hydrochloride can be used for eradication of Helicobacter pylori .
|
-
- HY-P2625
-
|
|
GCGR
|
Metabolic Disease
|
|
GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC50=5.8 nM) .
|
-
- HY-P2625S1
-
|
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
|
GLP-2(3-33) (Leu- 13C6, 15N) TFA is 13C and 15N labeled GLP-2(3-33) (HY-P2625). GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC50=5.8 nM).
|
-
- HY-P2625S
-
|
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
|
GLP-2(3-33) (Leu- 13C6, 15N) is 13C and 15N labeled GLP-2(3-33) (HY-P2625). GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC50=5.8 nM).
|
-
- HY-100007
-
|
TAK-438 free base
|
Proton Pump
Bacterial
|
Endocrinology
|
|
Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan can be used for eradication of Helicobacter pylori .
|
-
- HY-100007R
-
|
TAK-438 (Standard)
|
Proton Pump
Bacterial
|
Endocrinology
|
|
Vonoprazan (Standard) is the analytical standard of Vonoprazan. This product is intended for research and analytical applications. Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan can be used for eradication of Helicobacter pylori .
|
-
- HY-149404
-
|
|
Reactive Oxygen Species
Tyrosinase
|
Others
|
|
Non-competitive tyrosinase inhibitor (Tyrosinase-IN-12) is a potent, non-competitive tyrosinase inhibitor with an IC50 value of 49.33 ± 2.64 µM and Ki value of 31.25 ± 0.25 µM. Non-competitive tyrosinase inhibitor (Tyrosinase-IN-12) have the highest radical scavenging activity to reduce the production of reactive oxygen species (ROS) with an IC50 value of 25.39 ± 0.77 µM. Non-competitive tyrosinase inhibitor (Tyrosinase-IN-12) can be used for anti-browning substances in the food and agricultural sectors .
|
-
- HY-B0140
-
-
- HY-W016645
-
|
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
4-Diethylaminobenzaldehyde is a reversible aldehyde dehydrogenases (ALDHs) inhibitor, with a Ki of 4 nM for ALDH1. 4-Diethylaminobenzaldehyde displays potent anti-androgenic effect (IC50= 1.71μM) .
|
-
- HY-B0437S
-
-
- HY-100785
-
-
- HY-B1413
-
-
- HY-131408
-
|
|
Others
|
Others
|
|
L-Allooctopine is a competitive inhibitor of D-octopine .
|
-
- HY-120189
-
-
- HY-N3090
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
Peucedanol is a non-competitive inhibitor of CYP3A4 with a Ki value of 4.07 μM and a competitive inhibitor of CYP1A2 and CYP2D6 with Ki values of 3.39 μM and 6.77 μM, respectively .
|
-
- HY-100255
-
-
- HY-22385
-
-
- HY-135072
-
|
|
Others
|
Infection
|
|
N,N',N''-Triacetylchitotriose is a competitive inhibitor of lysozyme .
|
-
- HY-115939
-
|
|
Bacterial
|
Infection
|
|
Urease-IN-2 (compound 8g) is a non-competitive urease inhibitor with an IC50 of 0.94 μM and a Ki of 1.6 μM. Urease-IN-2 inhibits the Jack bean urease (JBU) in a non-competitive manner .
|
-
- HY-15073
-
-
- HY-50948
-
-
- HY-B0009
-
-
- HY-17502
-
-
- HY-N2194
-
|
5-Geranoxypsoralen; Bergamotine; Bergaptin
|
Cytochrome P450
|
Cancer
|
|
Bergamottin is a potent and competitive CYP1A1 inhibitor with a Ki of 10.703 nM.
|
-
- HY-W013673
-
-
- HY-110097
-
|
CNS 1102
|
iGluR
|
Neurological Disease
|
|
Aptiganel hydrochloride (Cerestat) is a non-competitive NMDA receptor antagonist with neuroprotective effect.
|
-
- HY-W013744
-
|
|
Others
|
Others
|
|
S-Octylglutathione is a competitive glutathione S-transferase (GST) inhibitor .
|
-
- HY-126306
-
-
- HY-101631
-
-
- HY-108032
-
|
Pyrostatin A; 5-Hydroxyectoine
|
OGA
|
Metabolic Disease
|
|
Hydroxyectoin (Pyrostatin A) is a competitive inhibitor of GlcNAcase, with the Ki of 1.7 μM .
|
-
- HY-A0066
-
-
- HY-B1239
-
-
- HY-13646A
-
|
HM30181 mesylate; HM30181A mesylate
|
P-glycoprotein
|
Cancer
|
|
Encequidar mesylate (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor.
|
-
- HY-125145
-
-
- HY-22385A
-
-
- HY-W015876
-
|
(+)-Leucinol
|
Aminopeptidase
|
Others
|
|
L-Leucinol ((+)-Leucinol) is a competitive aminopeptidase inhibitor with Ki value of 17 μM .
|
-
- HY-116290
-
|
Squalestatin S1
|
Others
|
Others
|
|
Zaragozic acid A is a fungal metabolite that acts as a reversible competitive inhibitor of squalene synthase .
|
-
- HY-B0385
-
|
FOY
|
Proteasome
Factor Xa
|
Inflammation/Immunology
|
|
Gabexate mesylate (FOY) is is a competitive and non-antigenic synthetic inhibitor of trypsin-like serine proteinases. Gabexate mesylate inhibits human thrombin, urokinase, plasmin, and Factor Xa with Kis of 0.97, 1.3, 1.6, and 8.5 μM, respectively. Gabexate mesylate binds to human and bovine tryptase with Kis of 3.4 nM and 18 μM, respectively. Gabexate mesylate exerts an anticoagulant effect on the clotting activity of thrombin and has anti-inflammatory effect by viainhibition of NF-κB, proinflammatory cytokines, and nitric oxide. Gabexate mesylate is used for pancreatitis and disseminated intravascular coagulation .
|
-
- HY-15066
-
|
FG9065
|
iGluR
|
Neurological Disease
|
|
CNQX (FG9065) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX is a competitive non-NMDA receptor antagonist . CNQX blocks the expression of fear-potentiated startle in rats .
|
-
- HY-E70252
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
1-Pyrenebutanoyl-CoA is a type of coenzyme A that can non-competitively inhibit (Ki = 2 μM) phosphorylating (ADP-stimulated) respiration in rat liver mitochondria, and competitively inhibit (Ki = 2.1 μM and 15 μM) carnitine palmitoyl-CoA transferase and octanoyl-CoA transferase .
|
-
- HY-11092
-
-
- HY-U00188
-
-
- HY-12471
-
VLX1570
2 Publications Verification
|
Deubiquitinase
|
Cancer
|
|
VLX1570 is a competitive inhibitor of proteasome deubiquitinases (DUBs) with an IC50 of approximate 10 μM.
|
-
- HY-16461
-
|
(-)-Solenopsin A
|
Akt
|
Cardiovascular Disease
|
|
Solenopsin ((-)-Solenopsin A) is an ATP-competitive AKT inhibitor with IC50 value of 10 μM .
|
-
- HY-W010510
-
-
- HY-122641A
-
-
- HY-122641C
-
-
- HY-135404
-
-
- HY-50949
-
-
- HY-115743
-
|
|
MAP3K
|
Cancer
|
|
TAK1-IN-3 is a potent ATP-competitive TAK1 inhibitor.
|
-
- HY-15269
-
|
|
mTOR
PI3K
|
Cancer
|
|
PP30, a TORKinib, is a potent, selective, and ATP-competitive inhibitor of mTOR with an IC50 of 80 nM.
|
-
- HY-112465
-
|
|
PKA
|
Cancer
|
|
H-8 (dihydrochloride) is a cell-permeable, reversible and ATP-competitive PKA inhibitor .
|
-
- HY-W000932
-
|
|
Bacterial
|
Infection
|
|
Butylboronic acid is a competitive soybean urease inhibitor with an IC50 of 2.9 mM and a Ki of 1.5 mM .
|
-
- HY-116290A
-
|
Squalestatin S1 trisodium
|
Others
|
Others
|
|
Zaragozic acid A trisodium is a fungal metabolite that acts as a reversible competitive inhibitor of squalene synthase .
|
-
- HY-134382
-
|
7-Deaza-2'-deoxyadenosine-5'-O-diphosphate
|
Others
|
Others
|
|
7-CH-dADP is a competitive inhibitor or regulator of enzymes that interact with dADP .
|
-
- HY-B1239A
-
-
- HY-115570A
-
|
(Z/E)-GW108X
|
Kinesin
ULK
Autophagy
|
Cancer
|
|
(Z/E)-GW406108X is a mixture of different configurations of GW406108X (HY-115570). GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM .
|
-
- HY-B0140R
-
|
|
Phosphodiesterase (PDE)
Adenosine Receptor
|
Inflammation/Immunology
Cancer
|
|
Aminophylline (Standard) is the analytical standard of Aminophylline. This product is intended for research and analytical applications. Aminophylline is a competitive and non-selective phosphodiesterase (PDE) inhibitor. Aminophylline is a competitive adenosine receptor antagonist. Aminophylline has apulmonary vasodilator action as well as a bronchodilator action and has the potential for asthma research .
|
-
- HY-126055
-
|
|
Others
|
Others
|
|
Hadacidin is a competitive inhibitor of adenylate synthase. Hadacidin binds to the active site of adenylate synthase, competitively inhibiting L-aspartate binding. Hadacidin can be used in drug design, to help develop new inhibitors or activators to regulate adenylate synthase activity, and to play a role in the study of related diseases .
|
-
- HY-126055A
-
|
|
Others
|
Others
|
|
Hadacidin sodium is a competitive inhibitor of adenylate synthase. Hadacidin sodium binds to the active site of adenylate synthase, competitively inhibiting L-aspartate binding. Hadacidin sodium can be used in drug design, to help develop new inhibitors or activators to regulate adenylate synthase activity, and to play a role in the study of related diseases .
|
-
- HY-12382
-
|
|
Mps1
|
Cancer
|
|
NMS-P715 is a selective, ATP-competitive inhibitor of MPS1, with an IC50 of 182 nM.
|
-
- HY-B1258
-
|
Aminomethylbenzoic acid; α-Amino-p-toluic acid
|
Amino Acid Derivatives
|
Cancer
|
|
4-(Aminomethyl)benzoic acid is a competitive inhibitor of PepT1 and has antifibrinolytic activity .
|
-
- HY-16194
-
|
BAY o 1248
|
Others
|
Metabolic Disease
|
|
Emiglitate (BAY o 1248) is a potent, selective and competitive inhibitor of α-glucoside hydrolase.
|
-
- HY-101769
-
|
|
Dipeptidyl Peptidase
|
Cancer
|
|
UAMC00039 dihydrochloride is a potent, reversible and competitive dipeptidyl peptidase II inhibitor with an IC50 of 0.48 nM.
|
-
- HY-103533
-
-
- HY-122641B
-
-
- HY-19670
-
-
- HY-20558
-
-
- HY-107537
-
-
- HY-145678
-
|
|
Others
|
Metabolic Disease
|
|
α-HNJNAc is a potent, competitive hexosaminidases inhibitor without interfering with other glycosidases .
|
-
- HY-P4543
-
-
- HY-107710
-
-
- HY-B0385R
-
|
|
Proteasome
Factor Xa
|
Inflammation/Immunology
|
|
Gabexate (mesylate) (Standard) is the analytical standard of Gabexate (mesylate). This product is intended for research and analytical applications. Gabexate mesylate (FOY) is is a competitive and non-antigenic synthetic inhibitor of trypsin-like serine proteinases. Gabexate mesylate inhibits human thrombin, urokinase, plasmin, and Factor Xa with Kis of 0.97, 1.3, 1.6, and 8.5 μM, respectively. Gabexate mesylate binds to human and bovine tryptase with Kis of 3.4 nM and 18 μM, respectively. Gabexate mesylate exerts an anticoagulant effect on the clotting activity of thrombin and has anti-inflammatory effect by viainhibition of NF-κB, proinflammatory cytokines, and nitric oxide. Gabexate mesylate is used for pancreatitis and disseminated intravascular coagulation .
|
-
- HY-15066A
-
|
FG9065 disodium
|
iGluR
|
Neurological Disease
|
|
CNQX disodium (FG9065 disodium) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX disodium is a competitive non-NMDA receptor antagonist . CNQX disodium blocks the expression of fear-potentiated startle in rats .
|
-
- HY-121787
-
|
OLC20
|
Others
|
Others
|
|
OX1a (OLC20) is an Orco antagonist with non-competitive activity that inhibits the activation of oxygen odor receptors (ORs). OX1a is able to reduce the activation of ORs by competitively inhibiting the effects of Orco agonists. OX1a also shows non-competitive inhibition of odor molecules, which may affect the olfactory-mediated behavior of insects. Through structural optimization, OX1a analogs have shown higher antagonistic potency, indicating that this type of compound may have application potential in a wide range of insect species .
|
-
- HY-W424730
-
|
|
Others
|
Others
|
|
HA-966 hydrochloride is a glycine site antagonist of the NMDA receptor, exhibiting non-competitive antagonism on NMDA responses. HA-966 hydrochloride effectively blocks the enhancement of NMDA responses by glycine in a competitive manner. HA-966 hydrochloride plays a significant role in mediating the antagonist action at the glycine modulatory site of the NMDA receptor.
|
-
- HY-12660
-
|
|
Mps1
Apoptosis
|
Cancer
|
|
MPI-0479605 is a potent and selective ATP-competitive inhibitor of Mps1, with an IC50 of 1.8 nM.
|
-
- HY-16902
-
|
|
Syk
|
Inflammation/Immunology
|
|
RO9021 is an orally bioavailable, novel ATP-competitive inhibitor of SYK, with an average IC50 of 5.6 nM.
|
-
- HY-100152
-
|
SX 810
|
mAChR
|
Inflammation/Immunology
|
|
Beperidium iodide shows a competitive antagonistic effect against acetylcholine receptor with a pA2 of 7.93.
|
-
- HY-110399
-
-
- HY-101334
-
|
|
GlyT
|
Neurological Disease
|
|
MPDC is a potent and competitive inhibitor of the Na +-dependent high-affinity glutamate transporter in forebrain synaptosomes .
|
-
- HY-135405
-
-
- HY-139675
-
-
- HY-113894
-
|
|
Aurora Kinase
|
Cancer
|
|
Retreversine is an inactive control for Reversine. Reversine is a novel class of ATP-competitive Aurora kinase inhibitor .
|
-
- HY-N3906
-
-
- HY-122439
-
-
- HY-112736
-
-
- HY-135436
-
|
|
IGF-1R
|
Cancer
|
|
AG 538 is a potent, competitive inhibitor of IGF-1 receptor kinase, with an IC50 of 400 nM .
|
-
- HY-101334A
-
|
|
GlyT
|
Neurological Disease
|
|
MPDC hydrochloride is a potent and competitive inhibitor of the Na +-dependent high-affinity glutamate transporter in forebrain synaptosomes .
|
-
- HY-117256
-
-
- HY-12371
-
|
|
mGluR
|
Neurological Disease
|
|
VU0431316 is a potent and selective non-competitive antagonist of mGlu5 with an IC50 value of 24 nM .
|
-
- HY-P10657
-
-
- HY-124163
-
-
- HY-N0340
-
|
Hyoscine butylbromide; (-)-Scopolamine butylbromide; Butylscopolamine bromide
|
mAChR
|
Neurological Disease
|
|
Scopolamine butylbromide is a competitive antagonist of muscarinic acetylcholine receptor (mAChR) with an IC50 of 55.3 ± 4.3 nM.
|
-
- HY-149775
-
|
|
Bacterial
|
Infection
|
|
Urease-IN-10 (Conjugate 4) is a competitive Urease inhibitor, with an IC50 of 3.59±0.07 μM and a Ki of 7.45 μM. Urease-IN-10 is a conjugate consisting of Diclofenac (HY-15036) and Sulfanilamide (HY-B0242). Diclofenac-sulfanilamide inhibits the Jack bean urease(JBU) in a competitive manner .
|
-
- HY-120020
-
|
|
Others
|
Others
|
|
LY-395153 is an AMPA receptor enhancer with the activity of binding to AMPA receptors. LY-395153 can bind to natural and recombinant AMPA receptors, and its binding is affected by AMPA receptor agonists and can be competitively or non-competitively inhibited by some compounds. It is a useful probe for marking unique regulatory sites of AMPA receptors.
|
-
- HY-10992
-
-
- HY-15512A
-
|
OTS167 hydrochloride
|
MELK
|
Cancer
|
|
OTSSP167 (OTS167) hydrochloride is a highly potent and ATP-competitive MELK inhibitor with IC50 value of 0.41 nM.
|
-
- HY-13059
-
|
|
iGluR
|
Neurological Disease
|
|
SDZ 220-581 is an orally active, potent, competitive NMDA receptor antagonist with pKi value of 7.7 .
|
-
- HY-13059B
-
|
|
iGluR
|
Neurological Disease
|
|
SDZ 220-581 hydrochloride is an orally active, potent, competitive NMDA receptor antagonist with pKi value of 7.7 .
|
-
- HY-N1201
-
-
- HY-104009A
-
|
|
Histone Methyltransferase
|
Others
|
|
GSK2807 Trifluoroacetate is a potent, selective and SAM-competitive inhibitor of SMYD3, with a Ki of 14 nM and an IC50 of 130 nM .
|
-
- HY-13503
-
-
- HY-Y0504
-
|
Hegzadesil; Trimethylamine hydrochloric acid; Trimethylamine monohydrochloride
|
Endogenous Metabolite
Cholinesterase (ChE)
|
Metabolic Disease
|
|
Trimethylammonium chlorideIt is an endogenous metabolite that inhibits deacetylation. Trimethylammonium chlorideIs a non-competitive inhibitor of acetylcholinesterase .
|
-
- HY-W008350
-
|
Pachycarpine
|
nAChR
|
Neurological Disease
|
|
(+)-Sparteine is a natural alkaloid acting as a ganglionic blocking agent. (+)-Sparteine competitively blocks nicotinic ACh receptor in the neurons.
|
-
- HY-B0183A
-
|
|
Casein Kinase
|
Cancer
|
|
Ellagic acid hydrate is a natural antioxidant, and acts as a potent and ATP-competitive CK2 inhibitor, with an IC50 of 40 nM and a Ki of 20 nM .
|
-
- HY-14715
-
-
- HY-12054A
-
-
- HY-16015
-
|
ABC294640
|
SphK
|
Cancer
|
|
Opaganib (ABC294640) is a selective, competitive sphingosine kinase 2 (SK2) inhibitor with Ki of 9.8 μM.
|
-
- HY-15512
-
|
OTS167
|
MELK
|
Cancer
|
|
OTSSP167 (OTS167) is a highly potent and ATP-competitive MELK inhibitor with IC50 value of 0.41 nM.
|
-
- HY-110331
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
CCT241533 dihydrochloride is a potent and selective ATP competitive inhibitor of CHK2 with an IC50 of 3 nM and Ki of 1.16 nM .
|
-
- HY-B1304A
-
|
(+)-Lupinidine sulfate pentahydrate
|
nAChR
|
Neurological Disease
|
|
(+)-sparteine (sulfate pentahydrate) is a ganglionic blocking agent. (+)-Sparteine competitively blocks nicotinic ACh receptor in the neurons .
|
-
- HY-103351
-
-
- HY-10992A
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
AZD-7762 hydrochloride is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
|
-
- HY-133178
-
|
|
Ephrin Receptor
|
Cancer
|
|
Urolithin D is competitive and reversible antagonist of EphA receptors. Urolithin D exhibits intra-classes selectivity .
|
-
- HY-N11521
-
|
|
Tyrosinase
|
Cancer
|
|
7-Methoxy obtusifolin (Compound 4) is a competitive tyrosinase inhibitor with an IC50 of 7.0 μM .
|
-
- HY-149888
-
-
- HY-155600
-
|
β,γ-Methylene-GTP sodium
|
Others
|
Others
|
|
5′-Guanylyl methylenediphosphonate (sodium) is a GTP analogue and a specific, competitive inhibitor of the GTP reaction in protein synthesis .
|
-
- HY-P5188A
-
-
- HY-N12427
-
|
|
Tyrosinase
|
Cancer
|
|
Litchinol B (compound 2) is a non-competitive tyrosinase inhibitor with an inhibition constant of 5.70 μM .
|
-
- HY-16015A
-
|
ABC294640 hydrochloride
|
SphK
|
Cancer
|
|
Opaganib (ABC294640) hydrochloride is a selective, competitive sphingosine kinase 2 (SK2) inhibitor with Ki of 9.8 μM.
|
-
- HY-159628A
-
-
- HY-14806S1
-
|
MP-513-d4
|
Isotope-Labeled Compounds
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Teneligliptin-d4 is deuterium labeled Teneligliptin. Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM[1].
|
-
- HY-152032
-
|
|
Histone Demethylase
|
Cancer
|
|
LSD1-IN-23 is a competitive/non-competitive mixed inhibitor of lysine specific demethylase 1 (LSD1). LSD1-IN-23 has LSD1 inhibitory activity with an IC50 value of 0.58 μM. LSD1-IN-23 can be used for the research of neuroblastoma (NB) .
|
-
- HY-14731
-
|
|
ATM/ATR
|
Cancer
|
|
VE-821 is a potent ATP-competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM.
|
-
- HY-16060
-
|
ARN-509
|
Androgen Receptor
|
Cancer
|
|
Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM .
|
-
- HY-17353
-
|
|
Telomerase
Apoptosis
|
Cancer
|
|
BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay.
|
-
- HY-15465
-
|
|
CaMK
Autophagy
|
Cancer
|
|
KN-93 is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.
|
-
- HY-77195
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
Poloxime, a hydrolysis product of poloxin, is a non-ATP-competitive Plk1 inhibitor, with moderate Plk1 inhibitory activity.
|
-
- HY-13059A
-
|
|
iGluR
|
Neurological Disease
|
|
SDZ 220-581 Ammonium salt is an orally active, potent, competitive NMDA receptor antagonist with pKi value of 7.7 .
|
-
- HY-15465A
-
|
|
CaMK
Autophagy
|
Cancer
|
|
KN-93 hydrochloride is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.
|
-
- HY-B0183
-
-
- HY-50703
-
MK-2461
1 Publications Verification
|
c-Met/HGFR
|
Cancer
|
|
MK-2461 is a novel ATP-competitive multitargeted inhibitor of activated c-Met with a mean IC50 of 2.5 nM.
|
-
- HY-13447A
-
-
- HY-12428
-
-
- HY-15068
-
|
FG9202
|
iGluR
|
Neurological Disease
|
|
NBQX (FG9202) is a highly selective and competitive AMPA receptor antagonist. NBQX has neuroprotective and anticonvulsant activity .
|
-
- HY-112860
-
-
- HY-P1292A
-
|
|
PKG
|
Cancer
|
|
PKG inhibitor peptide TFA is an ATP-competitive inhibitor of cGMP-dependent protein kinase (PKG), with a Ki of 86 μM .
|
-
- HY-19433A
-
|
|
iGluR
|
Neurological Disease
|
|
(S)-ATPO is the (S)-enantiomer of ATPO, which is a competitive antagonist at GluR1-4 (AMPA-preferring) receptors .
|
-
- HY-W013386
-
-
- HY-146117
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp modulator 2 (Compound 27) is a potent, competitive, allosteric P-glycoprotein (P-gp) modulator .
|
-
- HY-146118
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp modulator 3 (Compound 37) is a potent, competitive, allosteric P-glycoprotein (P-gp) modulator .
|
-
- HY-101062
-
-
- HY-13447
-
-
- HY-154828
-
|
3′,5′-UDP
|
DNA/RNA Synthesis
|
Others
|
|
Uridine 3′,5′-diphosphate (3′,5′-UDP; Compound pUp) is a competitive RNase inhibitor .
|
-
- HY-129298
-
|
|
Aminopeptidase
|
Others
|
|
Amastatin is A slow, tightly bound, competitive inhibitor of aminopeptidase (AP) with an IC50 of 0.54 μg/mL for AP-A .
|
-
- HY-163974
-
-
- HY-105332
-
|
|
CRFR
|
Neurological Disease
|
|
CRA1000 is an orally active, selective and competitive CRF1 receptor antagonist with anxiolytic- and antidepressant-like properties .
|
-
- HY-162997
-
-
- HY-104050
-
M-31850
1 Publications Verification
|
Others
|
Metabolic Disease
|
|
M-31850 is a potent, selective and competitive β-hexosaminidase (Hex) inhibitor with IC50s of 6.0 µM and 3.1 µM for human HexA and human HexB, respectively. M-31850 also competitively inhibits β-N-acetyl-D-hexosaminidase OfHex2 with a Ki of 2.5 μM .
|
-
- HY-162059
-
|
|
Pim
Apoptosis
Caspase
|
Cancer
|
|
Pim-1 kinase inhibitor 10 (compound 13a) is a both competitive and non-competitive inhibitor of PIM-1/2 kinase. Pim-1 kinase inhibitor 10 can induce cell apoptosis and exhibits anticancer activity. Pim-1 kinase inhibitor 10 also induces caspase 3/7 activation .
|
-
- HY-N0219
-
|
(+)-Bicuculline; d-Bicuculline
|
GABA Receptor
|
Neurological Disease
|
|
Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca 2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .
|
-
- HY-161507
-
|
|
Carbonic Anhydrase
Cholinesterase (ChE)
|
Metabolic Disease
|
|
hCAI/II-IN-8 (Compound 8) is a hydrazide derivative based on 4-hydroxybenzaldehyde. hCAI/II-IN-8 primarily targets human carbonic anhydrase isomerase I (hCA I) and II (hCA II) for inhibition (IC50 = 21.35 ± 0.39 nM (hCA I); 7.12 ± 0.12 nM (hCA II)). hCAI/II-IN-8 inhibits AChE and BChE as well(IC50 = 46.27 ±0.75 nM (AChE); 43.38 ± 0.83 nM (BChE)). . .
|
-
- HY-110333
-
|
|
EGFR
|
Cancer
|
|
BMS-599626 dihydrochloride is a small molecule pan-HER (human epidermal growth factor receptor) kinase inhibitor. BMS-599626 dihydrochloride primarily targets HER1 (IC50=20 nmol/L) and HER2 (IC50=30 nmol/L) kinase activity in the HER family. BMS-599626 inhibits the kinase activity of HER1 and HER2 by competing with their ATP-binding sites, and can inhibit the downstream signaling pathway by blocking the heterodimer formation of HER1 and HER2. BMS-599626 dihydrochloride can be used to study the antitumor effects of multiple HER1 or HER2 overexpressed tumor models .
|
-
- HY-N0219R
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Bicuculline (Standard) is the analytical standard of Bicuculline. This product is intended for research and analytical applications. Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .
|
-
- HY-50877
-
|
GSK461364A
|
Polo-like Kinase (PLK)
|
Cancer
|
|
GSK461364 is a selective, reversible and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with a Ki value of 2.2 nM.
|
-
- HY-14394
-
|
NSC 231634; Casein Kinase II Inhibitor I
|
Casein Kinase
|
Cancer
|
|
TBB is a cell-permeable and ATP-competitive CK2 inhibitor with an IC50 of 0.15 μM for rat liver CK2.
|
-
- HY-15084
-
|
(+)-MK 801 Maleate
|
iGluR
|
Neurological Disease
|
|
Dizocilpine maleate (MK-801 maleate) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.
|
-
- HY-13949
-
|
SRPK inhibitor
|
SRPK
Virus Protease
|
Cancer
|
|
SRPIN340 is an ATP-competitive serine-arginine-rich protein kinase (SRPK) inhibitor, with a Ki of 0.89 μM for SRPK1.
|
-
- HY-B0165
-
-
- HY-B0686
-
|
|
Integrin
|
Cardiovascular Disease
|
|
Eptifibatide is a cyclic heptapeptide, acts as a competitive antagonist for the activated platelet glycoprotein IIb/IIIa receptor, with anti-platelet activity .
|
-
- HY-13823
-
-
- HY-100717
-
-
- HY-112945
-
|
|
Others
|
Metabolic Disease
|
|
MLS0315771 is a potent and biologically active competitive phosphomannose isomerase (MPI) inhibitor, with an IC50 ~1 μM and a Ki of 1.4 μM.
|
-
- HY-126253
-
-
- HY-P1017
-
-
- HY-136596
-
|
|
Drug Metabolite
|
Cancer
|
|
Apalutamide-COOH is a metabolite of Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM .
|
-
- HY-107699
-
|
|
iGluR
|
Neurological Disease
|
|
PPPA is a competitive NMDA receptor antagonist that displays moderate selectivity for NR2A-containing receptors .
|
-
- HY-W042648
-
|
|
Casein Kinase
|
Others
|
|
4,5,6,7-Tetrabromobenzimidazole is a selective and ATP competitive CK2 (casein kinase 2) inhibitor .
|
-
- HY-112392
-
|
|
GSK-3
|
Cancer
|
|
GSK-3 Inhibitor XIII is a potent and ATP-competitive GSK-3 inhibitor with a Ki of 24 nM .
|
-
- HY-20696
-
|
Tryptoline
|
5-HT Receptor
|
Metabolic Disease
|
|
Tetrahydro-β-carboline (Tryptoline) is a metabolite of tryptamine, also is a competitive serotonin reuptake inhibitor with an Ki value of 6.1 µM .
|
-
- HY-124204
-
|
|
iGluR
|
Neurological Disease
|
|
LY 274614 is an orally active, competitive NMDA receptor antagonist. LY 274614 can be used for Neurological Disease study .
|
-
- HY-P1315
-
|
Glycylglycyl-L-tyrosyl-L-arginine
|
Cathepsin
|
Others
|
|
Papain inhibitor (Glycylglycyl-L-tyrosyl-L-arginine) acts as an effective competitive inhibitor to papain, with a Ki of 9 μM at pH 6.2 .
|
-
- HY-78036
-
|
Citronic acid; Methylfumaric acid
|
Endogenous Metabolite
|
Others
|
|
Mesaconic acid is an active product that can be extracted from Saxifraga stolonifera. Mesaconic acid is used as a fire retardant and is a competitive inhibitor of fumarate reduction .
|
-
- HY-15410
-
|
|
iGluR
|
Others
|
|
Gacyclidine, a non competitive N-methyl-D-aspartate (NMDA) antagonist, can be used in the study of spinal cord injuries .
|
-
- HY-106769
-
-
- HY-W278777
-
|
|
Others
|
Others
|
|
Monohexyl phthalate is a competitive inhibitor towards UGT1A9, with an IC50 of 12.46 μM and a Ki of 7.47 μM .
|
-
- HY-131816
-
|
|
Others
|
Others
|
|
5'-dUMPS is a competitive inhibitor or regulator of enzymes that interacts with 2′-deoxypyrimidine-5′-monophosphate .
|
-
- HY-117672
-
|
|
Phosphatase
|
Others
|
|
L-671776 can be isolated from a fungal strain (ATCC 20928B), is a non-competitive inhibitor of IMPase .
|
-
- HY-15410A
-
|
|
iGluR
|
Others
|
|
Gacyclidine hydrochloride, a non competitive N-methyl-D-aspartate (NMDA) antagonist, can be used in the study of spinal cord injuries .
|
-
- HY-12042A
-
|
AS703026 hydrochloride; MSC1936369B hydrochloride
|
MEK
|
Cancer
|
|
Pimasertib hydrochloride is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor .
|
-
- HY-106769C
-
|
GR50360 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
Fluparoxan hydrochloride is an orally active, selective and competitive alpha 2-adrenoceptor antagonist. Fluparoxan hydrochloride is an anti-depressant agent .
|
-
- HY-117769
-
|
|
Fatty Acid Synthase (FASN)
|
Metabolic Disease
|
|
GSK837149A is a selective inhibitor of human Fatty Acid Synthase (FASN) targeting the KR domain. GSK837149A has reversible inhibition effect on FASN and selectivity for type I FASN (Ki=30 nM). GSK837149A is also a competitive inhibitor of NADPH and a non-competitive inhibitor of acetoacetyl-CoA. GSK837149A can be used for the research of obesity and breast cancer .
|
-
- HY-114511
-
|
|
Factor VIIa
|
Cardiovascular Disease
|
|
BMS-593214 is an active site-directed factor (F) VIIa inhibitor. BMS-593214 shows antithrombotic and antihaemostatic properties. BMS-593214 is a direct competitive inhibitor of human FVIIa and a non-competitive inhibitor of Viia-activated substrate FX. BMS-593214 prevents electroinduced carotid artery thrombosis (AT) and wire induced vena cava thrombosis (VT) .
|
-
- HY-101578
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
2614W94 is a selective, reversible inhibitor of monoamine oxidase-A with a competitive mechanism of inhibition and IC50 of 5 nM and Ki of 1.6 nM with serotonin as substrate.
|
-
- HY-14761
-
|
AS 602801
|
JNK
|
Cancer
|
|
Bentamapimod (AS 602801) is an ATP-competitive JNK inhibitor with IC50 of 80 nM, 90 nM, and 230 nM for JNK1, JNK2, and JNK3, respectively.
|
-
- HY-A0013
-
-
- HY-A0013A
-
-
- HY-15538
-
-
- HY-15646
-
-
- HY-13805
-
|
AGL 1879
|
Src
|
Cancer
|
|
PP2 is a reversible and ATP-competitive Src family kinases inhibitor with IC50s of 4 and 5 nM for Lck and Fyn, respectively.
|
-
- HY-B0322
-
|
Ro 4-2130
|
Bacterial
Antibiotic
|
Infection
|
|
Sulfamethoxazole (Ro 4-2130) is a sulfonamide bacteriostatic antibiotic, used for bacterial infections. Sulfonamides is a competitive antagonists of para-aminobenzoic acid (PABA) .
|
-
- HY-I0020
-
|
(-)-Narwedine; Narwedin
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Galanthaminone (Narwedin) is a competitive and reversible cholinesterase (AChE) inhibitor; is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments.
|
-
- HY-13298
-
|
|
Mps1
|
Cancer
|
|
Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM .
|
-
- HY-B1542A
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Benactyzine hydrochloride is a competitive BChE inhibitor with a Ki of 0.01 mM. Benactyzine hydrochloride is an anticholinergic drug. Benactyzine hydrochloride has the potential for organophosphate poisoning research .
|
-
- HY-19677
-
|
Ro 32-3555
|
MMP
|
Cancer
|
|
Cipemastat is a potent, competitive inhibitor of human collagenases 1, 2 and 3 with Kis of 3.0, 4.4 and 3.4 nM, respectively.
|
-
- HY-P0177
-
-
- HY-B0242S1
-
|
Sulphanilamide-d4
|
Bacterial
Antibiotic
|
Infection
|
|
Sulfanilamide-d4 is the deuterium labeled Sulfanilamide. Sulfanilamide is a competitive inhibitor for bacterial enzyme dihydropteroate synthetase with IC50 of 320 μM.
|
-
- HY-125643
-
|
|
Drug Metabolite
|
Cardiovascular Disease
|
|
Pitavastatin lactone is a major metabolite of Pitavastatin in humans. Pitavastatin is a potent competitive inhibitor of HMG-CoA reductase little metabolized in hepatic microsomes .
|
-
- HY-33914
-
-
- HY-B0686A
-
|
|
Integrin
|
Cardiovascular Disease
|
|
Eptifibatide monoacetate is a cyclic heptapeptide, acts as a competitive antagonist for the activated platelet glycoprotein IIb/IIIa receptor, with anti-platelet activity .
|
-
- HY-122933
-
-
- HY-120279A
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
CFI-400437 is an indolinone-derived, ATP-competitive kinase inhibitor with high selectivity for PLK4 (IC50 of 0.6 nM) .
|
-
- HY-121394
-
-
- HY-101353
-
|
(-)-LY 235959
|
iGluR
|
Neurological Disease
|
|
LY 235959 is a competitive N-methyl-D-aspartate (NMDA)-receptor antagonist. LY 235959 potentiates the anticonvulsant action of antiepileptics .
|
-
- HY-160124
-
|
|
FGFR
|
Cancer
|
|
Infigratinib-Boc is a derivative of Infigratinib containing a Boc (t-Butyloxy carbonyl) group. Infigratinib is an ATP-competitive pan-FGFR inhibitor .
|
-
- HY-127178
-
|
|
Phosphatase
|
Cancer
|
|
ML120 analog 1 (compound 1) is a competitive inhibitor with a Ki of 0.69 μM for Hematopoietic protein tyrosine phosphatase (HePTP) .
|
-
- HY-N2087
-
|
|
Others
|
Metabolic Disease
|
|
Ligupurpuroside A is an active product that can be extracted from Ligustrum robustum. Ligupurpuroside A acts as a natural inhibitor of lipase in a competitive manner .
|
-
- HY-138165
-
|
|
Others
|
Others
|
|
Ac-Phe-NH2 is a non-competitive inhibitor of polyubiquitin chain elongation at Ki value of 8 mM by destabilizing the active trimer .
|
-
- HY-105027
-
-
- HY-14486
-
|
PRT060128 potassium
|
P2Y Receptor
|
Inflammation/Immunology
|
|
Elinogrel (PRT060128) potassium is a reversible, competitive and orally active P2Y12 antagonist. Elinogrel potassium inhibits thrombosis .
|
-
- HY-112333
-
-
- HY-161680
-
|
|
Others
|
Cancer
|
|
Pyruvate Carboxylase-IN-4 (Compd 8V) is a potent and competitive Pyruvate Carboxylase inhibitor with an IC50 of 4.3 μM .
|
-
- HY-131812
-
|
2'-Deoxyadenosine 5'-O-thiophosphate
|
Others
|
Others
|
|
5'-dAMPS is an analogue of 5'-dAMP and thus a potential substrate, competitive inhibitor or regulator of enzymes that interact with dAMP .
|
-
- HY-128466
-
|
|
Biochemical Assay Reagents
|
Others
|
|
N-Biotinyl-L-cysteine is a biotinylated biochemical assay reagent, which is used to detect avidin and biotin through a competitive binding reaction .
|
-
- HY-116554
-
-
- HY-131810
-
|
|
Others
|
Others
|
|
5'-AMPS is an analogue of 5'-AMP and a substrate and competitive inhibitor or regulator of enzymes that interact with 5'-AMP .
|
-
- HY-164371
-
|
|
Androgen Receptor
|
Cancer
|
|
(+)-JJ-74-138, a novel non-competitive androgen receptor (AR) antagonist, is capable of inhibiting Enzalutamide-resistant CRPC .
|
-
- HY-B1542
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Benactyzine is a competitive BChE inhibitor with a Ki of 0.01 mM. Benactyzine is an anticholinergic drug. Benactyzine has the potential for organophosphate poisoning research .
|
-
- HY-112081A
-
|
|
Others
|
Others
|
|
BAY-707 acetate is a highly potent and selective substrate-competitive inhibitor of MTH1 with superior cellular target engagement and pharmacokinetic properties.
|
-
- HY-12042
-
|
AS703026; MSC1936369B
|
MEK
|
Cancer
|
|
Pimasertib (AS703026) is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor .
|
-
- HY-15251
-
-
- HY-13820
-
|
|
PERK
Autophagy
Apoptosis
|
Cancer
|
|
GSK2656157 is a selective and ATP-competitive inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) with an IC50 of 0.9 nM.
|
-
- HY-12465
-
|
Z-IL-CHO; GSI-XII; γ-Secretase inhibitor XII
|
Notch
γ-secretase
Apoptosis
|
Cancer
|
|
Z-Ile-Leu-aldehyde (Z-IL-CHO) is a potent and competitive peptide aldehyde inhibitor of γ-secretase and notch .
|
-
- HY-12524
-
Bikinin
1 Publications Verification
Abrasin
|
GSK-3
|
Others
|
|
Bikinin is a non-steroidal, ATP-competitive inhibitor of plant GSK-3/Shaggy-like kinases and activates BR (brassinosteroids) signaling.
|
-
- HY-16982
-
|
(-)-Cercosporamide
|
Fungal
MNK
PKC
|
Infection
Cancer
|
|
Cercosporamide is a highly potent, ATP-competitive PKC kinase inhibitor targeting to PKC1, with an IC50 of <50 nM and a Ki of <7 nM. Cercosporamide is a unique Mnk inhibitor.
|
-
- HY-18714
-
|
|
Bacterial
|
Others
|
|
BRD7116 competitively binds to bacterial DNA gyrase, exhibits an EC50 of 200 nM for LSCe cells, with cell-non-autonomous anti-leukemia activity.
|
-
- HY-101503
-
|
|
FABP
|
Metabolic Disease
|
|
HTS01037 is an inhibitor of fatty acid binding; and a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 with a Ki of 0.67 μM.
|
-
- HY-114349
-
-
- HY-W020215
-
-
- HY-15068A
-
|
FG9202 disodium
|
iGluR
|
Neurological Disease
|
|
NBQX disodium (FG9202 disodium) is a highly selective and competitive AMPA receptor antagonist. NBQX disodium has neuroprotective and anticonvulsant activity .
|
-
- HY-114503
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
NSAH is a reversible and competitive nonnucleoside ribonucleotide reductase (RR) inhibitor, with cell-free IC50 of 32 μM and cell-based IC50 of ~250 nM, respectively .
|
-
- HY-10243
-
|
MK-7009
|
HCV
HCV Protease
|
Infection
|
|
Vaniprevir (MK-7009) is a non-covalent competitive inhibitor of the hepatitis C virus (HCV) NS3/4A protease.
|
-
- HY-132907
-
-
- HY-101356
-
|
|
mGluR
|
Neurological Disease
|
|
CPCCOEt is a low affinity, selective, non-competitive and reversible antagonist of metabotropic glutamate receptor 1b (mGluR1b) .
|
-
- HY-W092533
-
|
|
Tryptophan Hydroxylase
|
Neurological Disease
|
|
6-Fluorotryptophan, a competitive inhibitor of tryptophan hydroxylase, produced a transient disruption of sleep in rats chronically implanted with EEG recording electrodes .
|
-
- HY-148394
-
|
|
Others
|
Infection
Cancer
|
|
UCK2 Inhibitor-1 (Compound 20874830-2) is a non-competitive UCK2 inhibitor with an IC50 of 4.7 µM .
|
-
- HY-149524
-
|
|
Sirtuin
|
Cancer
|
|
SIRT5 inhibitor 8 (compound 10) is a competitive inhibitor (IC50: 5.38 μM) of sirtuin SIRT5 with anticancer potential .
|
-
- HY-149525
-
|
|
Sirtuin
|
Cancer
|
|
SIRT5 inhibitor 9 (compound 14) is a competitive inhibitor (IC50: 4.07 μM) of sirtuin SIRT5 with anticancer potential .
|
-
- HY-129450
-
|
|
Others
|
Others
|
|
Ethyl-L-NIO hydrochloride is a potent and competitive human dimethylarginine dimethylaminohydrolase 1 (hDDAH-1) inhibitor with an IC50 of 70 μM and a Ki of 32 μM .
|
-
- HY-119582
-
|
|
Others
|
Inflammation/Immunology
|
|
Safironil is an antifibrotic compound. Safironil is a competitive inhibitor of collagen protein synthesis. Safironil reduces liver fibrogenesis by inhibiting HSC activation .
|
-
- HY-124230
-
|
|
15-PGDH
|
Metabolic Disease
|
|
15-PGDH-IN-3 (Compound 61) is a selective competitive inhibitor of 15-hydroxyprostaglandin dehydrogenase (15-PGDH) .
|
-
- HY-N8246
-
|
Uridine-2', 3'-cyclic monophosphate sodium salt
|
Others
|
Others
|
|
2',3'-cUMP sodium (Uridine-2', 3'-cyclic monophosphate sodium salt) is a competitive inhibitor of dip-nitrophenyl diphosphate hydrolysis .
|
-
- HY-131814
-
|
|
Others
|
Others
|
|
5'-dGMPS is an analogue of 5'-dGMP and a potential substrate, competitive inhibitor or regulator of enzymes that interact with 5'-dGMP .
|
-
- HY-131815
-
|
|
Others
|
Others
|
|
5'-dIMPS is an analogue of 5'-dIMP and a potential substrate, competitive inhibitor or regulator of enzymes that interact with 5'-dIMP .
|
-
- HY-131813
-
|
2'-Deoxycytidine 5'-monophosphate
|
Others
|
Others
|
|
5'-dCMPS is an analogue of 5'-dCMP and a potential substrate, competitive inhibitor or regulator of enzymes that interact with 5'-dCMP .
|
-
- HY-159741
-
|
FCE 24928
|
Others
|
Cancer
|
|
Minamestane (FCE 24928) is a selective and competitive aromatase inhibitor with an IC50 value of 45.7 nM. Minamestane is promising for research of postmenopausal breast cancer .
|
-
- HY-137279
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
Naloxone methiodide is a peripherally restricted, nonselective, and competitive opioid receptor antagonist. Naloxone methiodide does not penetrate the blood-brain barrier .
|
-
- HY-113730
-
|
|
Others
|
Others
|
|
VUF5834 is a non-peptide chemokine receptor CXCR3 antagonist with non-competitive antagonistic and inverse agonistic activities. VUF5834 blocks the effects of CXCL10 and CXCL11 on human CXCR3, exhibits non-competitive antagonistic and inverse agonistic properties to CXCR3, and, except for TAK-779, has a slightly lower affinity for rodent CXCR3 than for primate CXCR3.
|
-
- HY-15247
-
|
AZD2014
|
mTOR
Autophagy
Apoptosis
|
Cancer
|
|
Vistusertib (AZD2014) is an ATP competitive mTOR inhibitor with an IC50 of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes.
|
-
- HY-13966
-
|
2-DG; 2-Deoxy-D-arabino-hexose; D-Arabino-2-deoxyhexose
|
Hexokinase
HSV
Apoptosis
|
Cancer
|
|
2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase .
|
-
- HY-B0377
-
-
- HY-14664AS
-
-
- HY-100129
-
|
|
TRP Channel
|
Neurological Disease
|
|
JNJ-17203212 is a selective, potent and competitive TRPV1 antagonist. JNJ-17203212 is developed for researching pain management, such as migraine .
|
-
- HY-100005A
-
|
|
Mitochondrial Metabolism
|
Cancer
|
|
Fumarate hydratase-IN-2 sodium salt (compound 3) is a cell-permeable and competitive fumarate hydratase inhibitor (Ki=4.5 μM) with nutrient-dependent cytotoxicity .
|
-
- HY-19548A
-
|
|
Arginase
|
Metabolic Disease
|
|
BEC hydrochloride is a slow-binding and competitive Arginase II inhibitor with Ki of 0.31 μM and 30 nM at pH 7.5 and pH 9.5, respectively .
|
-
- HY-101053
-
|
Src Kinase Inhibitor 1; Src-l1
|
Src
|
Cancer
|
|
Src Inhibitor 1 is a potent, ATP-competitive and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.
|
-
- HY-19778
-
-
- HY-112654
-
-
- HY-15656S
-
-
- HY-N1470
-
|
|
Others
|
Metabolic Disease
|
|
Plantagoside, isolated from the seeds of Plantago asiatica, is a specific and non-competitive inhibitor for jack bean α-mannosidase, with an IC50 of 5 μM .
|
-
- HY-128379
-
|
|
Drug Metabolite
|
Others
|
|
Labetalone hydrochloride is an impurity of Labetalol. Labetalol is an orally active adrenoceptor blocking agent which is a competitive antagonist at both alpha- and beta-adrenoceptor sites .
|
-
- HY-P2271
-
|
|
Apelin Receptor (APJ)
|
Cancer
|
|
MM 54 (compound 5) is a competitive antagonist at APJ, with an IC50 of 93 nM. MM 54 behaves as a potent and selective inhibitor of apelin binding and APLNR activation .
|
-
- HY-108609
-
-
- HY-16168B
-
|
FE 200486 acetate hydrate
|
GnRH Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
Degarelix acetate hydrate (FE 200486 acetate hydrate) is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix acetate hydrate can be used for prostate cancer research .
|
-
- HY-116530
-
-
- HY-123617
-
-
- HY-112405
-
|
PD 159121
|
EGFR
|
Cancer
|
|
BPIQ-I (PD 159121) is a potent and ATP-competitive EGFR tyrosine kinase inhibitor.. BPIQ-I shows anti-proliferative actively .
|
-
- HY-103557
-
|
|
mGluR
|
Neurological Disease
|
|
Ro 64-5229 is a selective, non-competitive mGlu2 antagonist. RO 64-5229 reduces the presynaptic inhibitory effect of Neuroligin 1 .
|
-
- HY-17502R
-
-
- HY-B0009R
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Flumazenil (Standard) is the analytical standard of Flumazenil. This product is intended for research and analytical applications. Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
|
-
- HY-N2194R
-
|
|
Cytochrome P450
|
Cancer
|
|
Bergamottin (Standard) is the analytical standard of Bergamottin. This product is intended for research and analytical applications. Bergamottin is a potent and competitive CYP1A1 inhibitor with a Ki of 10.703 nM.
|
-
- HY-13050A
-
|
AZD-8931 fumarate
|
EGFR
|
Cancer
|
|
Sapitinib fumarate is a reversible, ATP competitive EGFR inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.
|
-
- HY-110287
-
Apcin
5 Publications Verification
|
APC
|
Cancer
|
|
Apcin, a ligand of Cdc20, is a potent and competitive anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity inhibitor. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. Apcin occupes the D-box-binding pocket on the side face of the WD40-domain and can prolong mitosis .
|
-
- HY-12134
-
Poloxin
3 Publications Verification
|
Polo-like Kinase (PLK)
|
Cancer
|
|
Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1) inhibitor that targets the polo-box domain, with an IC50 of appr 4.8 μM.
|
-
- HY-10512
-
|
AR 0133418; GSK 3β inhibitor VIII; AR 014418
|
GSK-3
|
Metabolic Disease
Cancer
|
|
AR-A014418 is a potent, selective and ATP-competitive GSK3β inhibitor (IC50=104 nM; Ki=38 nM) .
|
-
- HY-14711
-
|
|
Aurora Kinase
Autophagy
|
Cancer
|
|
Reversine is a novel class of ATP-competitive Aurora kinase inhibitor with IC50s of 400, 500 and 400 nM for Aurora A, Aurora B and Aurora C, respectively.
|
-
- HY-13806
-
XL388
3 Publications Verification
|
mTOR
Autophagy
|
Cancer
|
|
XL388 is a highly potent and ATP-competitive mTOR inhibitor with an IC50 of 9.9 nM. XL388 simultaneously inhibits both mTORC1 and mTORC2.
|
-
- HY-N0021
-
-
- HY-12503
-
CFM-2
1 Publications Verification
|
iGluR
|
Neurological Disease
Cancer
|
|
CFM-2 is a potent and selective non-competitive AMPAR antagonist . CFM-2 possesses anticonvulsant activity in various models of seizures .
|
-
- HY-19715
-
-
- HY-10366
-
BI-78D3
1 Publications Verification
|
JNK
|
Metabolic Disease
Cancer
|
|
BI-78D3 functions as a substrate competitive inhibitor of JNK, inhibit the JNK kinase activity (IC50=280 nM).
|
-
- HY-14929A
-
|
GR181413A
|
Others
|
Others
|
|
Migalastat hydrochloride (GR181413A) is a potent and competitive inhibitor of α-galactosidase A (α-Gal A) with an IC50 of 0.04 μM for human α-Gal A.
|
-
- HY-15345
-
|
THU dihydrate; NSC-112907 dihydrate
|
Others
|
Cancer
|
|
Tetrahydrouridine dihydrate (THU dihydrate) is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine.
|
-
- HY-112113
-
|
SEL201-88; SEL-201
|
MNK
|
Cancer
|
|
SLV-2436 is a highly potent and ATP-competitive inhibitor of MNK1 and MNK2 with IC50s of 10.8 nM and 5.4 nM, respectively.
|
-
- HY-17502S
-
-
- HY-112914
-
|
|
mTOR
Autophagy
|
Cancer
|
|
mTOR inhibitor-1 (Compound C-4) is an ATP-Competitive mTOR inhibitor which can suppress cells proliferation and inducing autophagy .
|
-
- HY-N0575
-
-
- HY-108643
-
|
|
MAPKAPK2 (MK2)
|
Cancer
|
|
CMPD1 is a selective and non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor with apparent Ki (Ki app) of 330?nM .
|
-
- HY-N7114A
-
|
|
Bacterial
Antibiotic
|
Infection
Metabolic Disease
|
|
Chloramphenicol succinate sodium is a proagent of Chloramphenicol, with Haemotoxicity. Chloramphenicol succinate is a competitive substrate and inhibitor of succinate dehydrogenase (SDH) that is the possible reason for its toxicity .
|
-
- HY-135103
-
|
T-βMCA sodium
|
FXR
|
Cancer
|
|
Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM .
|
-
- HY-111184
-
|
|
PI3K
|
Cancer
|
|
PIK-108 is a non-ATP competitive, allosteric p110β/p110δ selective inhibitor .
|
-
- HY-115748
-
-
- HY-N3394
-
|
|
Others
|
Infection
|
|
Lecanoric acid is a histidine-decarboxylase inhibitor isolated from fungus. The inhibition by lecanoric acid is competitive with histidineand noncompetitive with pyridoxal phosphate. Lecanoric acid did not inhibit aromatic amino acid decarboxylase .
|
-
- HY-15345A
-
|
THU; NSC-112907
|
Others
|
Cancer
|
|
Tetrahydrouridine dihydrate is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine .
|
-
- HY-119024
-
|
|
Others
|
Infection
|
|
BCI-137 is a competitive AGO2 inhibitor, with an IC50 of 342 μM. BCI-137 tightly binds to several residues of the Mid domain .
|
-
- HY-107716
-
|
|
iGluR
|
Neurological Disease
|
|
Ro 8-4304 hydrochloride is a potent NMDA receptor antagonist. Ro 8-4304 hydrochloride is a NR2B selective, non-competitive, voltage-independent antagonist .
|
-
- HY-19797
-
|
|
p97
|
Cancer
|
|
ML241 is a potent, selective and competitive p97 ATPase inhibitor with an IC50 of 0.11 μM. ML241 can be used for the research of cancer .
|
-
- HY-156350
-
|
|
Others
|
Cancer
|
|
SGC-STK17B-1 is an ATP-competitive and selective STK17B inhibitor (IC50: 34 nM, KD: 5.6 nM) .
|
-
- HY-105163
-
|
MPV-2213ad
|
Cytochrome P450
|
Endocrinology
|
|
Finrozole (MPV-2213ad) is a nonsteroidal, orally active and competitive aromatase enzyme inhibitor. Finrozole can be used for urinary symptoms research .
|
-
- HY-161048
-
|
|
Others
|
Others
|
|
PDH E1-IN-1 (compound 24) is a selective TPP-competitive PDH E1 with an IC50 value of 0.99 μM .
|
-
- HY-117830
-
|
|
Phosphatase
|
Endocrinology
|
|
CX08005 is a competitive PTP1B inhibitor. CX08005 can directly enhance the action of insulin in vivo and in vitro and improve insulin resistance .
|
-
- HY-111199
-
|
|
FAAH
|
Neurological Disease
|
|
JP83 is an irreversible fatty acyl amide hydrolase (FAAH) inhibitor with an IC50 of 1.6 nM in competitive activity-based protein profiling (ABPP) experiments .
|
-
- HY-157829
-
|
Me-PEA
|
Endogenous Metabolite
|
Cancer
|
|
(R)-Palmitoyl-(2-methyl)ethanolamide (Me-PEA) is a competitive inhibitor of [3 H]-AEA metabolism with a Ki value of 6.6 μM .
|
-
- HY-112487
-
|
|
Acyltransferase
|
Endocrinology
|
|
Sandoz 58-035 is a competitive inhibitor of cholesterol acyltransferase (ACAT). Sandoz 58-035 effectively inhibits (>98%) hormonally stimulated cholesterol esterification in cells .
|
-
- HY-122148
-
-
- HY-164264
-
|
|
iGluR
|
Neurological Disease
|
|
Caged MK801 (cMK801) is a selective, non-competitive, irreversible NMDA receptor open-channel blocker. NVOC cages are neuro pharmocologically compatible .
|
-
- HY-104009
-
|
|
Others
|
Cancer
|
|
GSK2807 is a potent and selective SAM-competitive inhibitor of SMYD3, exhibiting a Ki value of 14 nM, and it may be useful for cancer treatment by preventing the methylation of MEKK2.
|
-
- HY-111094
-
|
|
Others
|
Cancer
|
|
NPD7155 is a purine-based competitive inhibitor of MTH1, designed to target cancer cells while exhibiting off-target effects that contribute to its cytotoxicity.
|
-
- HY-10005
-
|
HMR-1275; Alvocidib; L86-8275
|
CDK
Autophagy
HIV
Apoptosis
|
Cancer
|
|
Flavopiridol (Alvocidib) is a broad spectrum and competitive inhibitor of CDKs, inhibiting CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.
|
-
- HY-10193
-
|
|
JAK
|
Cancer
|
|
AZD-1480 is an ATP-competitive inhibitor of JAK1 and JAK2 with IC50s of 1.3 nM and <0.4 nM, respectively .
|
-
- HY-70035
-
|
FXV673
|
Factor Xa
|
Cardiovascular Disease
|
|
Otamixaban(FXV673) is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa.
|
-
- HY-15248
-
|
|
mTOR
Autophagy
|
Cancer
|
|
GDC-0349 is a potent and selective ATP-competitive mTOR inhibitor with a Ki of 3.8 nM. GDC-0349 inhibits of both mTORC1 and mTORC2 complexes.
|
-
- HY-14574
-
|
|
Aurora Kinase
VEGFR
|
Cancer
|
|
PF-03814735 is a potent, orally available, ATP-competitive and reversible aurora A and aurora B inhibitor with IC50s of 0.8 and 0.5 nM, respectively.
|
-
- HY-10889
-
|
SCH-420814
|
Adenosine Receptor
|
Neurological Disease
|
|
Preladenant is a potent and competitive antagonist of the human adenosine A2A receptor with a Ki of 1.1 nM and has over 1000-fold selectivity over other adenosine receptors.
|
-
- HY-B0134
-
-
- HY-100844
-
|
|
MAP3K
Apoptosis
|
Cancer
|
|
GS-444217 is a potent, orally available and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87 nM .
|
-
- HY-101736
-
AMG9810
4 Publications Verification
|
TRP Channel
|
Neurological Disease
|
|
AMG9810 is a selective and competitive vanilloid receptor 1 (TRPV1) antagonist with IC50 values of 24.5 and 85.6 nM for human and rat TRPV1, repectively.
|
-
- HY-101760
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively .
|
-
- HY-12432A
-
|
ASP2215 hemifumarate
|
FLT3
TAM Receptor
|
Cancer
|
|
Gilteritinib (ASP2215) hemifumarate is a potent and ATP-competitive FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.
|
-
- HY-B1655
-
|
R 6218; Redeptin
|
Calcium Channel
|
Neurological Disease
|
|
Fluspirilene is a non-competitive antagonist of L-type calcium channels with an IC50 of 0.03 μM. Fluspirileneis a long-acting injectable depot antipsychotic agent used for schizophrenia.
|
-
- HY-12806
-
|
|
EGFR
|
Cancer
|
|
AG1557 is a specific and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, has a pIC50 value of 8.194 .
|
-
- HY-112080
-
|
|
Histone Methyltransferase
|
Cancer
|
|
BAY-6035 is a potent, selective and substrate-competitive inhibitor of SMYD3. BAY-6035 inhibits methylation of MEKK2 peptide with an IC50 of 88 nM .
|
-
- HY-50949A
-
|
|
IKK
|
Inflammation/Immunology
|
|
Bay 65-1942 R form is the less active R-form of Bay 65-1942. Bay 65-1942 is an ATP-competitive and selective IKKβ inhibitor.
|
-
- HY-115194
-
|
|
Aminopeptidase
Bacterial
|
Infection
|
|
Amastatin hydrochloride is a slow, tight binding, competitive aminopeptidase (AP) inhibitor with Ki values of 0.26 nM, 30 nM, 52 nM for Aeromonas aminopeptidase, cytosolic leucine aminopeptidase, microsomal aminopeptidase .
|
-
- HY-136548
-
-
- HY-16060S
-
|
ARN-509-d4
|
Androgen Receptor
|
Cancer
|
|
Apalutamide-d4 is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[1].
|
-
- HY-133117A
-
|
|
IKK
|
Cancer
|
|
(Rac)-BAY-985 (Compound Example 100.01) is a potent, ATP-competitive and selective TBK1 inhibitor with an IC50 of 1.5 nM. Antitumor efficacy .
|
-
- HY-112355
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase inhibitor-2 is a selective and ATP-competitive Aurora kinase inhibitor with IC50s of 310 nM and 240 nM for Aurora A and Aurora B, respectively .
|
-
- HY-19519A
-
|
DF 2156A
|
CXCR
|
Infection
Inflammation/Immunology
|
Ladarixin sodium (DF 2156A) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin sodium can be used for the research of COPD and asthma .
|
-
- HY-17502S1
-
-
- HY-116559
-
|
|
Others
|
Others
|
|
TIBI is a potent and ATP-competitive inhibitor of Rio1 (IC50: 0.09 μM, Ki: 0.05 μM). TIBI enhances the thermostability of the enzyme Rio1 .
|
-
- HY-N0793A
-
-
- HY-121813
-
|
BW 234U
|
Others
|
Neurological Disease
|
|
Rimcazole (BW 234U) is a potent antipsychotic agent. Rimcazole also is a competitive antagonist of sigma sites. Rimcazole can be used for the research of acute schizophrenic diseases .
|
-
- HY-10193A
-
|
|
JAK
|
Cancer
|
|
(1R)-AZD-1480 is the (1R) chiral isomer of AZD-1480, an ATP competitive JAK1 and JAK2 inhibitor .
|
-
- HY-131811
-
|
5'-O-Thiophosphonocytidine
|
Others
|
Others
|
|
5’CMPS (5’-O-Thiophosphonocytidine) is a 5’-CMP analog that is a potential competitive inhibitor or regulator of enzymes that interact with cytidine 5’phosphate .
|
-
- HY-162909
-
|
|
Tyrosinase
|
Metabolic Disease
|
|
Tyrosinase-IN-38 (compound 6b) is a competitive Tyrosinase inhibitor with IC50 value of 25.82 μM. Tyrosinase-IN-38 has antioxidant activity .
|
-
- HY-135404R
-
|
|
Drug Metabolite
|
Cardiovascular Disease
Cancer
|
|
Anhydrosimvastatin (Standard) is the analytical standard of Anhydrosimvastatin. This product is intended for research and analytical applications. Anhydrosimvastatin (Impurity C) is an impurity of Simvastatin. Simvastatin is a competitive inhibitor of HMG-CoA reductase .
|
-
- HY-100412A
-
|
AZD-0865 mesylate
|
Proton Pump
|
Cancer
|
|
Linaprazan mesylate can inhibit H+,K+ -ATPase in the stomach through K+ competitive binding. (IC 50: 1.0 ± 0.2 μM), it has a strong inhibitory effect on acid.
|
-
- HY-N4110
-
|
|
Cytochrome P450
NF-κB
Interleukin Related
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Friedelin is derived from the leaves of Maytenus ilicifolia (Mart). Friedelin is an orally active non-competitive inhibitor of CYP3A4, with IC50 and Ki values of 10.79 μM and 6.16 μM, respectively. Friedelin is also a competitive inhibitor of CYP2E1, with IC50 and Ki values of 22.54 μM and 18.02 μM, respectively. Friedelin can be used in research related to inflammation, neurological diseases, and metabolic disorders .
|
-
- HY-123311
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
CP59430 is an azide analog of the α-adrenaline receptor antagonist Prazosin (HY-B0193). P59430 behaves as a competitive antagonist of α1-adrenaline receptor before photolysis. After photolysis, it specifically and irreversibly labels α1-adrenaline receptor and exhibits non-competitive antagonist activity. CP59430 can be used for the study of receptor molecular characterization .
|
-
- HY-14660
-
|
GSK2118436A; GSK2118436
|
Raf
|
Cancer
|
|
Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-Raf V600E, respectively .
|
-
- HY-15663
-
|
|
PAK
|
Cancer
|
|
IPA-3 is a selective non-ATP competitive PAK1 inhibitor with IC50 of 2.5 μM, and shows no inhibition to group II PAKs (PAKs 4-6).
|
-
- HY-15313
-
|
|
Histone Demethylase
|
Cancer
|
|
CBB1007 is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
|
-
- HY-10458
-
|
VS-6062 besylate
|
FAK
Pyk2
|
Cancer
|
|
PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively .
|
-
- HY-15687
-
|
|
ROCK
|
Metabolic Disease
|
|
SAR407899 hydrochloride is a selective, potent and ATP-competitive ROCK inhibitor, with an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively.
|
-
- HY-15313B
-
|
|
Histone Demethylase
|
Cancer
|
|
CBB1007 Hcl is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
|
-
- HY-12432
-
|
ASP2215
|
FLT3
TAM Receptor
|
Cancer
|
|
Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC50s of 0.29 nM/0.73 nM, respectively.
|
-
- HY-13050
-
|
AZD-8931
|
EGFR
|
Cancer
|
|
Sapitinib (AZD-8931) is a reversible, ATP competitive EGFR inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.
|
-
- HY-15313C
-
|
|
Histone Demethylase
|
Cancer
|
|
CBB1007 trihydrochloride is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
|
-
- HY-N0793
-
-
- HY-110231
-
-
- HY-116564
-
|
|
Parasite
GABA Receptor
|
Infection
|
|
Lotilaner is a parasiticide, acts as a potent non-competitive antagonist of insects GABACl receptors, with an IC50 of 23.84 nM for Drosophila melanogaster GABA receptor. No effect on a dog GABAA receptor .
|
-
- HY-124330
-
|
(E)-Tripolin A
|
Aurora Kinase
|
Others
|
Tripolin A ((E)-Tripolin A) is a specific non-ATP competitive Aurora A kinase inhibitor, with IC50 values of 1.5 μM and 7 μM for Aurora A and Aurora B, respectively .
|
-
- HY-118660
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Anhydrotetracycline hydrochloride, a tetracycline biosynthetic precursor, is a potent competitive broad-spectrum tetracycline destructase enzymes inhibitor. Anhydrotetracycline hydrochloride is an effector for tetracycline controlled gene expression systems in eukaryotic cells .
|
-
- HY-P1083
-
|
|
Dynamin
|
Neurological Disease
|
|
Dynamin inhibitory peptide competitively blocks binding of dynamin to amphiphysin, thus preventing endocytosis. Dynamin inhibitory peptide blocks the dopamine D3 effect on GABAA receptors .
|
-
- HY-131449
-
|
|
Adrenergic Receptor
|
Others
|
|
Terazosin dimer impurity dihydrochloride, a dimer of Terazosin, is an impurity of Terazosin. Terazosin is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist .
|
-
- HY-138489
-
|
Lats-IN-1
|
YAP
|
Others
|
|
TRULI (Lats-IN-1) is a potent and ATP-competitive inhibitor of Lats1 and Lats2 kinases. TRULI promotes Yap-dependent proliferation in postmitotic mammalian tissues .
|
-
- HY-P1628
-
|
|
GnRH Receptor
|
Metabolic Disease
|
|
Ganirelix is a competitive and selective gonadotropin releasing hormone (GnRH) antagonist. Ganirelix prevents endogenous GnRH from inducing luteinising hormone (LH) and follicle stimulating hormone relea .
|
-
- HY-116675
-
|
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Sulmazole is a cardiotonic agent. Sulmazole has competitive inhibitory for A1 adenosine receptor. Sulmazole can improve cardiac index and reduce pulmonary capillary wedge pressure .
|
-
- HY-Y1787
-
|
|
Apoptosis
|
Neurological Disease
|
|
Dimethyl malonate is a competitive inhibitor of succinate dehydrogenase (SDH). Dimethyl malonate is able to cross the blood-brain barrier and hydrolyse to malonate. Dimethyl malonate reduces neuronal apoptosis .
|
-
- HY-152194
-
|
|
Tyrosinase
|
Cancer
|
|
Tyrosinase-IN-10 (Compound 23) is a partially competitive tyrosinase inhibitor with an IC50 of 1.6 μM against tyrosinase activity from human melanoma cell lysates .
|
-
- HY-115748A
-
-
- HY-153176
-
|
|
Ras
|
Cancer
|
|
PAT-IN-1 is a protein acyl transferases (PAT) inhibitor. PAT-IN-1 competitively inhibits Erf2 autopalmitoylation (WO2017011518A1; compound 13) .
|
-
- HY-153177
-
|
|
Ras
|
Cancer
|
|
PAT-IN-2 is a protein acyl transferases (PAT) inhibitor. PAT-IN-2 competitively inhibits Erf2 autopalmitoylation (WO2017011518A1; compound 25) .
|
-
- HY-121966
-
|
Riparin III
|
Others
|
Cancer
|
|
Riparin is a nonspecific smooth muscle relaxant. Riparin inhibits CaCl2-induced contractions in a reversible and non-competitive manner and can be used in spasmolytic studies .
|
-
- HY-P1264F1
-
|
|
nAChR
|
Neurological Disease
|
|
Biotin-α-Bungarotoxin is the Biotin labelled α-Bungarotoxin (HY-P1264). α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs) .
|
-
- HY-W168754
-
|
|
Others
|
Others
|
|
DB28 is a novel MR1 ligand. DB28 decreases cell surface expression of MR1 and competitively inhibits activation of MAIT cells by agonist ligands .
|
-
- HY-162149
-
|
|
Bacterial
|
Infection
|
|
Urease-IN-12 (compound 5e) is a competitive urease inhibitor (IC50: 0.35 μM) with the potential to inhibit gastritis and peptic ulcer caused by Helicobacter pylori .
|
-
- HY-116208
-
|
KU-1257
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Dalcotidine (KU-1257) is an orally active and competitive histamine H2 receptor antagonist. Dalcotidine promotes the healing of chronic ulcers and inhibits gastric acid secretion .
|
-
- HY-N1201S
-
-
- HY-19156A
-
|
ICI-D 6888 hydrochloride
|
Angiotensin Receptor
|
Others
|
|
ZD-6888 hydrochloride (ICI-D 6888 hydrochloride) is an antagonist for angiotensin II, which competitively inhibits the angiotensin II-mediated release of renin, affects the renal structure and function .
|
-
- HY-117595
-
|
|
FAK
FGFR
Apoptosis
|
Cancer
|
|
PHM16 is an ATP competitive inhibitor of FAK and FGFR2 (IC50: 0.4 μM and 0.37 μM, respectively), with direct potent anti-angiogenic activity .
|
-
- HY-13450
-
|
|
JAK
EGFR
|
Inflammation/Immunology
|
|
ZM 449829 is a potent, selective and ATP competitive inhibitor of JAK3, with a pIC50 of 6.8. ZM 449829 will be useful pharmacological tools for the investigation of the JAK3 .
|
-
- HY-70044
-
|
GSK-1070916A
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with Kis of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A.
|
-
- HY-10459
-
|
VS-6062
|
FAK
Pyk2
|
Cancer
|
|
PF-562271 (VS-6062) is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively .
|
-
- HY-15716
-
|
|
Ras
Apoptosis
|
Cancer
|
|
Kobe0065 is a novel and effective inhibitor of Ras-Raf interaction, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46±13 μM.
|
-
- HY-N0598
-
|
20(S)-Ginsenoside F1
|
Cytochrome P450
Endogenous Metabolite
|
Cancer
|
|
Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.
|
-
- HY-19712
-
LJH685
2 Publications Verification
|
Ribosomal S6 Kinase (RSK)
Apoptosis
|
Cancer
|
|
LJH685 is a potent, ATP-competitive and selective RSK inhibitor, inhibits RSK1, 2, and 3 biochemical activities with IC50s of 6, 5, 4 nM, respectively .
|
-
- HY-100011
-
SR-3029
2 Publications Verification
|
Casein Kinase
|
Cancer
|
|
SR-3029 is a potent and ATP competitive CK1δ and CK1ε inhibitor, with IC50s of 44 nM and 260 nM, respectively, and Kis of 97 nM for both kinases.
|
-
- HY-100412
-
|
AZD0865
|
Proton Pump
|
Cancer
|
|
Linaprazan (AZD0865) can inhibit H+,K+ -ATPase in the stomach through K+ competitive binding. (IC 50: 1.0 ± 0.2 μM), it has a strong inhibitory effect on acid.
|
-
- HY-107723
-
-
- HY-107702
-
|
|
iGluR
|
Neurological Disease
|
|
CGP 37849 is a potent, competitive and orally active N-methyl-D-aspartate (NMDA) receptor antagonist. CGP 37849 is an anticonvulsant in rodents and has antidepressant and anxiolytic-like effects .
|
-
- HY-101381
-
|
AF-DX 116
|
mAChR
|
Neurological Disease
Metabolic Disease
|
|
Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively .
|
-
- HY-114702
-
M77976
1 Publications Verification
|
PDHK
|
Metabolic Disease
|
|
M77976 is a specific ATP-competitive inhibitor of PDK4 (pyruvate dehydrogenase kinase isoforms 4), with an IC50 of 648 μM. M77976 is potential for the research of obesity and diabetes .
|
-
- HY-20403
-
|
VS-6062(hydrochloride)
|
FAK
Pyk2
|
Cancer
|
|
PF-562271 (VS-6062) hydrochloride is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively .
|
-
- HY-16958
-
|
|
Antibiotic
|
Inflammation/Immunology
|
|
PD 404182 is a potent and competitive inhibitor of human dimethylarginine dimethylaminohydrolase 1 (DDAH1), with an IC50 of 9 μM. PD 404182 exhibits antiangiogenic and antiviral activity in vitro .
|
-
- HY-128380
-
|
N-(2-Chloroethyl)dibenzylamine hydrochloride
|
Adrenergic Receptor
|
Metabolic Disease
|
|
Dibenamine hydrochloride is a competitive and irreversible adrenergic blocking agent and is known to modify the pharmacological effects of epinephrine. Dibenamine hydrochloride cause a significant increase in the rate of destruction of I-epinephrine in the mouse .
|
-
- HY-136548A
-
|
TFV-DP triethylamine
|
Reverse Transcriptase
|
Infection
Inflammation/Immunology
|
|
Tenofovir diphosphate triethylamine (TFV-DP triethylamine) is a competitive DNA polymerases inhibitor (with respect to dATP) and a substrate of HIV type 1 (HIV-1) reverse transcriptase (RT) .
|
-
- HY-15159
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
Cyclapolin 9 is a potent, selective and ATP-competitive polo-like kinase 1 (PLK1) inhibitor with an IC50 of 500 nM. Cyclapolin 9 is inactive against other kinases .
|
-
- HY-79457
-
|
|
NO Synthase
HSV
|
Infection
Inflammation/Immunology
|
|
S-Methylisothiourea sulfate is a potent, selective and competitive inhibitor of inducible nitric oxide synthase (iNOS). S-Methylisothiourea sulfate exerts beneficial effects in rodent models of septic shock .
|
-
- HY-119611A
-
-
- HY-19519
-
|
DF 2156A free base
|
CXCR
|
Inflammation/Immunology
Cancer
|
Ladarixin (DF 2156A free base) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin can be used for the research of COPD and asthma .
|
-
- HY-B0199A
-
|
RS 61443 hydrochloride; TM-MMF hydrochloride
|
Endogenous Metabolite
Bacterial
|
Cancer
|
|
Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD) type I/II with IC50s of 39 nM and 27 nM, respectively.
|
-
- HY-115740
-
|
Ara-CTP
|
DNA/RNA Synthesis
|
Cancer
|
|
Cytarabine triphosphate (Ara-CTP), an active metabolite of Cytarabine, is a competitive inhibitor of DNA synthesis. Intracellular Cytarabine triphosphate levels can be used to predict chemosensitivity of leukemic blasts to Cytarabine .
|
-
- HY-135189
-
|
|
Others
|
Others
|
|
6-Aminophenanthridine inhibits the protein folding activity of the ribosome (PFAR). 6-Aminophenanthridine competitively occludes the protein substrates from binding to rRNA and thereby inhibits PFAR .
|
-
- HY-108479
-
|
SR140333
|
Neurokinin Receptor
|
Neurological Disease
|
|
Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK1 receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation .
|
-
- HY-146154
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-58 (Compound 4a) is a potent, ATP-competitive, and selective EGFR inhibitor. EGFR-IN-58 shows potent cytotoxicity against melanoma, colon, and blood cancers .
|
-
- HY-151150
-
|
|
Parasite
|
Infection
|
|
Trypanothione synthetase-IN-2 (Compound 3) is a competitive Leishmania infantum trypanothione synthetase (TryS) inhibitor with an IC50 of 5.4 μM when triamine spermidine is as polyamine S .
|
-
- HY-151148
-
|
|
Parasite
|
Infection
|
|
Trypanothione synthetase-IN-1 (Compound 1) is a competitive Leishmania infantum trypanothione synthetase (TryS) inhibitor with an IC50 of 14.8 μM when triamine spermidine is as polyamine S .
|
-
- HY-139196
-
-
- HY-119242
-
-
- HY-W012888
-
|
(-)-Leucinol
|
Others
|
Others
|
|
D-Leucinol is the isomer of L-Leucinol (HY-W015876), and can be used as an experimental control. L-Leucinol ((+)-Leucinol) is a competitive aminopeptidase inhibitor with Ki value of 17 μM .
|
-
- HY-76409
-
|
FXV673 hydrochloride
|
Factor Xa
|
Inflammation/Immunology
|
|
Otamixaban (FXV673) is a potent, selective, rapid-acting, competitive, and reversible fXa inhibitor (Ki=0.5 nM) that effectively inhibits both free and prothrombinase-bound fXa .
|
-
- HY-155837
-
|
|
Others
|
Metabolic Disease
|
|
hPL-IN-2 (compound 2u) is a potent, reversible, and non-competitive inhibitor of pancreatic lipase (IC50: 1.63 μM) and can be used in anti-obesity research .
|
-
- HY-N9685
-
|
D-(+)-Digitoxose
|
Biochemical Assay Reagents
|
Metabolic Disease
|
|
Digitoxose (D-(+)-Digitoxose), a natural product, specifically and competitively inhibits glucose-stimulated insulin release from islets in lean and obese mice. Digitoxose can be used in diabetes research .
|
-
- HY-103366
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
NSC 109555 ditosylate is a potent, selective, ATP-competitive checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 240 nM. NSC 109555 ditosylate can be used for the research of cancer .
|
-
- HY-120650
-
|
|
FAAH
|
Infection
|
|
CAY10435 is a β-ketooxazapyridine, selective FAAH inhibitor with antimicrobial activity. CAY10435 binds non-competitively to the FAAH of Dictyostelium discoideum with a Kd value of 0.57 nM .
|
-
- HY-163549
-
-
- HY-W010510R
-
|
|
Endogenous Metabolite
Arginase
|
Metabolic Disease
|
|
DL-Norvaline (Standard) is the analytical standard of DL-Norvaline. This product is intended for research and analytical applications. DL-Norvaline, a derivative of L-norvaline, L-norvaline is a non-competitive inhibitor of arginase.
|
-
- HY-13100A
-
|
|
Others
|
Metabolic Disease
|
|
(S)-PF 03716556 is a K+-competitive acid blocker with gastric acid pump inhibitory activity. (S)-PF 03716556 can be used to inhibit disease states mediated by acid pump inhibitory activity .
|
-
- HY-13303
-
|
|
MEK
|
Cancer
|
|
RO 4927350 is a potent and selective non-ATP-competitive MEK1/2 inhibitor. RO 4927350 exhibits significant antitumor efficacy in a broad spectrum of tumor models .
|
-
- HY-50697
-
|
|
P2X Receptor
|
Neurological Disease
|
|
A-740003 is a potent, selective and competitive P2X7 receptor antagonist with IC50 values are 18 and 40 nM for rat and human P2X7 receptors, respectively.
|
-
- HY-15513
-
|
|
DAPK
|
Cancer
|
|
TC-DAPK 6 is a potent, ATP-competitive, and highly selective DAPK inhibitor (IC50=69 and 225 nM against DAPK1 and DAPK3, respectively, with 10 μM ATP).
|
-
- HY-10017
-
|
|
CXCR
|
Inflammation/Immunology
Endocrinology
|
|
SCH 546738 is a potent, orally active and non-competitive CXCR3 antagonist, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.
|
-
- HY-B0418A
-
|
R-18553 hydrochloride
|
Opioid Receptor
Autophagy
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Loperamide (hydrochloride) (R-18553 (hydrochloride)) is an opioid receptor agonist . Loperamide hydrochloride is a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. Loperamide hydrochloride has anti-diarrheal effect .
|
-
- HY-N0471
-
|
Daturine
|
mAChR
|
Neurological Disease
|
|
L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205) .
|
-
- HY-13462
-
|
HTS466284
|
TGF-β Receptor
|
Cancer
|
|
LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, and exhibits 7-fold selectivity over TGFβR-II .
|
-
- HY-15186A
-
|
GDC-0068 dihydrochloride; RG-7440 dihydrochloride
|
Organoid
Akt
|
Cancer
|
|
Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective and ATP-competitive pan-Akt inhibitor with IC50s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively.
|
-
- HY-12964
-
|
|
TAM Receptor
|
Cancer
|
|
SGI-7079 is a potent and ATP-competitive Axl inhibitor, significantly inhibits the proliferation of SUM149 or KPL-4 cells with an IC50 of 0.43 or 0.16 μM, respectively.
|
-
- HY-115417
-
-
- HY-B0882S
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Edrophonium-d5 (chloride) is the deuterium labeled Edrophonium chloride. Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
|
-
- HY-N2197
-
|
|
nAChR
|
Neurological Disease
|
|
Hirsuteine is an indole alkaloid extracted from Uncaria rhynchophylla. Hirsuteine non-competitively antagonizes nicotine-mediated dopamine release by blocking ion permeation through nicotinic receptor channel complexes .
|
-
- HY-U00189
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
Sch412348 is a potent competitive antagonist of the human adenosine A2A receptor (Ki=0.6 nM) and has >1000-fold selectivity over all other adenosine receptors.
|
-
- HY-P1083A
-
|
|
Dynamin
|
Neurological Disease
|
|
Dynamin inhibitory peptide TFA competitively blocks binding of dynamin to amphiphysin, thus preventing endocytosis. Dynamin inhibitory peptide TFA blocks the dopamine D3 effect on GABAA receptors .
|
-
- HY-103384
-
|
|
Casein Kinase
|
Cancer
|
|
TMCB is a selective, ATP-competitive CK2 (casein kinase II) inhibitor with distinct Ki values of 83 nM and 21 nM for the two different catalytic CK2 subunits α and α', respectively .
|
-
- HY-134274
-
|
8-Bromoguanosine-5'-triphosphate
|
Bacterial
|
Infection
|
|
8-Br-GTP, a GTP analog, is a competitive FtsZ polymerization and GTPase activity (Ki of 31.8 μM) inhibitor. 8-Br-GTP can be used for nucleic acid modification .
|
-
- HY-115887
-
-
- HY-126730
-
|
|
Phosphatase
|
Cancer
|
|
Rubratoxin A is a natural mycotoxin and competitive inhibitor of protein phosphatase 2A (PP2A) with an IC50 of 170 nM. Rubratoxin A causes suppression of tumor metastasis and reduction of primary tumor volume in mouse xenografts .
|
-
- HY-N6054
-
|
|
Parasite
Topoisomerase
|
Infection
Inflammation/Immunology
|
|
Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis research.
|
-
- HY-16168AS
-
-
- HY-107610
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
SR2640 (hydrochloride) is a potent and selective competitive leukotriene D4/leukotriene E4 antagonist. SR2640 can be used for researching the role of leukotrienes in human asthma .
|
-
- HY-14929
-
|
GR181413A free base
|
Others
|
Others
|
|
Migalastat (GR181413A free base) is an orally active and competitive inhibitor of α-galactosidase A (α-Gal A) with an IC50 of 0.04 μM for human α-Gal A .
|
-
- HY-W025443
-
|
|
Others
|
Others
|
|
6-(4-Methoxyphenyl)pyridazin-3-amine is an aminopyridazine derivative, and can be used for the synthesis of SR 95103. SR 95103 is a selective and competitive GABA-A receptor antagonist .
|
-
- HY-N2383
-
|
(1R,2S,3S,4S,6R)-4-Amino-6-(hydroxymethyl)cyclohexane-1,2,3-triol
|
Glucosidase
|
Metabolic Disease
|
|
Validamine competitively inhibits β-glucosidase in a pH-dependent and dose-dependent manner, with an IC50 value of 2.92mM, and the maximum inhibitory ability is at the optimum pH value of this enzyme .
|
-
- HY-153320
-
|
|
MAP3K
|
Cancer
|
|
AZ-TAK1, an ATP-competitive small molecule inhibitor of TAK1, dephosphorylates TAK1, p38, and IκB-α in lymphoma cell lines .
|
-
- HY-N3320
-
|
|
Others
|
Neurological Disease
|
|
Marmin is a coumarin, that can be isolated from the immature bark of Aegle marmelos Correa. Marmin antagonizes the Histamine (HY-B1204)-induced contraction in competitive manner .
|
-
- HY-P4633
-
|
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
γ-Glu-Tyr, a competitive inhibitor of dipeptidyl peptidase-IV (DPP-IV) (IC50=6.77 mM), is a potentially functional component of the type 2 diabetes diet .
|
-
- HY-P1264F
-
|
|
nAChR
|
Neurological Disease
|
|
α-Bungarotoxin, FITC labeledis the FITC labelled α-Bungarotoxin (HY-P1264). α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs) .
|
-
- HY-119953
-
|
|
mAChR
|
Neurological Disease
|
|
BIBN-99 is a selective, BBB-penetrable and competitive muscarinic M2 receptor antagonist. BIBN-99 improves cognitive performancein rats with traumatic brain injury .
|
-
- HY-103360A
-
|
UCB35625
|
CCR
|
Inflammation/Immunology
|
|
cis-J-113863 is a competitive chemokine receptor 1 (CCR1) antagonist, with IC50 values of 0.9 and 5.8 nM for human and mouse CCR1 receptors, respectively .
|
-
- HY-N1201R
-
|
4',5,7-Trihydroxyflavone(Standard); Apigenol(Standard); C.I. Natural Yellow 1 (Standard)
|
Autophagy
Cytochrome P450
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
|
Apigenin (Standard) is the analytical standard of Apigenin. This product is intended for research and analytical applications. Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a Ki of 2 μM.
|
-
- HY-N12736
-
|
|
Phosphatase
|
Metabolic Disease
|
|
Dehydrodanshenol A is a non-competitive inhibitor of Protein tyrosine phosphatase 1B (PTP1B), with an IC50 value of 8.5 μM. Dehydrodanshenol A can be used in diabetes-related research .
|
-
- HY-Y0504R
-
|
|
Endogenous Metabolite
Cholinesterase (ChE)
|
Metabolic Disease
|
|
Trimethylammonium chloride (Standard) is the analytical standard of Trimethylammonium chloride. This product is intended for research and analytical applications. Trimethylammonium chlorideIt is an endogenous metabolite that inhibits deacetylation. Trimethylammonium chlorideIs a non-competitive inhibitor of acetylcholinesterase .
|
-
- HY-20558R
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
D-(+)-Malic acid (Standard) is the analytical standard of D-(+)-Malic acid. This product is intended for research and analytical applications. D-(+)-Malic acid (D-Malic acid), an active enantiomer of Malic acid, is a competitive inhibitor of L(--)malic acid transport .
|
-
- HY-N9949
-
|
Lupinidine
|
nAChR
|
Neurological Disease
|
|
Sparteine (Lupinidine) is an alkaloid compound derived from leguminous plants and can act as a ganglionic blocker. Sparteine competitively inhibits the activity of the neuronal nicotinic acetylcholine receptor (nACh receptor) .
|
-
- HY-117858
-
-
- HY-13503R
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Epothilone A (Standard) is the analytical standard of Epothilone A. This product is intended for research and analytical applications. Epothilone A is a competitive inhibitor of the binding of [3H] paclitaxel to tubulin polymers, with a Ki of 0.6-1.4 μM.
|
-
- HY-135072R
-
|
|
Others
|
Infection
|
|
N,N',N''-Triacetylchitotriose (Standard) is the analytical standard of N,N',N''-Triacetylchitotriose. This product is intended for research and analytical applications. N,N',N''-Triacetylchitotriose is a competitive inhibitor of lysozyme .
|
-
- HY-121483
-
|
|
Others
|
Others
|
|
Leucinal is a competitive inhibitor of brain aminopeptidase, inhibits brain soluble aminopeptidase activity (Ki = 22 microM), and can enhance the analgesia induced by leuprorelin, but has no effect on the analgesia induced by some other substances.
|
-
- HY-10422
-
|
|
mTOR
Autophagy
Apoptosis
|
Cancer
|
|
AZD-8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM. AZD-8055 inhibits both mTORC1 and mTORC2 .
|
-
- HY-16082
-
AZD7545
1 Publications Verification
|
PDHK
|
Metabolic Disease
|
|
AZD7545 is a potent, competitive, selective PDHK2 (pyruvate dehydrogenase kinase 2) inhibitor with IC50s of 36.8 nM, 6.4 nM for PDHK1 and PDHK2, respectively .
|
-
- HY-13217
-
|
GBR-12909 dihydrochloride; I893 dihydrochloride
|
Dopamine Transporter
|
Neurological Disease
|
|
Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) binds to the target site on the dopamine transporter (DAT) .
|
-
- HY-13217A
-
|
GBR 12909; I893
|
Dopamine Transporter
|
Neurological Disease
|
|
Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine (GBR-12909) binds to the target site on the dopamine transporter (DAT) .
|
-
- HY-17572
-
|
RW22164; RWJ22164
|
Oxytocin Receptor
Vasopressin Receptor
|
Endocrinology
Cancer
|
|
Atosiban (RW22164; RWJ22164) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research .
|
-
- HY-12293
-
|
|
CDK
Apoptosis
|
Cancer
|
|
LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9 (IC50 11 nM) and other transcription kinases CDK8 (IC50 16 nM), and CDK7 (IC50 246 nM).
|
-
- HY-12493A
-
|
|
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
LY-2584702 tosylate salt is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.
|
-
- HY-18689
-
|
|
iGluR
|
Neurological Disease
|
|
SYM2206 is a potent and non-competitive AMPA receptor antagonist, with an IC50 of 1.6 μM. SYM2206 blocks Nav1.6-mediated persistent currents .
|
-
- HY-19541
-
-
- HY-N6650
-
|
|
Phosphatase
|
Metabolic Disease
|
|
Isotanshinone IIA, an abietane-type diterpene metabolite, could non-competitively inhibit Protein Tyrosine Phosphatase 1B (PTP1B) activity with an IC50 0f 11.4 μM.
|
-
- HY-B0165CS
-
-
- HY-101190
-
-
- HY-N4289
-
|
|
Cathepsin
|
Cancer
|
|
3-Epiursolic Acid is a triterpenoid that can be isolated from Eriobotrya japonica, acts as a competitive inhibitor of cathepsin L (IC50, 6.5 μM; Ki, 19.5 μM), with no obvious effect on cathepsin B .
|
-
- HY-N1750
-
|
|
Tyrosinase
Endogenous Metabolite
|
Others
|
|
3-(2,4-Dihydroxyphenyl)propanoic acid (DPPacid) is a potent and competitive tyrosinase inhibitor, inhibits L-Tyrosine and DL-DOPA with an IC50 and a Ki of 3.02 μM and 11.5 μM, respectively .
|
-
- HY-12493B
-
|
|
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
LY-2584702 hydrochloride is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.
|
-
- HY-12853
-
|
|
Reactive Oxygen Species
|
Others
|
|
Mesotrione is a herbicide belongs to the benzoylcyclohexanedione family. Mesotrione is a potent and competitive and reversible inhibitor of HPPD enzyme. Mesotrione is selective to maize due to rapid metabolism and relative high tolerance by the susceptible crop plant .
|
-
- HY-119611
-
-
- HY-B0394S
-
|
Tropine tropate-d5; DL-Hyoscyamine-d5
|
mAChR
Autophagy
|
Neurological Disease
|
|
Atropine-d5 is the deuterium labeled Atropine (sulfate monohydrate). Atropine (Tropine tropate) sulfate monohydrate is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect[1].
|
-
- HY-105860
-
|
BGG 492
|
iGluR
|
Neurological Disease
|
|
Selurampanel (BGG 492) is an orally active and competitive AMPA receptor antagonist with an IC50 of 190 nM. Selurampanel has reasonable blood-brain barrier penetration. Selurampanel can be used for epilepsy research .
|
-
- HY-19263
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
BMS-193884 is a selective, orally active, and competitive ETA antagonist with 10000-fold greater affinity for the human ETA receptor (Ki=1.4 nM) than for the ETB receptor .
|
-
- HY-D1493
-
|
|
PKC
|
Others
|
|
FIM-1 is a fluorescent PKC (protein kinase C) probe that can be used for mitochondrial staining. FIM-1 inhibits PKC and acts as ATP-competitive catalytic site inhibitor .
|
-
- HY-151115
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
JNJ-1289 is a potent, selective, competitive and allosteric human spermine oxidase (hSMOX) inhibitor (IC50: 50 nM). JNJ-1289 can be used in the research of polyamine catabolism, inflammation and cancers .
|
-
- HY-N10497
-
|
|
nAChR
|
Neurological Disease
|
|
Dihydro-β-erythroidine is a a competitive nicotinic receptor antagonist. Dihydro-β-erythroidine blocks the discriminative stimulus properties of nicotine. Dihydro-β-erythroidine inhibits the anxiolytic effect of nicotine induced .
|
-
- HY-118563
-
|
|
Biochemical Assay Reagents
|
Others
|
|
S-Farnesyl thioacetic acid is an analog of S-farnesyl cysteine, which is a prenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase) competitive inhibitors. It also inhibits the methylation of farnesylated and geranylgeranylated substrates.
|
-
- HY-N7114
-
|
|
Antibiotic
Bacterial
|
Infection
Metabolic Disease
|
|
Chloramphenicol succinate is a proagent of Chloramphenicol, with Haemotoxicity. Chloramphenicol succinate also is an antibiotic. Chloramphenicol succinate is a competitive substrate and inhibitor of succinate dehydrogenase (SDH) that is the possible reason for its toxicity .
|
-
- HY-W179181
-
|
|
GLUT
|
Metabolic Disease
|
|
MSNBA is a specific inhibitor of GLUT5 fructose transport in proteoliposomes. MSNBA competitively inhibits GLUT5 fructose uptake with a KI of 3.2±0.4?μM in MCF7 cells .
|
-
- HY-N2962
-
|
|
Tyrosinase
|
Inflammation/Immunology
|
|
Broussonin C is a competitive inhibitor of Tyrosinase that can be isolated from Broussonetia kazinoki. Broussonin C inhibits monophenolase and diphenolase with IC50s of 0.43 and 0.57 μM, respectively .
|
-
- HY-121908
-
|
|
ATP Synthase
|
Cancer
|
|
FCPT, an ATP competitive inhibitor, induces a tight-binding of kinesin-5 onto microtubules and induced loss of microtubules selectively at the poles of Xenopus extract spindles without altering microtubule dynamics .
|
-
- HY-149711
-
|
|
ICMT
|
Metabolic Disease
|
|
Farnesylcysteine (FC) is a competitive inhibitor of ICMT. The fcly mutant has quantitatively low farnesylcysteine (FC) lyase activity and an enhanced response to ABA. Farnesylcysteine induces an ABA hypersensitive phenotype in Arabidopsis thaliana .
|
-
- HY-115740A
-
|
Ara-CTP trisodium
|
DNA/RNA Synthesis
|
Cancer
|
|
Cytarabine triphosphate (Ara-CTP) trisodiu, an active metabolite of Cytarabine, is a competitive inhibitor of DNA synthesis. Intracellular Cytarabine triphosphate trisodiu levels can be used to predict chemosensitivity of leukemic blasts to Cytarabine .
|
-
- HY-161137
-
|
|
Others
|
Neurological Disease
|
|
LQFM215 is a proline transporter (PROT) inhibitor. LQFM215 inhibits proline transport by competitively binding to the active site of PROT. LQFM215 effectively reduces hyperlocomotion and enhances social interaction .
|
-
- HY-122200
-
|
JS399-19
|
Myosin
Fungal
|
Infection
|
|
Phenamacril (JS399-19) inhibits activity of myosin I non-competitively with an IC50 of 360 nM through suppression of the ATPase activity, exhibits therefore an antifungal efficacy towards Fusarium species .
|
-
- HY-16060S3
-
|
ARN-509-d7
|
Androgen Receptor
Isotope-Labeled Compounds
|
Cancer
|
|
Apalutamide-d7 is deuterated labeled Apalutamide (HY-16060). Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM .
|
-
- HY-16060R
-
|
|
Androgen Receptor
|
Cancer
|
|
Apalutamide (Standard) is the analytical standard of Apalutamide. This product is intended for research and analytical applications. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM .
|
-
- HY-103265A
-
|
FPL 67156
|
Phosphatase
|
Others
|
|
ARL67156 is an inhibitor of ecto-ATPase. ARL 67156 is a weak competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12 μM, respectively .
|
-
- HY-N0471C
-
|
Daturine sulfate hydrate
|
mAChR
|
Neurological Disease
|
|
L-Hyoscyamine sulfate hydrate, a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine sulfate hydrate is a levo-isomer to Atropine (HY-B1205) .
|
-
- HY-B0183R
-
-
- HY-123665
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
PSB-1410 is a selective and competitive monoamine oxidase B (MAO-B) inhibitor with IC50 for human MAO-B and rat MAO-B Values are 0.23 and 1.01 nM respectively .
|
-
- HY-100785A
-
|
γDGG acetate; γ-D-Glutamylglycine acetate
|
iGluR
|
Neurological Disease
|
|
gamma-DGG acetate (γDGG acetate) is a competitive AMPA receptor blocker. gamma-DGG acetate is also a reversible Excitatory post-synaptic potentials (e.p.s.p.s) antagonist .
|
-
- HY-P1619
-
|
|
Others
|
Others
|
|
ICI 186756 is a compound that inhibits the activity of human neutrophil elastase, has a competitive inhibitory effect on the enzyme, can inhibit enzyme-induced lung changes, and can also modulate hamster lung lesions.
|
-
- HY-169205
-
|
|
Cholinesterase (ChE)
|
Cancer
|
|
AChE/BChE-IN-22 (compund 7) competitively inhibits both AChE and BChE enzymes, with values of 28.18±2.51 and 41.74±3.18μM, respectively .
|
-
- HY-N1860
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
3-O-Methylquercetin (3-MQ) is a major component from the plant Rhamnus nakaharai and has antiviral activity and potential antiasthmatic efficacy. 3-O-Methylquercetin inhibits total cAMP and cGMP-phosphodiesterase (PDE). The IC50 values of 3-O-Methylquercetin (3-MQ) against PDE1-PDE5 are in the range of 1.6-86.9 μM. 3-O-Methylquercetin is a non-competitive inhibitor of PDE2 and a competitive inhibitor of PDE4 .
|
-
- HY-50706
-
|
AZD6244; ARRY-142886
|
MEK
Apoptosis
|
Cancer
|
|
Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
|
-
- HY-11087
-
|
SD-06
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
|
SD 0006 (SD-06) is an orally active, selective, ATP-competitive and potent diaryl pyrazole inhibitor of p38α MAP kinase, with an IC50 of 110 nM for p38α .
|
-
- HY-12012
-
-
- HY-10474
-
|
PP 242
|
mTOR
Autophagy
Mitophagy
Apoptosis
|
Cancer
|
|
Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor with an IC50 of 8 nM . PP242 inhibits both mTORC1 and mTORC2 with IC50s of 30 nM and 58 nM, respectively .
|
-
- HY-13994
-
|
|
Mps1
Polo-like Kinase (PLK)
|
Cancer
|
|
Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC50 and a Kd of 145 nM and 12 nM for Mps1 and a Kd of 61 nM for Plk1.
|
-
- HY-15084A
-
|
(-)-MK-801 maleate
|
iGluR
|
Neurological Disease
|
|
(-)-Dizocilpine maleate ((-)-MK-801 maleate) is a less active (-)-enantiomer of Dizocilpine. (-)-Dizocilpine maleate is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with a Ki of 211.7 nM. (-)-Dizocilpine maleate has antidepressant effects .
|
-
- HY-12774
-
IC261
4 Publications Verification
|
Casein Kinase
Apoptosis
|
Cancer
|
|
IC261 is a selective, ATP-competitive CK1 inhibitor, with IC50s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively.
|
-
- HY-101212
-
|
CYC065
|
CDK
|
Cancer
|
|
Fadraciclib (CYC065) is a second-generation, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with IC50s of 5 and 26 nM, respectively .
|
-
- HY-100888
-
|
TAK-931
|
CDK
|
Cancer
|
|
Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC50 of <0.3 nM. Simurosertib has anti-cancer activity .
|
-
- HY-103261
-
|
|
Proton Pump
|
Endocrinology
|
|
SCH28080 is a reversible, K +-competitive inhibitor of the gastric H,K-ATPase, with a Ki of 0.12 μM. SCH28080 is an effective inhibitor of acid secretion in vivo and with anti-gastric ulcer activity .
|
-
- HY-59090
-
-
- HY-11021
-
|
PRT060128
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Elinogrel (PRT060128) is a potent, direct acting, competitive, and reversible platelet P2Y12 antagonist (IC50=20 nM). It is orally and intravenously available and has potent antiplatelet effects .
|
-
- HY-N4225
-
|
|
Adrenergic Receptor
|
Endocrinology
Cancer
|
|
Aaptamine, a spongean alkaloid isolated from a sea sponge Aaptos aaptos, is a competitive antagonist of α-adrenoceptor and activates the p21 promoter in a p53-independent manner .
|
-
- HY-118047
-
-
- HY-10963
-
|
CYT387 mesylate
|
JAK
Autophagy
|
Cancer
|
|
Momelotinib mesylate (CYT387 mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.
|
-
- HY-117319
-
|
TAK-083; PA-155A
|
Antibiotic
Bacterial
|
Infection
Inflammation/Immunology
|
|
Indolmycin (TAK-083), an antibiotic, is a competitive inhibitor of prokaryotic tryptophanyl-tRNA synthetase (TrpS). Indolmycin (TAK-083) possesses both anti-viral and anti-bacterial activity .
|
-
- HY-N2368
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Arecaidine, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine is a substrate of H +-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake .
|
-
- HY-W015514
-
|
|
Others
|
Neurological Disease
|
|
N-(3-Aminopropyl)cyclohexylamine, a cyclohexylamine derivative, acts as a selective and competitive inhibitor of spermine synthase. N-(3-Aminopropyl)cyclohexylamine can be used for the research of neurological diseases .
|
-
- HY-N2368A
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Arecaidine hydrochloride, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine hydrochloride is a substrate of H +-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake .
|
-
- HY-B0322S1
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Sulfamethoxazole- 13C6 is a 13C labeled Sulfamethoxazole. Sulfamethoxazole (Ro 4-2130) is a sulfonamide bacteriostatic antibiotic, used for bacterial infections. Sulfonamides is a competitive antagonist of para-aminobenzoic acid (PABA)[1].
|
-
- HY-147823
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-6 (compound 18) is a competitive α-glucosidase inhibitor with an IC50 of 5.69 µM. α-Glucosidase-IN-6 has anti-diabetic potential .
|
-
- HY-N10488
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-11 (compound 10) is a potent, selective and non-competitive BChE (butyrylcholinesterase) inhibitor, with an IC50 of 2.1 μM. BChE-IN-11 can be used for Alzheimer's disease (AD) research .
|
-
- HY-117468
-
|
|
Fluorescent Dye
|
Others
|
|
Lissamine rhodamine B is a red-fluorescent dye, it is a derivative of rhodamine. Lissamine rhodamine B can be used as a fluorescent probe to develop competitive aptamer fluorescence anisotropy/polarization (FA/FP) assays .
|
-
- HY-119995
-
|
|
Apoptosis
Histamine Receptor
|
Cardiovascular Disease
Cancer
|
|
Chloropyramine is competitive reversible H1 receptor antagonist. Chloropyramine also has anti-tumour activity in breast cancer. Chloropyramine can be used for the research of allergic conditions, such as conjunctivitis and bronchial asthma .
|
-
- HY-16060S1
-
|
ARN-509-d3
|
Androgen Receptor
|
Cancer
|
|
Apalutamide-d3 is the deuterium labeled Apalutamide[1]. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[2].
|
-
- HY-117992
-
|
|
Complement System
|
Others
|
|
BR103 is a C3aR-specific small molecule ligand. BR103 can be used to measure ligand affinity for a G protein-coupled receptor for saturation and competitive binding .
|
-
- HY-155569
-
|
|
Fungal
|
Infection
|
|
Chitin synthase inhibitor 13 (compound 12g) is a non-competitive inhibitor of chitin synthase, with an IC50 of 106.7 μM. Chitin synthase inhibitor 13 exhibits a broad-spectrum of antifungal activity .
|
-
- HY-155970
-
-
- HY-155973
-
-
- HY-114503A
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
(E/Z)-NSAH is an isoform of NSAH (HY-114503), which is reversible and competitive nonnucleoside ribonucleotide reductase (RR) inhibitor, with cell-free IC50 of 32 μM and cell-based IC50 of ~250 nM, respectively .
|
-
- HY-W653723
-
|
NDCHA
|
Androgen Receptor
|
Endocrinology
|
|
N-Nitrosodicyclohexylamine (NDCHA) is a N-nitrosocompound with anti-androgenic activities. N-Nitrosodicyclohexylamine shows the competitive binding to androgen receptor (AR) against 5α-dihydrotestosterone and decreased the level of AR protein .
|
-
- HY-W727627
-
|
|
Amylases
|
Metabolic Disease
|
|
5-O-Coumaroylquinic acid is a potent, reversible, non-competitive α-amylase inhibitor with an IC50 value of 69.39 μM. 5-O-Coumaroylquinic acid can be used in diabetes research .
|
-
- HY-N9075
-
|
|
Glucosidase
|
Cancer
|
|
9-(4′-Hydroxyphenyl)-2-methoxyphenalen-1-one is a phytoalexin and mixed competitive α-glucosidase inhibitor of Bacillus stearothermophilus (IC50: 3.86 mg/L) .
|
-
- HY-117636
-
|
|
Others
|
Others
|
|
(Rac)-L-659989 is the racemate of L-659989 (HY-121394). L-659989 s an orally active, extremely potent, selective and competitive platelet activating factor (PAF) receptor antagonist .
|
-
- HY-125558
-
|
ORG-34517
|
Glucocorticoid Receptor
|
Neurological Disease
|
|
PT150 (ORG-34517) is a competitive and orally active glucocorticoid receptor antagonist. PT150 shows neuroprotective effects. PT150 has the potential for the research of Parkinson’s disease .
|
-
- HY-137613
-
|
|
HIV
|
Infection
Inflammation/Immunology
|
|
Sp-TTPαS is a competitivesterile alpha motif and HD domain containing protein 1 (SAMHD1) catalysis inhibitor. Sp-TTPαS competitively inhibits TTP hydrolysis with a Ki value of 46 µM .
|
-
- HY-19301
-
|
J-104135
|
Farnesyl Transferase
|
Cancer
|
|
J 104871 (J-104135) is a farnesyl pyrophosphate (FPP)-competitive farnesyltransferase (FTase) inhibitor. J 104871 inhibits rat brain FTase with an IC50 of 3.9 nM in the presence of farnesyl pyrophosphate (FPP) .
|
-
- HY-137144
-
|
ZB716
|
Estrogen Receptor/ERR
|
Cancer
|
|
Fulvestrant-3-boronic acid is an orally active ERα inhibitor, which binds to ERα competitively (IC50 = 4.1 nM) and effectively degrades ERα in breast cancer cells .
|
-
- HY-10017A
-
|
|
CXCR
|
Inflammation/Immunology
Endocrinology
|
|
(R)-SCH 546738 is the R-isomer of SCH 546738 (HY-10017). SCH 546738 is an orally active and non-competitive antagonist for CXCR3 with Ki of 0.4 nM for human CXCR3 receptor .
|
-
- HY-109060
-
|
ZYDPLA1
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Garvagliptin (ZYDPLA1) is an orally active, competitive and long acting DPP4 Inhibitor, with an IC50 of 2.99 nM against human recombinant DPP IV. Garvagliptin (ZYDPLA1) exhibits antihyperglycemic effect .
|
-
- HY-12019
-
|
|
c-Met/HGFR
|
Cancer
|
|
SGX523 is a exquisitely selective and ATP-competitive MET inhibitor. SGX523 potently inhibits MET with an IC50 of 4 nM and is >1,000-fold selective versus other protein kinases. Antitumor activity .
|
-
- HY-10319
-
BAY-549
2 Publications Verification
ROCK-IN-2; Azaindole 1; TC-S 7001
|
ROCK
|
Cardiovascular Disease
|
|
BAY-549 (Azaindole 1) is an orally active and ATP-competitive ROCK inhibitor with IC50s of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2, respectively .
|
-
- HY-15339
-
|
Cdk2 Inhibitor III
|
CDK
|
Cancer
|
|
CVT-313 (Cdk2 Inhibitor III) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC50 of 0.5 μM. CVT-313 inhibits CDC5L phosphorylation .
|
-
- HY-14691
-
|
BAY 869766; RDEA119
|
MEK
|
Cancer
|
|
Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively.
|
-
- HY-18930
-
|
|
CDK
|
Cancer
|
|
NU6300 is a covalent, irreversible and ATP-competitive CDK2 inhibitor with an IC50 value of 0.16 μM. NU6300 can be used for the research of eukaryotic cell cycle- and transcription-related .
|
-
- HY-12866
-
|
LOXO-101; ARRY-470
|
Trk Receptor
Apoptosis
|
Cancer
|
|
Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
- HY-U00448
-
|
|
Others
|
Cancer
|
|
ADDA 5 hydrochloride is a partial non-competitive inhibitor of cytochrome c oxidase (CcO), with IC50s of 18.93 μM and 31.82 μM for purified CcO from human glioma and bovine heart, respectively.
|
-
- HY-111378
-
|
|
Casein Kinase
|
Metabolic Disease
|
|
Casein Kinase II Inhibitor IV is a potent, ATP-competitive of casein kinase II inhibitor with an IC50 of 9 nM. Casein Kinase II Inhibitor IV ia also a human keratinocytes (NHEK) differentiation inducer .
|
-
- HY-112668
-
|
SP2086 phosphate
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Retagliptin phosphate (SP2086 phosphate) is a selective, competitive and orally active dipeptidyl peptidase-4 (DPP-4) inhibitor. Retagliptin phosphate can be used for type 2 diabetes mellitus (T2DM) research .
|
-
- HY-16446
-
|
|
c-Met/HGFR
PI3K
Akt
MEK
Apoptosis
|
Cancer
|
|
SAR125844 is a potent, selective, and ATP-competitive MET kinase inhibitor with the value of IC50 is 4.2 nM and Ki is 2.8 nM. SAR125844 has antitumor activity and can be used for the research of cancer .
|
-
- HY-19168
-
|
EAA-090
|
iGluR
|
Neurological Disease
|
|
Perzinfotel (EAA-090) is a potent, selective, and competitive NMDA receptor antagonist with neuroprotective effects. Perzinfotel (EAA-090) shows high affinity (IC50=30 nM) for the glutamate site .
|
-
- HY-50706A
-
|
AZD6244 sulfate; ARRY-142886 sulfate
|
MEK
Apoptosis
|
Cancer
|
|
Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
|
-
- HY-N4195
-
|
Resveratrol glycoside; trans-Resveratrol 4'-O-β-D-glucopyranoside
|
Glucosidase
|
Cardiovascular Disease
Metabolic Disease
|
|
Resveratroloside (Resveratrol glycoside) is a competitive inhibitior of α-glucosidase with an IC50 of 22.9 μM. Resveratroloside has the ability to regulate PBG (postprandial blood glucose) levels. Resveratroloside exhibits cardioprotective effect .
|
-
- HY-N0471A
-
|
Daturine sulfate
|
mAChR
|
Neurological Disease
|
|
L-Hyoscyamine sulfate (Daturine sulfate), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine sulfate is a levo-isomer to Atropine (HY-B1205) .
|
-
- HY-113514
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
6-Phosphogluconic acid is a potent and competitive phosphoglucose isomerase (PGI) inhibitor with Kis of 48 μM for glucose 6-phosphate and 42 μM for fructose 6-phosphate. 6-Phosphogluconic acid is an endogenous metabolite .
|
-
- HY-12493
-
|
|
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
LY-2584702 free base is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.
|
-
- HY-I0096
-
|
|
Endogenous Metabolite
iGluR
|
Neurological Disease
|
|
Indole-2-carboxylic acid is a strong inhibitor of lipid peroxidation. Indole-2-carboxylic acid (I2CA) specifically and competitively inhibits the potentiation by glycine of NMDA-gated current .
|
-
- HY-17572A
-
|
RW22164 acetate; RWJ22164 acetate
|
Oxytocin Receptor
Vasopressin Receptor
|
Endocrinology
Cancer
|
|
Atosiban acetate (RW22164 acetate;RWJ22164 acetate) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research .
|
-
- HY-12031A
-
|
|
MEK
Autophagy
Mitophagy
Influenza Virus
|
Cancer
|
|
U0126 is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor .
|
-
- HY-125916
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Pseurotin A, a secondary metabolite of Aspergillus and other fungi, is a competitive inhibitor of chitin synthase and a neuritogenic agent. Pseurotin A inhibits IgE production (IC50=3.6 μM). Antitumor activity .
|
-
- HY-D0145
-
|
Resorufin ethyl ether
|
Cytochrome P450
NO Synthase
|
Others
|
|
7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase .
|
-
- HY-103568
-
|
|
mGluR
|
Neurological Disease
|
|
YM-298198 hydrochloride is a high-affinity, selective, orally active, and non-competitive antagonist of metabotropic glutamate receptor type 1 (mGluR1). YM-298198 hydrochloride can be used for the research of neurological disorders .
|
-
- HY-112668A
-
|
SP2086
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Retagliptin (SP2086) is a selective, competitive and orally active dipeptidyl peptidase-4 (DPP-4) inhibitor. Retagliptin can be used for type 2 diabetes mellitus (T2DM) research .
|
-
- HY-139253
-
-
- HY-103547
-
|
|
GCGR
|
Metabolic Disease
|
|
L-168049 is a potent, selective, orally active and non-competitive glucagon receptor antagonist with IC50s of 3.7 nM, 63 nM, and 60 nM for human, murine, and canine glucagon receptors, respectively .
|
-
- HY-10515
-
|
|
PDK-1
|
Cancer
|
|
BX-320 is a selective, ATP-competitive, orally acitive, and direct PDK1 inhibitor with an IC50 of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect .
|
-
- HY-145418
-
|
|
IRE1
|
Others
|
|
IRE1α kinase-IN-3 (compound 2) is a potent IRE1α inhibitor with an Ki of 480 nM. IRE1α kinase-IN-3 is the ATP-competitive ligands of IRE1α .
|
-
- HY-145419
-
|
|
IRE1
|
Others
|
|
IRE1α kinase-IN-4 (compound 6) is a potent IRE1α inhibitor with an Ki of 140 nM. IRE1α kinase-IN-4 is the ATP-competitive ligands of IRE1α .
|
-
- HY-145420
-
|
|
IRE1
|
Others
|
|
IRE1α kinase-IN-5 (compound 7) is a potent IRE1α inhibitor with an Ki of 98 nM. IRE1α kinase-IN-5 is the ATP-competitive ligands of IRE1α .
|
-
- HY-147875
-
|
|
Aldose Reductase
|
Metabolic Disease
|
|
Aldose reductase-IN-6 (Compound 3) is a competitive aldose reductase (AR) inhibitor with an IC50 of 3.164 μM and a Ki of 0.018 μM. Aldose reductase-IN-6 exhibits no cytotoxicity against healthy cells .
|
-
- HY-118795
-
|
|
Aminopeptidase
|
Inflammation/Immunology
|
|
SC-22716 is a potent, competitive, reversible inhibitor of human LTA4 hydrolase, with an IC50 of 0.20 µM. SC-22716 has potential for the research of inflammatory bowel disease (IBD) and psoriasis .
|
-
- HY-105173
-
|
EP 24332
|
GnRH Receptor
Histamine Receptor
|
Endocrinology
Cancer
|
|
Teverelix (EP 24332) is a GnRH antagonist. Teverelix binds competitively and reversibly to GnRH receptors, thereby suppressing the release of LH and FSH. Teverelix can be used in the research of prostatic hyperplasia, endometriosis, and prostate cancer .
|
-
- HY-P3853
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
GR 87389 is a potent NK2 receptor antagonist. GR 87389 antagonized GA 64349-induced smooth muscle strips contractions in a competitive manner in the human detrusor, prostate and prostatic urethra .
|
-
- HY-152214
-
|
|
Sirtuin
|
Cancer
|
|
SIRT5 inhibitor 5 is a potent SIRT5 inhibitor with an IC50 value of 0.21 µM. SIRT5 inhibitor 5 does not occupy the NNAD + -binding pocket and acts as a substrate-competitive inhibitor .
|
-
- HY-155030
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-25 (Compound (R)-8k) is a competitive inhibitor of α-glucosidase, with an IC50 of 1.19μM and can be used for anti-diabetic research .
|
-
- HY-149425
-
|
|
Sirtuin
|
Inflammation/Immunology
Cancer
|
|
SIRT5 Inhibitor 6 is a potent, substrate-competitive and selective SIRT5 inhibitor with an IC50 of 3.0 μM. SIRT5 Inhibitor6 has a therapeutic potential against septic AKI in vivo .
|
-
- HY-N7763
-
|
|
Glucosidase
|
Neurological Disease
|
|
Casuarictin is a potent and competitive α-glucosidase inhibitor with an IC50 of 0.21 μg/mL. Casuarictin is a presenilin stabilization factor like protein (PSFL) protein inhibitor. Casuarictin can be used for Alzheimer's disease research .
|
-
- HY-157132
-
|
|
FAAH
|
Neurological Disease
|
FAAH-IN-8 (compound 11) is a competitive inhibitor of FAAH with an IC50 value of 6.7 nM and a Ki value of 5 nM. FAAH-IN-8 has high blood-brain permeability and a significant antioxidant profile with no neurotoxicity .
|
-
- HY-116097
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
PSB-1491 is a selective and competitive monoamine oxidase B (MAO-B) inhibitor with an IC50 of 0.386 nM for hMAO-B. PSB-1491 shows >25000-fold selective versus MAO-A .
|
-
- HY-B0165S
-
-
- HY-16168AR
-
|
|
GnRH Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
Degarelix (Standard) is the analytical standard of Degarelix. This product is intended for research and analytical applications. Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix can be used for prostate cancer research .
|
-
- HY-A0013R
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Bosentan (Standard) is the analytical standard of Bosentan. This product is intended for research and analytical applications. Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.
|
-
- HY-122060
-
|
|
NO Synthase
|
Metabolic Disease
|
|
BYK 191023 is a selective and L-arginine competitive inducible nitric-oxide synthase inhibitor with an IC50 value of 86 nM, 17 µM, 162 µM for inducible (iNOS), neuronal (nNOS), and endothelial (eNOS) NO synthases respectively .
|
-
- HY-122370A
-
|
|
Aurora Kinase
|
Cancer
|
|
Tripolin B is an ATP-competitive Aurora kinase inhibitor with IC50 values of 2.5 µM and 6 µM for Aurora A and Aurora B kinases, respectively. Tripolin B does not inhibit Aurora kinase in cells .
|
-
- HY-B0322R
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Sulfamethoxazole (Standard) is the analytical standard of Sulfamethoxazole. This product is intended for research and analytical applications. Sulfamethoxazole (Ro 4-2130) is a sulfonamide bacteriostatic antibiotic, used for bacterial infections. Sulfonamides is a competitive antagonists of para-aminobenzoic acid (PABA) .
|
-
- HY-A0013AR
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Bosentan (hydrate) (Standard) is the analytical standard of Bosentan (hydrate). This product is intended for research and analytical applications. Bosentan hydrate is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.
|
-
- HY-135405R
-
|
|
Others
|
Cardiovascular Disease
Cancer
|
|
4-Acetylsimvastatin (Standard) is the analytical standard of 4-Acetylsimvastatin. This product is intended for research and analytical applications. 4-Acetylsimvastatin is an acetylated simvastatin. Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM .
|
-
- HY-165438
-
|
|
Others
|
Others
|
|
Sergliflozin-A is a compound used to inhibit type 2 diabetes. It can inhibit glucose transporters in the kidney, competitively inhibit hSGLT1 and hSGLT2, and mutations at different sites have different effects on its inhibitory effect.
|
-
- HY-120566
-
|
|
Others
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
PSB-16131 is a potent inhibitor of human NTPDase2, exhibiting non-competitive inhibition with an IC50 of 539 nM. PSB-16131 has the potential to be a novel therapeutic agent for the treatment of inflammation, neurodegenerative diseases, and cancer.
|
-
- HY-11003
-
|
GW843682
|
Polo-like Kinase (PLK)
|
Cancer
|
|
GW843682X is a selective, ATP-competitive inhibitor of PLK1 and PLK3, with IC50s of 2.2 nM and 9.1 nM, respectively, and is also >100-fold selective against ～30 other kinases.
|
-
- HY-10961
-
|
CYT387
|
JAK
Autophagy
Apoptosis
|
Cancer
|
|
Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.
|
-
- HY-13206
-
|
|
mGluR
|
Neurological Disease
|
|
MTEP hydrochloride is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP hydrochloride shows antidepressant and anxiolytic-like effects. MTEP hydrochloride can be used for Parkinson's disease research .
|
-
- HY-B0574
-
|
|
COX
|
Inflammation/Immunology
|
|
Mefenamic acid is a non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively.
|
-
- HY-15272
-
|
|
mTOR
|
Inflammation/Immunology
Cancer
|
|
WAY-600 is a potent, ATP-competitive, and selective mTOR inhibitor with an IC50 of 9 nM for recombinant mTOR enzyme. WAY-600 blocks mTOR complex 1/2 (mTORC1/2) assemble and activation.
|
-
- HY-100714A
-
|
D-APV; D-2-Amino-5-phosphonovaleric acid
|
iGluR
|
Neurological Disease
|
|
D-AP5 (D-APV) is a selective and competitive NMDA receptor antagonist with a Kd of 1.4 μM. D-AP5 (D-APV) inhibits the glutamate binding site of NMDA receptors .
|
-
- HY-17000S
-
-
- HY-W015309S
-
|
|
iGluR
|
Neurological Disease
|
|
Decanoic acid-d3 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
|
-
- HY-100472
-
|
|
Caspase
|
Cancer
|
|
ZYZ-488 is a competitive apoptotic protease activating factor-1 (Apaf-1) inhibitor. ZYZ-488 inhibits the activation of binding protein procaspase-9 and procaspase-3 .
|
-
- HY-16007
-
|
Garcinia acid
|
ATP Citrate Lyase
|
Metabolic Disease
|
|
(-)-Hydroxycitric acid (Garcinia acid) is the principal acid of fruit rinds of Garcinia cambogia. (-)-Hydroxycitric acid is a potent and competitive and orally active inhibitor of ATP citrate lyase. (-)-Hydroxycitric acid suppresses the fatty acid synthesis, lipogenesis, food intake, and induced weight loss .
|
-
- HY-B0743A
-
|
|
nAChR
|
Neurological Disease
|
|
Pipecuronium bromide is a potent long-acting nondepolarizing steroidal neuromuscular blocking agent (NMBA), and a bisquaternary ammonium compound. Pipecuronium bromide is a powerful competitive nAChR antagonist with a Kd of 3.06 μM .
|
-
- HY-10716A
-
|
|
GlyT
|
Neurological Disease
|
|
PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research .
|
-
- HY-124793
-
|
|
Cyclin G-associated Kinase (GAK)
|
Infection
|
|
GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 also shows binding to RIPK2 .
|
-
- HY-124793A
-
|
|
Cyclin G-associated Kinase (GAK)
|
Infection
|
|
GAK inhibitor 49 hydrochloride is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 hydrochloride also shows binding to RIPK2 .
|
-
- HY-110060
-
|
|
Complement System
|
Inflammation/Immunology
|
|
NDT 9513727 is a potent, selective, orally active and competitive inverse agonist of the human C5aR (C5a receptor), with an IC50 of 11.6 nM. NDT 9513727 can be used for the research of human inflammatory diseases .
|
-
- HY-106467B
-
|
|
iGluR
|
Neurological Disease
|
|
Caroverine hydrochloride is a potent, competitive and reversible antagonist of NMDA and AMPA glutamate receptor. Caroverine hydrochloride is also an antioxidant and calcium-blocking agent that exhibits vasorelaxant action. Caroverine hydrochloride can be used for the research of inner ear tinnitus .
|
-
- HY-W015309S2
-
|
|
iGluR
|
Neurological Disease
|
|
Decanoic acid-d2 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
|
-
- HY-115062
-
|
|
Phospholipase
|
Metabolic Disease
|
|
MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6 .
|
-
- HY-14117
-
-
- HY-W015309S1
-
|
|
iGluR
|
Neurological Disease
|
|
Decanoic acid-d199 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
|
-
- HY-W015309S3
-
|
|
iGluR
|
Neurological Disease
|
|
Decanoic acid-d5 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
|
-
- HY-107700
-
|
GV 150526A
|
iGluR
|
Cardiovascular Disease
|
|
Gavestinel (GV 150526A) is a potent, selective, orally active and non-competitive antagonist of NMDA receptor. Gavestinel binds to the glycine site of the NMDA receptor, with a pKi of 8.5. Gavestinel can be used for the research of acute ischemic stroke .
|
-
- HY-103222
-
|
3',4'-Dimethoxy-αNF
|
Aryl Hydrocarbon Receptor
|
Inflammation/Immunology
|
|
DiMNF (3',4'-Dimethoxy-αNF) is a selective aryl hydrocarbon receptor (AHR) modulator. DiMNF is a competitive AHR ligand (IC50 = 21 nM) with apparent antagonistic activity. DiMNF can be used as an anti-inflammatory agent .
|
-
- HY-111173
-
|
|
Dipeptidyl Peptidase
|
Others
|
|
Diprotin B is a dipeptidyl aminopeptidase IV (DPP IV) inhibitor. The apparent competitive inhibition of DPP-IV by the diprotins is a kinetic artifact, derived from the substrate-like nature of tripeptides containing a penultimate proline residue .
|
-
- HY-100786
-
-
- HY-W087937
-
|
Benzenecarboximidamide hydrochloride hydrate
|
Ser/Thr Protease
|
Cancer
|
|
Benzamidine (Benzenecarboximidamide) hydrochloride hydrate is a reversible competitive trypsin-like serine proteases inhibitor with Kis of 20, 21, 97, 110, 320 and 750 μM against Tryptase, Trypsin, uPA, Factor Xa, Thrombin and tPA, respectively .
|
-
- HY-121377
-
-
- HY-153629
-
|
|
Ferroptosis
|
Cancer
|
|
FSEN1 is a potent and non-competitive FSP1 inhibitor with an IC50 value of 313 nM. FSEN1 triggers iron death in cancer cells by inhibiting FSP1. FSEN1 can be used in research of cancer .
|
-
- HY-149477
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
IHC3 is a competitive and reversible MAO-B inhibitor (IC50: 1.672 μM). IHC3 can interact with the amino acid Cys172 of MAO-B. IHC3 can be used for neurological diseases research .
|
-
- HY-N2368B
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Arecaidine hydrobromide, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine hydrobromide is a substrate of H +-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake .
|
-
- HY-156136
-
|
|
Biochemical Assay Reagents
|
Others
|
|
5-n-Heptyl-6-hydroxy-4,7-dioxobenzothiazole is a competitive Qo site inhibitor of the cytochrome bc 1 complex (cytochrome c oxidoreductase) from Saccharomyces cerevisiae .
|
-
- HY-N12399
-
|
|
PKA
|
Inflammation/Immunology
|
|
Aplithianines A is a potent inhibitor against J-PKAcα with an IC50 of 1 μM , and inhibits wild-type PKA with an IC50 of 84 nM. Aplithianines A inhibits J-PKAcα catalytic activity by competitively binding to the ATP pocket .
|
-
- HY-N10002
-
|
|
Phosphatase
Glucosidase
|
Metabolic Disease
|
|
Caffeoyltryptophan is a competitive PTP1B inhibitor, with an IC50 of 16.99 μM. Caffeoyltryptophan can also inhibit α-glucosidase, linoleic acid peroxidation and haemolysis. Caffeoyltryptophan can be used for the research of type 2 diabetes .
|
-
- HY-162139
-
|
|
Bacterial
|
Inflammation/Immunology
|
|
Urease-IN-11 (Compound 6e) is a competitive urease inhibitor (IC50)=10.41 µM). Urease-IN-11 can be used to study diseases such as urease-related gastritis and peptic ulcer .
|
-
- HY-116392B
-
|
|
Glucosylceramide Synthase (GCS)
|
Cancer
|
|
DL-threo-PDMP hydrochloride is the hydrochloride form of DL-threo-PDMP that is a competitive glucosylceramide synthase (GCS) inhibitor. DL-threo-PDMP resensitizes refractory testicular germ cell tumors and epithelial ovarian cancer orthoxenografts to cisplatin in mice .
|
-
- HY-131817
-
|
|
Others
|
Others
|
|
5'-GMPS is an analogue of 5'-GMP and a substrate, competitive inhibitor or regulator of enzymes that interact with 5'-GMP. 5'-GMPS is suitable as a primer of RNA synthesis by T7 RNA polymerase .
|
-
- HY-W039920
-
|
β-D-Galactosylamine, 98%
|
Biochemical Assay Reagents
|
Others
|
|
1-Amino-1-deoxy-β-D-galactose, 98% is a galactose analog used as a competitive inhibitor to aid in the separation, purification, identification, differentiation, and characterization of β-D-galactosidase and galactose oxidase.
|
-
- HY-10716
-
|
|
GlyT
|
Neurological Disease
|
|
PF-03463275 hydrochloride is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 hydrochloride has the potential for Schizophrenia research .
|
-
- HY-113850
-
|
|
Others
|
Neurological Disease
Cancer
|
|
CPSA is a potent and competitive inhibitor against 20α-hydroxysteroid dehydrogenase (AKR1C1) with a Ki value of 0.86 nM. CPSA is promising for research of lung and endometrial cancers, premature birth and neuronal disorders .
|
-
- HY-153015
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
AAZ-A 154 is a selective, competitive and non-hallucinogenic 5-HT2AR antagonist. AAZ-A 154 can promote neuronal growth and produce long-lasting beneficial behavioral effects in rodents .
|
-
- HY-153015B
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
AAZ-A 154 hydrochloride is a selective, competitive and non-hallucinogenic 5-HT2AR antagonist. AAZ-A 154 hydrochloride can promote neuronal growth and produce long-lasting beneficial behavioral effects in rodents .
|
-
- HY-153015D
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
AAZ-A 154 mesylate is a selective, competitive and non-hallucinogenic 5-HT2AR antagonist. AAZ-A 154 mesylate can promote neuronal growth and produce long-lasting beneficial behavioral effects in rodents .
|
-
- HY-101549A
-
|
UNC2371 hydrochloride
|
FLT3
|
Cancer
|
|
MRX-2843 hydrochloride is an orally active, ATP-competitive dual MERTK and FLT3 tyrosine kinases inhibitor (TKI) with enzymatic IC50s of 1.3 nM for MERTK and 0.64 nM for FLT3, respectively .
|
-
- HY-106467
-
|
|
iGluR
|
Neurological Disease
|
|
Caroverine is a potent, competitive and reversible antagonist of NMDA and AMPA glutamate receptor. Caroverine is also an antioxidant and calcium-blocking agent that exhibits vasorelaxant action. Caroverine can be used for the research of inner ear tinnitus .
|
-
- HY-126133
-
|
|
Ras
|
Cardiovascular Disease
Others
|
|
AM-001 is a non-competitive inhibitor of Epac1 that blocks the activation of Rap1, a downstream effector of Epac1, in cultured cells. AM-001 can be used in heart disease-related research .
|
-
- HY-10337
-
|
BMS-540215
|
VEGFR
Autophagy
|
Cancer
|
|
Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β .
|
-
- HY-70072
-
|
|
Phospholipase
|
Infection
Inflammation/Immunology
Cancer
|
|
D609, an antitumoural xanthate, is a specific and competitive phosphatidyl choline-specific phospholipase C (PC-PLC) inhibitor with a Ki of 6.4 μM. D609 is an antioxidative protector and has antiviral and anti-inflammatory activity .
|
-
- HY-14281
-
|
Win 24540
|
Others
|
Endocrinology
Cancer
|
|
Trilostane (Win 24540) is a competitive and orally active 3-β-hydroxysteroiddehydrogenase (3β-HSD) inhibitor. Trilostane is a synthetic nonhormonal steroid. Trilostane can be used for the research of breast cancer and prostate cancer .
|
-
- HY-B0461
-
|
|
mAChR
|
Neurological Disease
|
|
Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
|
-
- HY-15687A
-
|
|
ROCK
|
Metabolic Disease
|
|
SAR407899 is a selective, potent and ATP-competitive ROCK inhibitor, with an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively. SAR407899 shows stable inhibition of migrasome formation.
|
-
- HY-12219
-
|
Trodusquemine; Aminosterol-1436
|
Phosphatase
|
Endocrinology
|
|
MSI-1436 is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTP1B), with an IC50 of appr 1 μM, 200-fold preference over TCPTP (IC50, 224 μM).
|
-
- HY-19794
-
|
|
SphK
|
Cancer
|
|
MP-A08 is a highly selective ATP competitive sphingosine kinase (SPHK1) inhibitor that targets both SphK1 and SphK2 with Ki values of 6.9 ± 0.8 μM and 27 ± 3 μM, respectively.
|
-
- HY-100483
-
|
|
P2X Receptor
|
Cancer
|
|
A-804598 is a CNS penetrant, competitive and selective P2X7 receptor antagonist with IC50s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively .
|
-
- HY-13848
-
|
KAND567
|
CX3CR1
CXCR
|
Inflammation/Immunology
Endocrinology
|
|
AZD8797 (KAND567) is an allosteric non-competitive and orally active antagonist of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively .
|
-
- HY-12219A
-
|
Trodusquemine lactate; Aminosterol-1436 lactate
|
Phosphatase
|
Endocrinology
|
|
MSI-1436 lactate is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTP1B), with an IC50 of 1 μM, 200-fold preference over TCPTP (IC50 of 224 μM).
|
-
- HY-100846
-
JQEZ5
3 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
|
JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitively inhibits polycomb repressive complex 2 (PRC2) with an IC50 of 80 nM. JQEZ5 has anti-tumor effects .
|
-
- HY-A0166
-
|
MK0791
|
Bacterial
Antibiotic
|
Infection
|
|
Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct .
|
-
- HY-14806B
-
|
MP-513 hydrobromide hydrate
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Teneligliptin hydrobromide hydrate is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM .
|
-
- HY-100888A
-
|
(R)-TAK-931
|
Others
|
Others
|
|
(R)-Simurosertib ((R)-TAK-931) is the (R)-enantiomer of Simurosertib. Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC50 of <0.3 nM .
|
-
- HY-101445A
-
|
|
Tyrosinase
|
Cancer
|
|
(R)-Trolox is a vitamin E analogue and a competitive tyrosinase inhibitor with a Ki value of 0.83 mM and a ID50 value of 1.88 mM . The (R)-Trolox has stronger tyrosinase affinity than the (S) enantiomer (Ki value of 0.61 mM) .
|
-
- HY-12122A
-
|
|
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
|
AR-C102222 hydrochloride is a potent, competitive, orally active and highly selective inducible nitric oxide synthase (iNOS) inhibitor, with an IC50 of 37 nM . AR-C102222 hydrochloride has antinociception and anti-inflammatory activities .
|
-
- HY-133125
-
|
|
Others
|
Inflammation/Immunology
|
|
ERAP1-IN-1 is an endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor. ERAP1-IN-1 competitively inhibits ERAP1 activity towards a nonamer peptide representative of physiological substrates .
|
-
- HY-N0301
-
|
|
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Thiocolchicoside is a competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties .
|
-
- HY-15260
-
XL413
4 Publications Verification
BMS-863233
|
CDK
|
Cancer
|
|
XL413 is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC50 of 3.4 nM, and also shows potent effect with IC50s of 215, 42 nM on CK2, PIM1, respectively, and an EC50 of 118 nM on pMCM.
|
-
- HY-A0166A
-
|
MK0791 sodium
|
Bacterial
Antibiotic
|
Infection
|
|
Cilastatin sodium (MK0791 sodium) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin sodium inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin sodium is an antibacterial adjunct .
|
-
- HY-135891
-
|
|
CCR
|
Neurological Disease
|
|
AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca 2+ flux .
|
-
- HY-100397
-
|
|
Elastase
|
Inflammation/Immunology
|
|
Elastatinal is a potent and competitive inhibitor of elastase, with a Ki of 0.21 μM. Elastatinal more potently inhibits pancreatic elastase versus leucocyte elastase. Elastatinal shows no activity on human leucocyte chymotrypsin-like protease .
|
-
- HY-108605
-
|
|
Pim
|
Cancer
|
|
PIM1-IN-2 is a potent and ATP competitive Pim-1 inhibitor with a Ki of 91 nM. PIM1-IN-2 targets the ATP-binding kinase hinge region not by forming classical hydrogen bonds .
|
-
- HY-111237
-
|
Olomoucin
|
CDK
|
Cancer
|
|
Butyrolactone I is an ATP-competitive inhibitor of CDK1 as a secondary metabolite from A. terreus . Butyrolactone I has antitumor effects in non-small cell lung, small cell lung, and prostate cancer cell lines .
|
-
- HY-12432S1
-
|
ASP2215-d8
|
FLT3
TAM Receptor
|
Cancer
|
|
Gilteritinib-d8 is deuterium labeled Gilteritinib. Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC50s of 0.29 nM/0.73 nM, respectively.
|
-
- HY-16060S2
-
|
ARN-509-13C,d3
|
Isotope-Labeled Compounds
Androgen Receptor
|
Cancer
|
|
Apalutamide- 13C,d3 is the 13C- and deuterium labeled Apalutamide. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[1].
|
-
- HY-B0690
-
-
- HY-W011184
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
6-Phosphogluconic acid trisodium is a potent and competitive phosphoglucose isomerase (PGI) inhibitor with Kis of 48 μM for glucose 6-phosphate and 42 μM for fructose 6-phosphate. 6-Phosphogluconic acid trisodium is an endogenous metabolite .
|
-
- HY-113054
-
|
|
Acyltransferase
Bacterial
Endogenous Metabolite
|
Infection
Metabolic Disease
|
|
DL-Glyceraldehyde 3-phosphate is an intermediate in several metabolic pathways, including glycolysis and gluconeogenesis. DL-Glyceraldehyde 3-phosphate is a potent inhibitor of the growth of E. coli. DL-Glyceraldehyde 3-phosphate is a competitive inhibitor of the acyltransferase .
|
-
- HY-P3808
-
-
![[D-Pro2,D-Trp7,9] Substance P](//file.medchemexpress.eu/product_pic/hy-p3808.gif)
- HY-103566
-
|
|
mGluR
EGFR
|
Neurological Disease
|
|
LY456236 is a selective, non-competitive and orally active mGlu1 receptor antagonist that inhibits phosphoinositide hydrolysis with an IC50 of 0.145 μM. LY456236 also inhibits EGFR with an IC50 of 0.91 μM .
|
-
- HY-101169
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Tetrindole mesylate is a selective inhibitor of monoamine oxidase A (MAO A). Tetrindole mesylate inhibits rat brain mitochondrial MAO A in a competitive manner with a Ki value of 0.4 μM and inhibits MAO B with a Ki of 110 μM. Tetrindole mesylate has antidepressant activity .
|
-
- HY-15251A
-
|
(Rac)-Repertaxin; (Rac)-DF 1681Y
|
Others
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
(Rac)-Reparixin is the isomer of Reparixin (HY-15251), and can be used as an experimental control. Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
|
-
- HY-107694
-
|
(Rac)-MK-801
|
Others
|
Others
|
|
(Rac)-Dizocilpine ((Rac)-MK-801) is the racemate of Dizocilpine (HY-15084B). Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist .
|
-
- HY-129682
-
-
- HY-110335
-
|
|
ROCK
|
Cancer
|
|
OXA-06 hydrochloride is an ATP-competitive ROCK inhibitor that blocks anchorage-dependent growth and invasion of non-small cell lung cancer cell lines. OXA-06 hydrochloride inhibits cofilin phosphorylation but does not stimulate apoptosis .
|
-
- HY-B0183S
-
|
|
Isotope-Labeled Compounds
|
Others
|
|
Ellagic acid- 13C12 is 13 C-labeled Ellagic acid (HY-B0183). Ellagic acid is a natural antioxidant and acts as a potent and ATP-competitive inhibitor of CK2 and SHP2, with an IC50 of 40 nM and a Ki of 20 nM .
|
-
- HY-19548
-
|
|
Arginase
|
Endocrinology
|
|
BEC, an arginine analogue, is a slow-binding competitive inhibitor of the binuclear manganese metalloenzyme arginase. BEC enhances substrate flux to NO synthase, thereby enhancing NO-dependent smooth muscle relaxation in the corpus cavernosum, and enhances penile erection .
|
-
- HY-117923
-
|
|
mTOR
PI3K
|
Cancer
|
|
PF-06465603 is a highly potent and selective ATP-competitive kinase inhibitor and a class 1 PI3K and mTOR inhibitor. PF-06465603 is a metabolite of PF-04691502 with a terminal carboxylic acid structure .
|
-
- HY-128379R
-
|
|
Drug Metabolite
|
Others
|
|
Labetalone (hydrochloride) (Standard) is the analytical standard of Labetalone (hydrochloride). This product is intended for research and analytical applications. Labetalone hydrochloride is an impurity of Labetalol. Labetalol is an orally active adrenoceptor blocking agent which is a competitive antagonist at both alpha- and beta-adrenoceptor sites .
|
-
- HY-B0377R
-
|
|
Histamine Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Famotidine (Standard) is the analytical standard of Famotidine. This product is intended for research and analytical applications. Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
|
-
- HY-123199
-
|
SABA
|
Serotonin Transporter
|
Neurological Disease
|
|
Serotonin azidobenzamidine is an arylazido derivative of 5-hydroxytryptamine (HY-B1473A). Serotonin azidobenzamide competitively inhibits [3H]5-hydroxytryptamine uptake by rat cortical synaptosomes in the dark with a Ki of 130 nM .
|
-
- HY-W040055A
-
|
L-erythro-Neopterin
|
Others
|
Neurological Disease
Metabolic Disease
|
|
L-(-)-Neopterin (L-erythro-Neopterin) is a cholinergic receptor that acts as a competitive antagonist, countering the inhibitory effects of pteridine diuretics on the growth of Crithidia fasciculata. L-(-)-Neopterin can be used in research related to the nervous system and purine metabolism .
|
-
- HY-106039
-
|
|
Others
|
Neurological Disease
|
|
LY 215490 is a selective, competitive AMPA receptor antagonist against AMPA, CGSl9755 and kainate with IC50 values of 4.8, 26.4 and 247 μM, respectively. LY 215490 shows neuroprotective effects in focal ischaemia .
|
-
- HY-122510
-
|
Atropine oxidation
|
Others
|
Neurological Disease
|
|
Atropine Oxide (Atropine oxidation), a derivative of Atropine, acts as a competitive antagonist to the muscarinic acetylcholine receptors M1, M2, M3, M4, and M5, and is utilized in the treatment of specific nerve agent and pesticide poisonings.
|
-
- HY-100513A
-
|
|
Apoptosis
DNA/RNA Synthesis
Antibiotic
|
Cancer
|
|
Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 μM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 μM) . Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis . Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo .
|
-
- HY-10531
-
|
|
EGFR
|
Cancer
|
|
ARRY-380 analog, an inhibitor of EGFR (ErbB1), is extracted from patent WO2015153959A2, compound 249 . ARRY-380 is a potent, selective, ATP-competitive, orally active inhibitor of HER2 .
|
-
- HY-10163
-
|
BIBR 953; BIBR 953ZW
|
Thrombin
|
Cardiovascular Disease
Cancer
|
|
Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM) .
|
-
- HY-10721
-
|
AKT protein kinase inhibitor
|
Akt
|
Cancer
|
|
PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM).
|
-
- HY-P0322
-
|
EMD 56574
|
Integrin
|
Cardiovascular Disease
Metabolic Disease
|
|
GRGDSPK (EMD 56574) is a peptide incluing Arg-Gly-Asp (RGD). GRGDSPK (EMD 56574) is an competitive and reversible inhibitory peptide for inhibiting integrin-fibronectin binding. GRGDSPK is used to study the role of integrins in bone formation and resorption .
|
-
- HY-101549
-
|
UNC2371
|
FLT3
|
Cancer
|
|
MRX-2843 (UNC2371) is an orally active, ATP-competitive dual MERTK and FLT3 tyrosine kinases inhibitor (TKI) with enzymatic IC50s of 1.3 nM for MERTK and 0.64 nM for FLT3, respectively .
|
-
- HY-103316A
-
Ned 19
2 Publications Verification
|
Calcium Channel
|
Cancer
|
|
Ned 19 is a selective membrane-permeant non competitive NAADP antagonist and inhibits NAADP-mediated Ca 2+ signaling, with an IC50 of 65 nM . Ned 19 strongly inhibits tumor growth and vascularization as well as lung metastases in mice .
|
-
- HY-101116
-
|
|
GCGR
|
Metabolic Disease
|
|
GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM .
|
-
- HY-14854
-
|
ATI-5923
|
Others
|
Cardiovascular Disease
|
|
Tecarfarin (ATI-5923) is an orally active and non-competitive vitamin K epoxide reductase (VKOR) antagonist, and impairs the activation of the vitamin K-dependent clotting factors II, VII, IX and X . Tecarfarin has the antithrombotic activity .
|
-
- HY-10787
-
|
H 376/95
|
Thrombin
|
Cardiovascular Disease
|
|
Ximelagatran (H 376/95) is an orally active thrombin inhibitor that selectively and competitively inhibits both free and clot-bound thrombin. Ximelagatran is an anticoagulant agent with a rapid onset of anticoagulant effect, predictable, dose-dependent pharmcokinetics and pharmacodynamics .
|
-
- HY-135878
-
|
|
Adenylate Cyclase
Adrenergic Receptor
|
Metabolic Disease
|
|
2',5'-Dideoxyadenosine is a potent and non-competitive adenylyl cyclase inhibitor via binding the P-site with an IC50 of 3 µM . 2',5'-Dideoxyadenosine is a nucleoside analog and exerts a potent antiadrenergic action in heart .
|
-
- HY-N7740
-
|
|
P2Y Receptor
Endogenous Metabolite
|
Others
|
|
Adenosine 2',5'-diphosphate sodium is a competitive P2Y1 antagonist. Adenosine 2',5'-diphosphate sodium exhibits non-selective antagonism at recombinant and human platelet P2X1 receptors .
|
-
- HY-112532
-
|
|
Leukotriene Receptor
Lipoxygenase
|
Inflammation/Immunology
|
|
REV 5901 is a competitive and orally active antagonist of leukotriene receptor, with a Ki of 0.7 μM. REV 5901 is also a 5-lipoxygenase inhibitor. REV 5901 can be used for the research of asthma in which leukotriene release be involved .
|
-
- HY-B0231A
-
|
MK-422 anhydrous
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Enalaprilat (MK-422 anhydrous), the active metabolite of the oral proagent Enalapril, is a potent, competitive and long-acting angiotensin-converting enzyme (ACE) inhibitor, with an IC50 of 1.94 nM. Enalaprilat can be used for the research of hypertension .
|
-
- HY-148395
-
|
|
Dihydroorotate Dehydrogenase
|
Cancer
|
|
UCK2 Inhibitor-2 is a non-competitive uridine-cytidine kinase 2 (UCK2) inhibitor with an IC50 value of 3.8 µM. UCK2 Inhibitor-2 can suppress uridine salvage in cells .
|
-
- HY-122289
-
|
|
Dihydrofolate reductase (DHFR)
Bacterial
|
Infection
|
|
Metioprim is a competitive inhibitor of bacterial Dihydrofolate reductase (DHFR). Metioprim has inhibitory activity against anaerobic bacteria. Metioprim shows synergistic activity in combination with DDS (HY-B0688) against E. coli. and various mycobacteria .
|
-
- HY-17610
-
|
TS-091
|
Histamine Receptor
|
Neurological Disease
|
|
Enerisant is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively .
|
-
- HY-15345AS
-
|
THU-d3; NSC-112907-d3
|
Isotope-Labeled Compounds
|
Cancer
|
|
Tetrahydrouridine-d3 is the deuterium labeled Tetrahydrouridine[1]. Tetrahydrouridine dihydrate is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine[2][3].
|
-
- HY-W661499
-
|
|
Phosphatase
|
Cancer
|
|
Orellanine is a fungal nephrotoxin. Orellanine is also a competitive inhibitor of alkaline phosphatase. Orellanine induces cell death in proximal tubular cells and in ccRCC cells. Orellanine can be used for research of clear cell renal cell carcinoma (ccRCC) .
|
-
- HY-157124
-
|
|
Tyrosinase
|
Metabolic Disease
|
Tyrosinase-IN-19 (compound 9) is a competitive tyrosinase inhibitor. Tyrosinase-IN-19 has strong antioxidant activities against ROS, ABTS+, and DPPH radicals. Tyrosinase-IN-19 suppresses tyrosinase expression in a dose-dependent manner .
|
-
- HY-111095S2
-
|
(R)-2-Hydroxypropionic acid-13C-1; D-Lactic acid-13C-1
|
Endogenous Metabolite
|
Others
|
|
D-(-)-Lactic acid- 13C-1 is the 13C labeled D-(-)-Lactic acid. D-(-)-Lactic acid is a normal intermediate in the fermentation (oxidation, metabolism) of sugar. D-(-)-Lactic acid is identified to be a competitive inhibitor of ProDH (proline dehydrogenase) in plants .
|
-
- HY-120308
-
|
SR140603
|
Neurokinin Receptor
|
Neurological Disease
|
|
(R)-Nolpitantium is the R-enantiomer of Nolpitantium (HY-108479). Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK1 receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation .
|
-
- HY-20696R
-
|
|
5-HT Receptor
|
Metabolic Disease
|
|
Tetrahydro-β-carboline (Standard) is the analytical standard of Tetrahydro-β-carboline. This product is intended for research and analytical applications. Tetrahydro-β-carboline (Tryptoline) is a metabolite of tryptamine, also is a competitive serotonin reuptake inhibitor with an Ki value of 6.1 μM .
|
-
- HY-N0021R
-
|
|
PKC
Apoptosis
Bacterial
HSV
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Verbascoside (Standard) is the analytical standard of Verbascoside. This product is intended for research and analytical applications. Verbascoside is isolated from Acanthus mollis, acts as an ATP-competitive inhibitor of PKC, with an IC50 of 25 μM, and has antitumor, anti-inflammatory and antineuropathic pain activity.
|
-
- HY-N0575R
-
|
|
Bacterial
Reactive Oxygen Species
Autophagy
|
Infection
Inflammation/Immunology
Cancer
|
|
Pinocembrin (Standard) is the analytical standard of Pinocembrin. This product is intended for research and analytical applications. Pinocembrin ((+)-Pinocoembrin) is a flavonoid found in propolis, acts as a competitive inhibitor of histidine decarboxylase, and is an effective anti-allergic agent, with antioxidant, antimicrobial and anti-inflammatory properties .
|
-
- HY-100824
-
|
|
Src
|
Cancer
|
|
PP2 Analog (compound 3) is a ATP-competitive Src family kinases inhibitor with the IC50 values of 0.22, 0.15, 2.68, and 7 aganist of lck (64-509), src , kdr, and tie-2 .
|
-
- HY-118086
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
Cancer
|
|
MRS 1067 is a competitive antagonist of the adenosine A3 receptor that inhibits the suppression of adenylate cyclase by adenosine A3 receptor agonists and affects the activation of G proteins. MRS 1067 can be used in research related to inflammation and cancer .
|
-
- HY-153015A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
AAZ-A 154 hydrobromide is a selective, competitive and non-hallucinogenic 5-HT2AR antagonist. AAZ-A 154 hydrobromide can promote neuronal growth and produce long-lasting beneficial behavioral effects in rodents .
|
-
- HY-153015C
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
AAZ-A 154 benzoate is a selective, competitive and non-hallucinogenic 5-HT2AR antagonist. AAZ-A 154 benzoate can promote neuronal growth and produce long-lasting beneficial behavioral effects in rodents .
|
-
- HY-112532A
-
|
|
Leukotriene Receptor
Lipoxygenase
|
Inflammation/Immunology
|
|
REV 5901 hydrochloride is a competitive and orally active antagonist of leukotriene receptor, with a Ki of 0.7 μM. REV 5901 hydrochloride is also a 5-lipoxygenase inhibitor. REV 5901 hydrochloride can be used for the research of asthma in which leukotriene release be involved .
|
-
- HY-12054
-
|
|
Aurora Kinase
Autophagy
Influenza Virus
Parasite
|
Cancer
|
|
Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC50 of 250 nM. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral .
|
-
- HY-10962
-
|
CYT387 sulfate salt
|
JAK
Autophagy
Apoptosis
|
Cancer
|
|
Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM).
|
-
- HY-14806A
-
|
MP-513 hydrobromide
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Teneligliptin (MP-513) hydrobromide is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM.
|
-
- HY-B0231
-
|
MK-422
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Enalaprilat dihydrate (MK-422), the active metabolite of the oral proagent Enalapril, is a potent, competitive and long-acting angiotensin-converting enzyme (ACE) inhibitor, with an IC50 of 1.94 nM. Enalaprilat dihydrate can be used for the research of hypertension .
|
-
- HY-18237
-
|
|
Src
|
Others
|
|
KX1-004 is a potent and non-ATP competitive Src-PTK inhibitor with an IC50 of 40 μM. KX1-004 protects the cochlea from hazardous noise and prevents noise-induced hearing loss (NIHL) .
|
-
- HY-15682
-
TTNPB
4 Publications Verification
Ro 13-7410; Arotinoid acid; AGN191183
|
RAR/RXR
Autophagy
Apoptosis
|
Cancer
|
|
TTNPB is a highly potent RAR agonist. Competitive binding assays using human RARs yield IC50s of α=5.1 nM, β= 4.5 nM, and γ=9.3 nM, respectively.
|
-
- HY-10079
-
CHS-828
1 Publications Verification
GMX1778
|
NAMPT
Apoptosis
|
Cancer
|
|
CHS-828 (GMX1778) is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), with an IC50 less than 25 nM. CHS-828 (GMX1778) exerts a cytotoxic effect by decreasing the cellular level of NAD + and exhibits a potent anticancer activity .
|
-
- HY-12832
-
-
- HY-12492
-
|
|
PDHK
|
Cancer
|
|
VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively.
|
-
- HY-14660S
-
|
GSK2118436A-d9; GSK2118436-d9
|
Isotope-Labeled Compounds
Raf
|
Cancer
|
|
Dabrafenib-d9 is the deuterium labeled Dabrafenib. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively[4].
|
-
- HY-124625
-
-
- HY-N2463
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
Kushenol E is a class of flavonoids isolated from Sophora flavescens and is a non-competitive indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 of 7.7 µM and a Ki of 9.5 µM, has anti-tumor activity .
|
-
- HY-108333
-
|
|
Tie
BRK
|
Cardiovascular Disease
Cancer
|
|
SB-633825 is a potent and ATP-competitive inhibitor of TIE2, LOK (STK10) and BRK with IC50s of 3.5 nM, 66 nM, 150 nM, respectively. SB-633825 can inhibit cancer cell growth and angiogenesis .
|
-
- HY-14854A
-
|
ATI-5923 sodium
|
Others
|
Metabolic Disease
|
|
Tecarfarin sodium (ATI-5923 sodium) is a novel orally active non-competitive vitamin K epoxide reductase (VKOR) antagonist, impairs the activation of the vitamin K-dependent clotting factors II, VII, IX and X .
Tecarfarin sodium has the antithrombotic activity .
|
-
- HY-126015
-
|
|
Acyltransferase
|
Metabolic Disease
|
|
P053 is a potent, non-competitive and selective ceramide synthase 1 (CerS1) inhibitor wirh an IC50 of 0.5 μM. P053 acts as an endogenous inhibitor of mitochondrial fatty acid oxidation in muscle. Whole-body adiposity regulator .
|
-
- HY-137768
-
|
|
Drug Metabolite
|
Others
|
|
Captopril EP Impurity B is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) .
|
-
- HY-137772
-
|
|
Drug Metabolite
|
Others
|
|
Captopril EP Impurity E is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) .
|
-
- HY-137769
-
|
3-Mercaptoisobutyric acid
|
Drug Metabolite
|
Others
|
|
Captopril EP Impurity C is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) .
|
-
- HY-W015332
-
|
3-Bromoisobutyric acid
|
Drug Metabolite
|
Others
|
|
Captopril EP Impurity D is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) .
|
-
- HY-W013886
-
|
S-Acetylcaptopril
|
Drug Metabolite
|
Others
|
|
Captopril EP Impurity J is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) .
|
-
- HY-122661
-
|
MPH
|
PARP
Apoptosis
|
Cancer
|
|
Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC50s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo .
|
-
- HY-108060
-
-
- HY-N9506
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Anisatin, a pure toxic substance isolated from the seeds of a Japanese plant (Illicium anisatum) acts as a picrotoxin-like, non-competitive GABA antagonist. Anisatin suppresses GABA-induced currents in a concentration-dependent manner with an EC50 of ~1.10 μM .
|
-
- HY-108660
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
PSB-0739 is a high-affinity potent, competitive, nonselective platelet P2Y12 receptor antagonist with a Ki values of 24.9 nM. The P2Y12 receptor plays a crucial role in platelet aggregation. Antithrombotic effect .
|
-
- HY-108060A
-
|
NM283 dihydrochloride
|
HCV
HCV Protease
Nucleoside Antimetabolite/Analog
|
Infection
|
|
Valopicitabine (NM283) dihydrochloride is a nucleoside analog and the orally bioavailable proagent of the potent anti-HCV agent 2'-C-methylcytidine (NM107). NM107competitively inhibits NS5B polymerase, causing chain termination .
|
-
- HY-131768
-
|
|
Cholinesterase (ChE)
|
Others
|
|
2'-O-Succinyl-cAMP is a cAMP analog that can be covalently coupled to acetylcholinesterase. 2'-O-Succinyl-cAMP conjugate has been used as tracers in a classical heterogeneous competitive enzyme immunoassay allowing the determination of cAMP .
|
-
- HY-121383
-
|
AH5158; Sch-15719W free base
|
Adrenergic Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Labetalol (AH5158) is an orally active selective α1- and non-selective β-adrenergic receptors competitive antagonist. Labetalol, an anti-hypertensive agent, can be used for the research of cardiovascular disease, such as hypertension in pregnancy .
|
-
- HY-145701
-
|
|
MEK
|
Cancer
|
|
MEK1/2-IN-2 is a potent ATP-competitive MEK1/2 inhibitor and shows equipotent inhibition of WT MEK1/2 and a panel of MEK1/2 mutant cell lines .
|
-
- HY-B0377S
-
-
- HY-122011
-
|
|
ROCK
SGK
PKA
PKC
|
Inflammation/Immunology
|
|
PF-4950834 is a potent, selective, orally bioavailable, ATP-competitive rho kinase inhibitor with IC50 values of 8.35 nM and 33.12 nM against ROCK2 and ROCK1, respectively. PF-4950834 inhibits neutrophil migration .
|
-
- HY-Y0978S2
-
|
N-tert-Butoxycarbonyl-2-aminoacetic acid-2-13C; NSC 127669-2-13C
|
Isotope-Labeled Compounds
Androgen Receptor
|
Endocrinology
|
|
Boc-Glycine-2- 13C is a 13C-labeled Linuron. Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive a
|
-
- HY-109532
-
|
Ganirest
|
GnRH Receptor
|
Metabolic Disease
|
|
Ganirelix acetate (Ganirest) is an injectable competitive gonadotropin-releasing hormone (GnRH) antagonist. Ganirelix acetate directly competes against the endogenous molecule for receptor binding, and causes a rapid reduction in estradiol levels. Ganirelix acetate can be used for researching ovarian hyperstimulation syndrome (OHSS) .
|
-
- HY-116750
-
|
|
Tyrosinase
|
Others
|
|
6-Hydroxykaempferol, a flavonoid, is a competitive tyrosinase inhibitor with an IC50 value of 124 μM. 6-Hydroxykaempferol has a Ki value of 148 μM relative to L-DOPA as a substrate and effectively inhibits the activity of the enzyme by binding to the active site of the enzyme .
|
-
- HY-P99652
-
|
AK 111
|
Interleukin Related
|
Inflammation/Immunology
|
|
Gumokimab (AK 111) is a monoclonal antibody targeting IL-17A, which can be used in the study of psoriasis, ankylosing spondylitis. Gumokimab competitively blocks the binding of human IL-17A to IL-17R.
|
-
- HY-130199
-
|
Parellic acid
|
Others
|
Metabolic Disease
|
|
Psoromic acid is a potent and selective RabGGTase (Rab geranylgeranyl transferase) inhibitor with an IC50 value of 1.3 µM. Psoromic acid is an antioxidative agent. Psoromic acid exhibits a competitive type of HMGR inhibition and mixed type of ACE (angiotensin converting enzyme) inhibition .
|
-
- HY-162107
-
|
|
DYRK
|
Neurological Disease
|
|
Dyrk1A-IN-6 (compound 7cc) is an EGCG-like non-competitive inhibitor of DYRK1A. Dyrk1A-IN-6 can be used to alleviate cognitive defects in Down syndrome models .
|
-
- HY-B0134R
-
|
|
Aminopeptidase
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Bestatin (Standard) is the analytical standard of Bestatin. This product is intended for research and analytical applications. Bestatin is a natural, broad-spectrum, and competitive CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase inhibitor. Bestatin has anticancer effects .
|
-
- HY-127128
-
|
ACC-9089 sulfate
|
Adrenergic Receptor
|
Neurological Disease
|
|
Flestolol (ACC-9089) sulfate is a competitive, ultra-short-acting beta-adrenergic blocking agent. Flestolol sulfate shows a half-life of approximately 6.5 minutes. Flestolol sulfate has the potential for the research of chest pain .
|
-
- HY-147342
-
|
|
Others
|
Others
|
|
β-Benzamide adenine dinucleotide is a bioactive metabolite of benzamide nucleoside and a potent inhibitor of inosine 5 '-monophosphate dehydrogenase (IMPDH). β-Benzamide adenine dinucleotide is a potent, competitive inhibitor of human NAD kinase (Ki = 90 µM) .
|
-
- HY-158987
-
|
APBADP
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Adenosine phosphonobutyric, 2'(3'), 5'-diposphate (APBADP) is a potent Bacillus subtilis and human adenylosuccinate lyase (ASL) inhibitor. Adenosine phosphonobutyric, 2'(3'), 5'-diposphate also is a competitive succinylaminoimidazole carboxamide ribotide (SAICAR) inhibitor .
|
-
- HY-162697
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-69 (compound 5k) is a competitive α-glucosidase inhibitor with an IC50 of 26.8 µM and a Ki value of 26.0 µM. α-Glucosidase-IN-69 has the potential for the diabetes research .
|
-
- HY-113786
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EZH2-IN-21 is a potent inhibitor of the histone lysine methyltransferase enhancer of zeste homologue 2 (EZH2) with anticancer activity. EZH2-IN-21 is competitive with the cofactor SAM and noncompetitive with peptide or nucleosome substrates .
|
-
- HY-13558
-
|
SH 489
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Atamestane (SH 489) is a specific aromatase inhibitor, which selectively blocks the estrogen biosynthesis resulting from the aromatization of androstenedione and testosterone. Atamestane is a competitive and irreversible inhibitor of estrogen biosynthesis. Atamestane can be used for the research of benign prostatic hyperplasia (BPH) .
|
-
- HY-10079A
-
|
GMX1778 (nicotinate)
|
NAMPT
Apoptosis
|
Cancer
|
|
CHS-828 nicotinate is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), with an IC50 less than 25 nM. CHS-828 nicotinate (GMX1778) exerts a cytotoxic effect by decreasing the cellular level of NAD + and exhibits a potent anticancer activity .
|
-
- HY-B0879
-
|
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
SARS-CoV
Parasite
Apoptosis
|
Infection
Cardiovascular Disease
Cancer
|
|
Suramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor . Suramin is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM) . Suramin is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM) . Suramin is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor .Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent .
|
-
- HY-10336
-
|
BMS-582664
|
VEGFR
Autophagy
|
Cancer
|
|
Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ .
|
-
- HY-10583
-
|
|
Organoid
ROCK
|
Neurological Disease
Cancer
|
|
Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor (ROCK-I Ki=220 nM; ROCK-II Ki=300 nM). Y-27632 dihydrochloride shows antiepileptic effects .
|
-
- HY-10873
-
|
SU-12662
|
Drug Metabolite
|
Cancer
|
|
N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively .
|
-
- HY-14664A
-
-
- HY-15260A
-
|
BMS-863233 monohydrochloride
|
CDK
|
Cancer
|
|
XL413 (BMS-863233) hydrochloride is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC50 of 3.4 nM, and also shows potent effect with IC50s of 215, 42 nM on CK2, PIM1, respectively, and an EC50 of 118 nM on pMCM.
|
-
- HY-16963
-
-
- HY-19981A
-
|
ARQ-087 Racemate
|
FGFR
|
Cancer
|
|
Derazantinib Racemate (ARQ-087 Racemate) is the racemate of Derazantinib. Derazantinib is an orally bioavailable, ATP competitive tyrosine kinase inhibitor; exhibits potent activity against FGFR1-3 chondrocytes with IC50s of 4.5, 1.8, and 4.5 nM, respectively.
|
-
- HY-139145S
-
|
Trimethylopropane phosphate-13C3
|
GABA Receptor
|
Neurological Disease
|
|
Etbicyphat- 13C3 is the 13C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors[1][2].
|
-
- HY-18963
-
|
RG-14355
|
EGFR
|
Cancer
|
|
Lavendustin A (RG-14355) is a potent, selective and ATP-competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC50 of 11 nM. Lavendustin A does not inhibit protein kinase A or C. Lavendustin A can suppress VEGF-induced angiogenesis .
|
-
- HY-125017
-
|
PLB-1001; CBT-101; Vebreltinib
|
c-Met/HGFR
|
Cancer
|
|
Bozitinib (PLB-1001) is a highly selective c-MET kinase inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) is a ATP-competitive small-molecule inhibitor, binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily .
|
-
- HY-N4193
-
|
|
Acyltransferase
|
Cardiovascular Disease
|
|
Glabrol (Compound 1), One isoprenyl flavonoid was isolated from ethanol extract of licorice roots, is a potent and non-competitive Acyl-coenzyme A: cholesterol acyltransferase (ACAT) inhibitor with an IC50 value of 24.6 μM for rat liver microsomal ACAT activity .
|
-
- HY-N7377
-
|
|
Glucosidase
|
Metabolic Disease
|
|
Butyl isobutyl phthalate is isolated from the rhizoid of Laminaria japonica. Butyl isobutyl phthalate is a non-competitive α-glucosidase inhibitor with an IC50 value of 38 μM. Butyl isobutyl phthalate shows a hypoglycemic effect and has the potential for diabetes treatment .
|
-
- HY-129993
-
-
- HY-136270
-
|
VX-803; M4344; ATR inhibitor 2
|
ATM/ATR
|
Cancer
|
|
Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity .
|
-
- HY-P0322A
-
|
EMD 56574 TFA
|
Integrin
|
Cardiovascular Disease
Metabolic Disease
|
|
GRGDSPK TFA (EMD 56574 TFA) is a peptide incluing Arg-Gly-Asp (RGD). GRGDSPK TFA is an competitive and reversible inhibitory peptide for inhibiting integrin-fibronectin binding. GRGDSPK TFA is used to study the role of integrins in bone formation and resorption .
|
-
- HY-W010378
-
|
H-D-Asn-OH
|
Endogenous Metabolite
|
Metabolic Disease
|
|
D-Asparagine (H-D-Asn-OH) is a competitive inhibitor of L-Asparagine hydrolysis with a Ki value of 0.24 mM. D-Asparagine is a source of nitrogen for yeast strains. D-Asparagine is a good substrate for the external yeast asparaginase but is a poor substrate for the internal enzyme .
|
-
- HY-P1271
-
|
|
nAChR
|
Cardiovascular Disease
|
|
Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
|
-
- HY-115555
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
K-Ras-PDEδ-IN-1 is a novel and potent competitive K-Ras-PDEδ inhibitor. K-Ras-PDEδ-IN-1 binds to the farnesyl binding pocket of PDEδ with a low nanomolar Kd of 8 nM .
|
-
- HY-P1107
-
|
aSvg-30
|
CRFR
|
Neurological Disease
|
|
Antisauvagine-30 (aSvg-30) is a potent, competitive and selective CRF2 receptor antagonist with Kd values of 1.4 nM and 153.6 nM for mouse CRF2β and rat CRF1 receptors, respectively .
|
-
- HY-102094
-
|
|
mGluR
|
Neurological Disease
|
|
(E/Z)-SIB-1893 is a racemic compound of (E)-SIB-1893 and (Z)-SIB-1893 isomers. (E)-SIB-1893 is a selective non-competitive metabotropic glutamate subtype 5 receptor (mGluR5) antagonist .
|
-
- HY-138813
-
|
SU-12662 hydrochloride
|
Drug Metabolite
|
Cancer
|
|
N-Desethyl Sunitinib (SU-12662) (hydrochloride) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively .
|
-
- HY-112401
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
p38 MAP Kinase Inhibitor IV is a highly specific ATP-competitive p38α MAPK inhibitor with IC50s of 0.13 and 0.55 μM for p38α and p38β MAPK, respectively .
|
-
- HY-108234
-
|
VU 255035
|
mAChR
|
Neurological Disease
|
|
VU 0255035 is a highly selective, competitive and brain penetrant muscarinic M1 receptor antagonist with an IC50 of 130 nM. VU 0255035 reduces pilocarpine-induced seizures in mice. VU0255035 is used to examine the role of the M1 receptor in diverse situations .
|
-
- HY-B0292
-
|
BW-33A free acid
|
nAChR
|
Cardiovascular Disease
Inflammation/Immunology
|
|
tracurium (BW-33A free acid) is a potent, competitive and non-depolarizing neuromuscular blocking agent.Atracurium also is an AChR receptor antagonist. Atracurium induces bronchoconstriction and neuromuscular blockade. Atracurium promotes astroglial differentiation .
|
-
- HY-134438
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Hexanoyl coenzyme A trilithium is a hexanoyl-based medium-chain fatty acyl coenzyme A that is present in all organisms. Hexanoyl coenzyme A trilithium can be used as a precursor for cannabinoid biosynthesis and acts as a competitive inhibitor of medium-chain acyl coenzyme A dehydrogenase (MCAD) .
|
-
- HY-150076
-
|
|
Others
|
Metabolic Disease
Cancer
|
|
BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor (IC50=0.3 nM). BLU2864 shows anti-tumor activity. BLU2864 can be used in cancer and polycystic kidney disease research .
|
-
- HY-160096
-
|
|
ATM/ATR
|
Cancer
|
|
M3541 is a potent, ATP-competitive and selective ATM inhibitor with an IC50 of 0.25 nM. M3541 shows remarkable selectivity against other protein kinases. M3541 suppresses double-strand breaks (DSB) repair and has antitumor activities .
|
-
- HY-14664D
-
|
XU 62-320 monohydrate
|
HMG-CoA Reductase (HMGCR)
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Fluvastatin (XU 62-320) sodium monohydrate is a first fully synthetic, competitive HMG-CoA reductaseinhibitor with an IC50 of 8 nM. Fluvastatin (sodium monohydrate) protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway .
|
-
- HY-116088
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
W123, a FTY720 analog, is a competitive sphingosine 1-phosphate type 1 (S1P1) receptor antagonist. W123 is measured by GTPγS activation, MAPK recruitment, cell migration, and ligand-induced receptor internalization .
|
-
- HY-W371164
-
-
- HY-12432R
-
|
|
FLT3
TAM Receptor
|
Cancer
|
|
Gilteritinib (Standard) is the analytical standard of Gilteritinib. This product is intended for research and analytical applications. Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC50s of 0.29 nM/0.73 nM, respectively.
|
-
- HY-14660R
-
|
|
Raf
|
Cancer
|
|
Dabrafenib (Standard) is the analytical standard of Dabrafenib. This product is intended for research and analytical applications. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-Raf V600E, respectively .
|
-
- HY-123490
-
|
INS50589
|
P2Y Receptor
|
Inflammation/Immunology
|
|
Regrelor disodium (INS 50589) is a platelet P2Y12 receptor antagonist. Regrelor disodium is a well-tolerated, reversible ADP competitive antagonist. Regrelor disodium inhibits cell proliferation. Regrelor disodium can be used in inflammation-related research .
|
-
- HY-N0793R
-
|
|
Cholinesterase (ChE)
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Protopine (Standard) is the analytical standard of Protopine. This product is intended for research and analytical applications. Protopine (Corydinine), an isoquinoline alkaloid, is a specific reversible and competitive inhibitor of acetylcholinesterase. Protopine exhibits anti-inflammation, anti-microbial, anti-angiogenic and anti-tumour activity .
|
-
- HY-118660R
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Anhydrotetracycline (hydrochloride) (Standard) is the analytical standard of Anhydrotetracycline (hydrochloride). This product is intended for research and analytical applications. Anhydrotetracycline hydrochloride, a tetracycline biosynthetic precursor, is a potent competitive broad-spectrum tetracycline destructase enzymes inhibitor. Anhydrotetracycline hydrochloride is an effector for tetracycline controlled gene expression systems in eukaryotic cells .
|
-
- HY-N7114AR
-
|
|
Bacterial
Antibiotic
|
Infection
Metabolic Disease
|
|
Chloramphenicol succinate (sodium) (Standard) is the analytical standard of Chloramphenicol succinate (sodium). This product is intended for research and analytical applications. Chloramphenicol succinate sodium is a proagent of Chloramphenicol, with Haemotoxicity. Chloramphenicol succinate is a competitive substrate and inhibitor of succinate dehydrogenase (SDH) that is the possible reason for its toxicity .
|
-
- HY-12017
-
|
|
c-Met/HGFR
|
Cancer
|
|
PF-04217903 is a potent ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM for human c-Met. PF-04217903 shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties .
|
-
- HY-10285
-
|
BMS-477118
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research .
|
-
- HY-12017A
-
|
|
c-Met/HGFR
|
Cancer
|
|
PF-04217903 mesylate is a potent ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM for human c-Met. PF-04217903 mesylate shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties .
|
-
- HY-17423
-
|
|
HIV
Reverse Transcriptase
Telomerase
Apoptosis
|
Infection
Cancer
|
|
Abacavir is an orally active and competitive nucleoside reverse transcriptase inhibitor. Abacavir can inhibits the replication of HIV. Abacavir shows anticancer activity in prostate cancer cell lines. Abacavir can trespass the blood-brain-barrier and suppresses telomerase activity .
|
-
- HY-15777
-
|
LEE011
|
CDK
|
Cancer
|
|
RRibociclib (LEE011) is an ATP-competitive and orally active CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex .
|
-
- HY-B0423
-
|
Eustigmin bromide; Neoserine bromide
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Neostigmine (Eustigmin) Bromide is an orally active and reversible cholinesterase inhibitor that acts on myasthenia gravis to prolong and intensify the muscarinic and nicotinic effects of acetylcholine. Neostigmine Bromide can be used in anesthesia to reverse the neuromuscular blockade produced by competitive neuromuscular blockers .
|
-
- HY-B0549A
-
|
Rec-7-0040; DW61
|
Phosphodiesterase (PDE)
Calcium Channel
mAChR
|
Neurological Disease
|
|
Flavoxate hydrochloride is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate hydrochloride is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate hydrochloride shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate hydrochloride can be used for the research of overactive bladder (OAB) and lower urinary tract infections .
|
-
- HY-15727
-
|
GSK2110183; LAE002
|
Akt
PKC
ROCK
|
Cancer
|
|
Afuresertib (GSK2110183) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3, respectively .
|
-
- HY-15727A
-
|
GSK2110183 hydrochloride; LAE002 hydrochloride
|
Akt
PKC
ROCK
|
Cancer
|
|
Afuresertib hydrochloride (GSK 2110183 hydrochloride) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively .
|
-
- HY-12881
-
|
SL-820715
|
iGluR
|
Neurological Disease
|
|
Eliprodil(SL-820715) is a non-competitive NR2B-NMDA receptor antagonist(IC50=1 uM), less potent for NR2A- and NR2C-containing receptors(IC50> 100 uM).
|
-
- HY-12866A
-
|
LOXO-101 sulfate; ARRY-470 sulfate
|
Trk Receptor
Apoptosis
|
Cancer
|
|
Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
- HY-18780
-
RR6
2 Publications Verification
|
Others
|
Cancer
|
|
RR6 is a potent, selective, reversible, competitive and orally active vanin inhibitor with an IC50 of 540 nM for recombinant vanin-1. RR6 also potently inhibits human, bovine and rat serum pantetheinase with IC50 values of 40 nM, 41 nM and 87 nM, respectively .
|
-
- HY-15257A
-
|
AFQ-056 racemate
|
mGluR
|
Neurological Disease
|
|
Mavoglurant racemate (AFQ-056 racemate) is the racemate of Mavoglurant. Mavoglurant is a novel, non-competitive mGlu5 receptor antagonist . Mavoglurant (racemate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-13634B
-
-
- HY-15590
-
AZ-23
3 Publications Verification
AZ23; AZ 23
|
Trk Receptor
|
Cancer
|
|
AZ-23 is an ATP-competitive and orally bioavailable Trk kinase A/B/C inhibitor with IC50s of 2 nM (TrkA), 8 nM (TrkB), 24 nM (FGFR1), 52 nM (Flt3), 55 nM (Ret), 84 nM (MuSk), 99 nM (Lck), respectively.
|
-
- HY-B0334AS
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Sulbactam-d5 (sodium) is the deuterium labeled Sulbactam sodium. Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex[1][2].
|
-
- HY-N0471S
-
|
Daturine-d3
|
mAChR
|
Neurological Disease
|
|
L-Hyoscyamine-d3 is the deuterium labeled L-Hyoscyamine. L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205)[1][2].
|
-
- HY-111055
-
|
|
GSK-3
|
Neurological Disease
|
|
BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC50s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively. BIP 135 exhibits neuroprotective effect .
|
-
- HY-133117
-
|
|
IKK
|
Cancer
|
|
BAY-985 is a highly potent, orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKε with IC50s of 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε, respectively. Antitumor efficacy .
|
-
- HY-P0027
-
|
|
Arp2/3 Complex
Fungal
|
Infection
Cancer
|
|
Jasplakinolide is a potent actin polymerization inducer and stabilizes pre-existing actin filaments. Jasplakinolide binds to F-actin competitively with phalloidin with a Kd of 15 nM. Jasplakinolide, a naturally occurring cyclic peptide from the marine sponge, has both fungicidal and anti-cancer activity .
|
-
- HY-10285A
-
|
BMS-477118 hydrate
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Saxagliptin hydrate (BMS-477118 hydrate) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin hydrate has the peotential for type 2 diabetes mellitus research .
|
-
- HY-B1729
-
|
|
Oxidative Phosphorylation
Bacterial
|
Infection
|
|
Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al .
|
-
- HY-P1376
-
|
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-W051513
-
|
|
PARP
|
Others
|
|
2-Methylquinazolin-4-ol is a potent competitive poly(ADP-ribose) synthetase inhibitor, with a Ki of 1.1 μM. 2-Methylquinazolin-4-ol mammalian aspartate transcarbamylase (ATCase) inhibitor, with 0.20 mM .
|
-
- HY-16448
-
|
BMS-477118 hydrochloride
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Saxagliptin hydrochloride (BMS-477118 hydrochloride) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin hydrochloride has the peotential for type 2 diabetes mellitus research .
|
-
- HY-108657
-
|
|
P2Y Receptor
|
Neurological Disease
|
|
MRS2279 is a selective and high affinity P2Y1 receptor antagonist, with a Ki of 2.5 nM and an IC50 of 51.6 nM. MRS2279 competitively inhibits ADP-promoted platelet aggregation with an apparent affnity (pKB=8.05) .
|
-
- HY-15756
-
|
|
Phosphatase
|
Metabolic Disease
|
|
PTP1B-IN-4 is a non-competitive allosteric inhibitor of the protein tyrosine phosphatase PTP1B, with an IC50 of 8 μM. PTP1B-IN-4 is potentail for the research of obesity and diabetes .
|
-
- HY-15281
-
|
|
mTOR
|
Cancer
|
|
QL-IX-55 is a selective ATP-competitive inhibitor of mTORC1/2 with IC50s of 50/50/10-50 nM for Human mTORC1/Yeast mTORC1/Yeast mTORC2, respectively.
|
-
- HY-135103S
-
|
|
FXR
|
Cancer
|
|
Tauro-β-muricholic acid-d4 (sodium) is the deuterium labeled Tauro-β-muricholic acid sodium. Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM[1][2][3].
|
-
- HY-115755
-
|
6-Thioinosine 5′-triphosphate; 6-Mercaptopurine-riboside-5'-triphosphate; 6-Thio-ITP
|
DNA/RNA Synthesis
|
Cancer
|
|
Thio-ITP (6-Thioinosine 5′-triphosphate) is an RNA polymerase activity competitive inhibitor. Thio-ITP has a high apparent affinity for the polymerases (RNA polymerase I Ki: 40.9 μM; RNA polymerase II Ki: 38.0 μM) .
|
-
- HY-17423E
-
|
|
HIV
Apoptosis
Reverse Transcriptase
Telomerase
|
Infection
Cancer
|
|
Abacavir hydrochloride is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir hydrochloride can inhibits the replication of HIV. Abacavir hydrochloride shows anticancer activity in prostate cancer cell lines. Abacavir hydrochloride can trespass the blood-brain-barrier and suppresses telomerase activity .
|
-
- HY-123419
-
|
|
Histone Demethylase
|
Cancer
|
|
CPI-4203 is a potent KDM5A inhibitor with an IC50 of 250 nM. CPI-4203 is competitive with 2-oxoglutarate (2-OG). CPI-4203 is structurally related to CPI-455 (HY-100421) but is less potent .
|
-
- HY-122592
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
Zifaxaban is an orally active, competitively and selective Factor Xa (FXa) inhibitor with an IC50 of 11.1 nM for human FXa. Zifaxaban shows >10000-fold greater selectivity than other serine proteases. Zifaxaban can be used for the arterial and venous thrombosis research .
|
-
- HY-17610A
-
|
TS-091 hydrochloride
|
Histamine Receptor
|
Neurological Disease
|
|
Enerisant (TS-091) hydrochloride is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively .
|
-
- HY-121208
-
|
R 46742
|
5-HT Receptor
Drug Metabolite
|
Neurological Disease
|
|
Ketanserinol (R 46742) is a metabolite of Ketanserin (HY-10562). Ketanserinol is a competitive antagonist of the effects of 5-HT (HY-B1473A) in both arteries. The KB values are 6.5 for large coronary arteries and 6.4 for pulmonary arteries .
|
-
- HY-120661
-
|
|
c-Met/HGFR
VEGFR
|
Cancer
|
|
T-1840383 is a potent, ATP-competitive inhibitor of c-Met/VEGFR-2, with the IC50s of 1.9 nM, 7.7 nM, 2.2 nM and 5.5 nM for c-Met, VEGFR1, VEGFR2 and VEGFR3, respectively .
|
-
- HY-116605
-
|
|
Histone Methyltransferase
|
Cancer
|
|
GSK926 (compound 3) is a selective histone lysine methyltransferase EZH2 inhibitor (IC50=0.02 μM; Ki=7.9 nM), with SAM-competitive and cell-active properties. GSK926 can be used in cancer research .
|
-
- HY-B0879A
-
|
Suramin hexasodium salt
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
SARS-CoV
Parasite
Apoptosis
|
Infection
Cardiovascular Disease
Cancer
|
|
Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor . Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM) . Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM) . Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor . Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent .
|
-
- HY-10423
-
|
ASP7486
|
mTOR
Autophagy
|
Cancer
|
|
OSI-027 (ASP7486) is a potent, selective, orally active and ATP-competitive mTOR kinase activity inhibitor with an IC50 of 4 nM. OSI-027 targets both mTORC1 and mTORC2 with IC50s of 22 nM and 65 nM, respectively .
|
-
- HY-14664
-
|
XU 62-320 free acid
|
HMG-CoA Reductase (HMGCR)
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Fluvastatin (XU 62-320 free acid) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway .
|
-
- HY-13945
-
NVP 231
2 Publications Verification
|
Apoptosis
|
Cancer
|
|
NVP 231 is a potent, specific, and reversible ceramide kinase (CerK) inhibitor(IC50=12 nM) that competitively inhibits binding of ceramide to CerK . NVP 231 induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage .
|
-
- HY-B0192A
-
|
SL 77499-10
|
Adrenergic Receptor
|
Endocrinology
|
|
Alfuzosin (SL 77499-10) hydrochloride is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin hydrochloride relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin hydrochloride can be used in study of benign prostatic hyperplasia (BPH) .
|
-
- HY-B0192
-
|
SL 77499
|
Adrenergic Receptor
|
Endocrinology
|
|
Alfuzosin (SL 77499-10) is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin can be used in study of benign prostatic hyperplasia (BPH) .
|
-
- HY-17443
-
|
EI546; LY544349; ONO5046
|
Elastase
SARS-CoV
|
Cancer
|
|
Sivelestat (EI546) is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19 .
|
-
- HY-17443A
-
|
ONO5046-Na; Sodium sivelestat; EI546 sodium; LY544349 sodium
|
Elastase
SARS-CoV
|
Cancer
|
|
Sivelestat (EI546) sodium is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) sodium has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19 .
|
-
- HY-15043
-
|
|
Bradykinin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
ELN-441958 is a potent, neutral, competitive and selective bradykinin B1 receptor antagonist with a Ki of 0.26 nM against native human bradykinin B1 receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse .
|
-
- HY-16755
-
|
GSK-2586184; GLPG-0778
|
JAK
|
Inflammation/Immunology
|
|
Solcitinib is an orally active, competitive, potent, selective JAK1 inhibitor, with an IC50 of 9.8 nM, and 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively; Solcitinib is used in the research of moderate-to-severe plaque-type psoriasis.
|
-
- HY-100371
-
|
alpha-MCPG
|
mGluR
|
Neurological Disease
|
|
(RS)-MCPG (alpha-MCPG) is a competitive and selective group I/group II metabotropic glutamate receptor (mGluR) antagonist. (RS)-MCPG blocks theta-burst stimulation (TBS)-induced shifts in both juvenile and neonatal rat hippocampal neurons .
|
-
- HY-10195B
-
|
LY333531 hydrochloride
|
PKC
|
Metabolic Disease
|
|
Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC50 of 5.9 nM .
|
-
- HY-18990
-
|
|
ROCK
|
Cardiovascular Disease
|
|
GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
|
-
- HY-19981
-
|
ARQ-087
|
FGFR
|
Cancer
|
|
Derazantinib (ARQ-087) is an ATP competitive and orally activeFGFR inhibitor (IC50s: 1.8 nM for FGFR2, 4.5 nM for FGFR1 and 3 nM). Derazantinib inhibits FGFR phosphorylation. Derazantinib inhibits tumor growth in multiple xenograft models .
|
-
- HY-103021
-
|
|
TGF-β Receptor
|
Inflammation/Immunology
Cancer
|
|
LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC50 of 38.2 nM. LY3200882 inhibits various pro-tumorigenic activities and is also used as an immune modulatory agent .
|
-
- HY-111388B
-
|
|
CDK
|
Cancer
|
|
SEL120-34A hydrochloride is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.
|
-
- HY-111388
-
|
|
CDK
|
Cancer
|
|
SEL120-34A is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.
|
-
- HY-15084B
-
|
MK-801
|
iGluR
|
Neurological Disease
|
|
Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca 2+ flux .
|
-
- HY-P1293
-
|
|
iGluR
|
Neurological Disease
|
|
Conantokin G, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G has neuroprotective properties .
|
-
- HY-100530A
-
|
|
PKA
|
Neurological Disease
|
|
Rp-cAMPS, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 μM and 4.5 μM, respectively) antagonist. Rp-cAMPS is resistant to hydrolysis by phosphodiesterases .
|
-
- HY-100530D
-
|
|
PKA
|
Neurological Disease
|
|
Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS sodium salt is resistant to hydrolysis by phosphodiesterases .
|
-
- HY-113038B
-
|
2-Hydroxyglutarate; 2-Hydroxyglutaric acid; 2-Hydroxypentanedioic acid
|
Histone Demethylase
Endogenous Metabolite
|
Cancer
|
|
α-Hydroxyglutaric acid (2-Hydroxyglutarate) is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases .
|
-
- HY-A0230A
-
|
SCH 33844 hydrochloride
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Spirapril (SCH 33844) hydrochloride is a potent angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril competitively binds to ACE and prevents the conversion of angiotensin I to angiotensin II. Spirapril is an orally active proagent of Spiraprilat and can be used for the research of hypertension, congestive heart failure .
|
-
- HY-108935
-
|
|
HIV Integrase
GLUT
Tyrosinase
|
Cancer
|
|
Lavendustin B is an inhibitor of HIV-1 integrase interaction with LEDGF/p75 with an IC50 of 94.07 μM. Lavendustin B is an ATP-competitive GLUT1 inhibitor with a Ki of 15 µM. Lavendustin B is also a weak inhibitor of tyrosine kinases .
|
-
- HY-107703
-
|
|
iGluR
|
Neurological Disease
|
|
CGP 39551 is a potent, orally active, competitive N-methyl-D-aspartate (NMDA) receptor antagonist with potent anticonvulsant activity . CGP 39551 shows measurable inhibitory activity at both L-[ 3H]-glutamate (Ki=8.4 μM) .
|
-
- HY-12182
-
|
|
Prostaglandin Receptor
|
Cancer
|
|
ONO-8711 is a potent and selective competitive antagonist of EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1 respectively). ONO-8711 effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer .
|
-
- HY-100616
-
|
cis-1-Aminocyclobutane-1,3-dicarboxylic acid
|
Others
|
Neurological Disease
|
|
cis-ACBD is a potent and selective inhibitor of the high-affinity, Na +-dependent plasma membrane glutamate transporter. cis-ACBD is a glutamate reuptake inhibitor. cis-ACBD also acts as linear competitive inhibitor of the uptake of D-[3H]aspartate .
|
-
- HY-B0549
-
|
Rec-7-0040 free base; DW61 free base
|
Phosphodiesterase (PDE)
Calcium Channel
mAChR
|
Neurological Disease
|
|
Flavoxate is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate can be used for the research of overactive bladder (OAB) and lower urinary tract infections .
|
-
- HY-150761
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
MY-875 is a competitive microtubulin polymerization inhibitor with an IC50 value of 0.92 μM. MY-875 inhibits microtubulin polymerization by targeting colchicine binding sites and activates the Hippo pathway. MY-875 induces apoptosis and has anticancer activity .
|
-
- HY-N10489
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-12 (compound 12) is a potent butyrylcholinesterase (BChE) non-competitive inhibitor with an IC50 value of 2.3 μM. BChE-IN-12 can be isolated from Bletilla striata. BChE-IN-12 can be used for the research of Alzheimer's disease (AD) .
|
-
- HY-13966S
-
|
2-DG-d1; 2-Deoxy-D-arabino-hexose-d1; D-Arabino-2-deoxyhexose-d1
|
Isotope-Labeled Compounds
Apoptosis
Hexokinase
HSV
|
Cancer
|
|
2-Deoxy-D-glucose-d is the deuterium labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1][2].
|
-
- HY-10254G
-
|
PD0325901; PD325901
|
MEK
|
Cancer
|
|
Mirdametinib (PD0325901) (GMP) is Mirdametinib (HY-10254) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Mirdametinib is an orally active, selective and non-ATP-competitive MEK inhibitor .
|
-
- HY-148645
-
|
|
STING
|
Inflammation/Immunology
|
|
STING modulator-4 (compound AIH05) is a competitive STING modulator with a Ki of 0.0933 μM for R232H STING. STING modulator-4 has an EC50 of >10 μM for p-IRF3 in THP-1 cell .
|
-
- HY-W099579
-
|
Kojic dipalmitate
|
Tyrosinase
|
Endocrinology
|
|
Kojic acid dipalmitate (Kojic dipalmitate) is a derivative of Kojic acid (HY-W050154), a fungal metabolite that can be produced by species of Aspergillus, Acetobacter and Penicillium. Kojic acid dipalmitate is a slow and reversible competitive inhibitor of tyrosinase. Kojic acid dipalmitate can be used for skin‐lightening agent research .
|
-
- HY-107525
-
|
|
EAAT
|
Neurological Disease
|
|
(±)-HIP-A is a non-competitive excitatory amino acid transporter (EAAT) blocker that effectively blocks Glu uptake (IC50=17-18 μM). (±)-HIP-A is also a lead compound against ischemia-induced neuronal degeneration. (±)-HIP-A can be used in the study of neurological diseases .
|
-
- HY-19981B
-
|
ARQ-087 dihydrochloride
|
EGFR
|
Cancer
|
|
Derazantinib (ARQ-087) dihydrochloride is an ATP competitive and orally activeFGFR inhibitor (IC50s: 1.8 nM for FGFR2, 4.5 nM for FGFR1 and 3). Derazantinib dihydrochloride inhibits FGFR phosphorylation. Derazantinib dihydrochloride inhibits tumor growth in multiple xenograft models .
|
-
- HY-B0418AR
-
|
R-18553 hydrochloride (Standard)
|
Opioid Receptor
Autophagy
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Loperamide (hydrochloride) (Standard) is the analytical standard of Loperamide (hydrochloride). This product is intended for research and analytical applications. Loperamide (hydrochloride) (R-18553 (hydrochloride)) is an opioid receptor agonist . Loperamide hydrochloride is a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. Loperamide hydrochloride has anti-diarrheal effect .
|
-
- HY-138877A
-
|
|
Phosphatase
|
Cancer
|
|
Phosphoglycolic acid (lithium) is a competitive inhibitor of phosphoglycerate mutase (PGAM)-B, an enzyme of the glycolytic pathway. Phosphoglycolic acid increases basal and fMLF-induced levels of G6P in intact neutrophils. Phosphoglycolic acid thereby increases upstream intermediates in neutrophils, thereby amplifying the respiratory oxidative burst .
|
-
- HY-19374
-
|
|
GCGR
|
Metabolic Disease
|
|
BAY-27-9955 is an orally active non-peptide glucagon receptor antagonist. Bay 27-9955 competitively blocks the interaction of glucagon with the human glucagonreceptor at an IC50 value of 110 nM. BAY-27-9955 can be used for the study of type 2 diabetes .
|
-
- HY-P1694
-
|
|
Bradykinin Receptor
|
Cardiovascular Disease
|
|
B4148 is a selective competitive bradykinin (BK) antagonist that significantly inhibits BK-induced hypotension in rats. In a rat model of endotoxin shock induced by Escherichia coli lipopolysaccharide, B4148 significantly attenuated the decrease in mean arterial blood pressure compared with the control group .
|
-
- HY-163907
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-71 (Compound 7h) is a competitive α-glucosidase inhibitor (IC50: 98.0 µM). α-Glucosidase-IN-71 can be used for research of carbohydrate-related diseases, especially type 2 diabetes mellitus .
|
-
- HY-N6054R
-
|
|
Parasite
Topoisomerase
|
Infection
Inflammation/Immunology
|
|
Niranthin (Standard) is the analytical standard of Niranthin. This product is intended for research and analytical applications. Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis research.
|
-
- HY-11001
-
|
|
CDK
Apoptosis
|
Cancer
|
|
PHA-793887 is a potent, ATP-competitive CDK inhibitor, can inhibit Cdk2, Cdk1, Cdk4, and Cdk9 with IC50s of 8 nM, 60 nM, 62 nM and 138 nM, respectively, and also inhibits glycogen synthase kinase 3β with an IC50 of 79 nM.
|
-
- HY-13204
-
|
KL 373 hydrochloride
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) hydrochloride is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden hydrochloride has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-50846
-
|
|
ERK
|
Cancer
|
|
SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations .
|
-
- HY-13204A
-
|
KL 373
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-B0292A
-
|
BW-33A
|
nAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Atracurium (BW-33A) besylate is a potent, competitive and non-depolarizing neuromuscular blocking agent. Atracurium besylate also is an AChR receptor antagonist. Atracurium besylate induces bronchoconstriction and neuromuscular blockade. Atracurium besylate promotes astroglial differentiation .
|
-
- HY-B0371
-
|
|
Adrenergic Receptor
|
Metabolic Disease
Endocrinology
|
|
Terazosin is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin works by relaxing blood vessels and the opening of the bladder. Terazosin has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment .
|
-
- HY-17537
-
|
|
IRE1
|
Cancer
|
|
APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain .
|
-
- HY-B0569
-
|
|
nAChR
Apoptosis
|
Cardiovascular Disease
Neurological Disease
|
|
Hexamethonium Bromide is a non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist, with mixed competitive and noncompetitive activity. Hexamethonium Bromide has anti-hypertensive activity. Hexamethonium Bromide attenuates sympathetic activity and blood pressure in spontaneously hypertensive animal models .
|
-
- HY-12275
-
|
|
Flavivirus
Dengue virus
ERK
Apoptosis
|
Cancer
|
|
FR 180204 is an ATP-competitive and selective ERK inhibitor. FR 180204 inhibits ERK1 and ERK2 with IC50s of 0.51 μM (Ki=0.31 μM) and 0.33 μM (Ki=0.14 μM), respectively .
|
-
- HY-12335
-
|
|
Histone Methyltransferase
|
Inflammation/Immunology
Cancer
|
|
UNC0379 is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM, KD value of 18.3 μM. UNC0379 can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma .
|
-
- HY-108474
-
|
AG 337
|
Thymidylate Synthase
|
Cancer
|
|
Nolatrexed dihydrochloride (AG 337) is a non-competitive lipophilic inhibitor of thymidylate synthase, interacts at the folate cofactor binding site of the enzyme, with a Ki of 11 nM for human thymidylate synthase . Nolatrexed dihydrochloride (AG 337) induces cell cycle arrest in S phase of cancer cells. Anti-cancer activity .
|
-
- HY-111926
-
|
|
Others
|
Metabolic Disease
|
|
N6-Methyladenosine 5'-monophosphate disodium salt is an activator of glycogen phosphorylase b, with a Ka value of 22 µM . N6-Methyladenosine 5'-monophosphate disodium salt is a non-competitive rat adenylate kinase II inhibitor .
|
-
- HY-108540
-
|
2-Amino-2-norbornanecarboxylic acid; LAT1-IN-1
|
Apoptosis
|
Cancer
|
|
BCH (2-Amino-2-norbornanecarboxylic acid) is a selective and competitive inhibitor of large neutral amino acid transporter 1 (LAT1) significantly inhibit cellular uptake of amino acids and mTOR phosphorylation, which induces the suppression of cancer growth and apoptosis .
|
-
- HY-112136
-
|
CP 43
|
MAP3K
|
Cancer
|
|
TAO Kinase inhibitor 1 (compound 43) is a selective, ATP-competitive thousand-and-one amino acid kinases (TAOK) inhibitor with IC50s of 11 to 15 nM for TAOK1 and 2, respectively. TAO Kinase inhibitor 1 delays mitosis and induces mitotic cell death .
|
-
- HY-14518
-
|
4-Aminofolic acid; APGA
|
Antifolate
|
Inflammation/Immunology
Cancer
|
|
Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia .
|
-
- HY-107339
-
|
Harmonyl
|
Angiotensin-converting Enzyme (ACE)
|
Neurological Disease
Metabolic Disease
|
|
Deserpidine (Harmonyl) is an alkaloid isolated from the root of Rauwolfia canescens related to Reserpine. Deserpidine is used as an antihypertensive agent and a tranquilizer. Deserpidine is a competitive angiotensin converting enzyme (ACE) inhibitor. Deserpidine also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex .
|
-
- HY-19826
-
|
|
DNA Methyltransferase
ADC Cytotoxin
Autophagy
Apoptosis
|
Cancer
|
|
Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC50 of 13.5 μM. Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin .
|
-
- HY-B0371F
-
|
|
Adrenergic Receptor
|
Metabolic Disease
Endocrinology
|
|
Terazosin hydrochloride is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin hydrochloride works by relaxing blood vessels and the opening of the bladder. Terazosin hydrochloride has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment .
|
-
- HY-12017B
-
|
|
c-Met/HGFR
|
Cancer
|
|
PF-04217903 phenolsulfonate is a potent ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM for human c-Met. PF-04217903 phenolsulfonate shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties .
|
-
- HY-P1271A
-
|
|
nAChR
|
Cardiovascular Disease
|
|
Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
|
-
- HY-14335
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Ro 04-6790 is a potent, competitive and selective 5-HT6 receptor antagonist with pKi values of 7.26, 7.35 for rat and human 5-HT6 receptors, respectively. Ro 04-6790 has no affinity at other receptors .
|
-
- HY-11028
-
|
PF-2413873
|
Progesterone Receptor
|
Endocrinology
|
|
PF-02413873 (PF-2413873) is a potent selective, fully competitive and orally active nonsteroidal progesterone receptor (PR) antagonist, with a Ki of 2.6 nM. PF-02413873 can block progesterone binding and PR nuclear translocation, and inhibit endometrial growth in vivo .
|
-
- HY-W011834
-
|
|
HCV
|
Infection
|
|
2'-O-Methylcytidine is a 2'-substituted nucleoside as a inhibitor of HCV replication. 2'-O-Methylcytidine inhibits RNA-dependent RNA polymerase (NS5B)-catalyzed RNA synthesis in vitro, in a manner that is competitive with substrate nucleoside triphosphate .
|
-
- HY-P1107A
-
|
aSvg-30 TFA
|
CRFR
|
Neurological Disease
|
|
Antisauvagine-30 TFA (aSvg-30 TFA) is a potent, highly selective and competitive CRF2 receptor peptidic antagonist. Antisauvagine-30 TFA exhibits a Kd of 1.4 nM and 150 nM for mCRFR2β and CRFR1, respectively .
|
-
- HY-109097
-
|
SP-8203
|
MMP
iGluR
|
Neurological Disease
|
|
Otaplimastat (SP-8203), a matrix metalloproteinase (MMP) inhibitor, blocks N-methyl-D-aspartate (NMDA) receptor-mediated excitotoxicity in a competitive manner. Otaplimastat also exhibits anti-oxidant activity. Otaplimastat can be used for the research of brain ischemic injury .
|
-
- HY-109191
-
|
PHP-201; AMA0076
|
ROCK
|
Others
|
|
Sovesudil (PHP-201) is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor with IC50s of 3.7 and 2.3 nM for ROCK-I and ROCK-II, respectively. Sovesudil lowers intraocular pressure (IOP) without inducing hyperemia .
|
-
- HY-N1193
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Sulfuretin inhibits the inflammatory response by suppressing the NF-κB pathway. Sulfuretin can be used for the research of allergic airway inflammation. Sulfuretin reduces oxidative stress, platelet aggregation, and mutagenesis . Sulfuretin is a competitive and potent inhibitor of monophenolase and diphenolase activities with the IC50 of 13.64 μM .
|
-
- HY-109191A
-
|
PHP-201 hydrochloride; AMA0076 hydrochloride
|
ROCK
|
Neurological Disease
|
|
Sovesudil (PHP-201) hydrochloride is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor with IC50s of 3.7 and 2.3 nM for ROCK-I and ROCK-II, respectively. Sovesudil hydrochloride lowers intraocular pressure (IOP) without inducing hyperemia .
|
-
- HY-110156
-
|
|
Others
|
Cancer
|
|
Y29 is a potent PFKFB3 inhibitor with an IC50 of 0.183 µM, and acts as a competitive inhibitor against Fru-6-P with a Ki of 0.094 µM. Y29 also inhibits the HeLa cell growth with a GI50 of 2.7 µM .
|
-
- HY-100714
-
|
2-APV; DL-2-Amino-5-phosphonovaleric acid
|
iGluR
|
Neurological Disease
Inflammation/Immunology
|
|
DL-AP5 (2-APV) is a competitive NMDA (N-methyl-D-aspartate) receptor antagonist. DL-AP5 shows significantly antinociceptive activity. DL-AP5 specifically blocks on channels in the rabbit retina .
|
-
- HY-118131
-
|
|
Ser/Thr Protease
|
Infection
|
|
PKR-IN-C51(compound 51) is an ATP-competitive double-stranded RNA-activated protein kinase (PKR) inhibitor with an IC50 of 9 μM. PKR-IN-C51 inhibits intracellular PKR activation in a dose-dependent manner in primary mouse macrophages .
|
-
- HY-D1594
-
|
|
Fluorescent Dye
|
Others
|
|
BODIPY TR Cadaverine, a cadaverine derivative, is a red fluorescent dye. BODIPY TR Cadaverine can be used in a a highly sensitive and robust fluorescent displacement assay, which binds to native LPS strongly, specifically recognizing lipid A, and is competitively displaced by compounds displaying an affinity for lipid A .
|
-
- HY-108657A
-
|
|
P2Y Receptor
|
Neurological Disease
|
|
MRS2279 diammonium is a selective and high affinity P2Y1 receptor antagonist, with a Ki value of 2.5 nM and an IC50 value of 51.6 nM. MRS2279 diammonium competitively inhibits ADP-promoted platelet aggregation with an pKb value of 8.05 .
|
-
- HY-129137
-
|
Cy 3-soph
|
Others
|
Others
|
|
Cyanidin 3-sophoroside chloride is a potent non-competitive reversible polyphenol oxidase (PPO) inhibitor. Also, Cyanidin 3-sophoroside chloride can be used as an anti-browning agent to inhibit the degree of PPO browning, enhance the antioxidant damage capacity of fruits and prolong the storage period .
|
-
- HY-148514
-
|
|
PDGFR
|
Cancer
|
|
CT52923 is a selective, orally active platelet-derived growth factor receptor (PDGFR) antagonist. CT52923 also is an ATP-competitive inhibitor. CT52923 can be used for the research variety of pathological diseases, including atherosclerosis, glomerulonephritis, liver cirrhosis, pulmonary fibrosis, and cancer .
|
-
- HY-105336
-
|
NSC 126849
|
DNA/RNA Synthesis
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
3-Deazauridine (NSC 126849) is a uridine analogue. 3-Deazauridine competitively inhibits cytidine triphosphate synthase to inhibit the biosynthesis of cytidine-5'-triphosphate. 3-Deazauridine acts synergistically with several antineoplastic agents, acting as a biological response modifier .
|
-
- HY-100047
-
|
|
Taste Receptor
|
Others
|
|
Nα,Nα-Bis(carboxymethyl)-L-lysine is a competitive inhibitor of bitter taste receptor 4, with an IC50 of 59 nM. Nα,Nα-Bis(carboxymethyl)-L-lysine can be used in bitter receptors related study .
|
-
- HY-100714C
-
|
2-APV sodium; DL-2-Amino-5-phosphonovaleric acid sodium
|
iGluR
|
Neurological Disease
Inflammation/Immunology
|
|
DL-AP5 (2-APV) sodium is a competitive NMDA (N-methyl-D-aspartate) receptor antagonist. DL-AP5 sodium shows significantly antinociceptive activity. DL-AP5 sodium specifically blocks on channels in the rabbit retina .
|
-
- HY-161421
-
|
|
Glucosidase
|
Metabolic Disease
|
α-Glucosidase-IN-61 (Compd 1j), a competitive α-glucosidase inhibitor, demonstrates excellent inhibition with an IC50 of 0.73 μM. α-Glucosidase-IN-61 (Compd 1j) is used for the research of type 2 diabetes mellitus .
|
-
- HY-17572R
-
|
|
Oxytocin Receptor
Vasopressin Receptor
|
Endocrinology
Cancer
|
|
Atosiban (Standard) is the analytical standard of Atosiban. This product is intended for research and analytical applications. Atosiban (RW22164; RWJ22164) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research .
|
-
- HY-119203
-
|
|
Histamine Receptor
|
Metabolic Disease
|
|
NNC 38-1049 is an orally active, potent and competitive histamine H3 receptor antagonist. NNC 38-1049 produced an increase in extracellular levels of histamine in the paraventricular nucleus. NNC 38-1049 decreases food intake and body weight, which is promising for research of obesity .
|
-
- HY-12853R
-
|
|
Reactive Oxygen Species
|
Others
|
|
Mesotrione (Standard) is the analytical standard of Mesotrione. This product is intended for research and analytical applications. Mesotrione is a herbicide belongs to the benzoylcyclohexanedione family. Mesotrione is a potent and competitive and reversible inhibitor of HPPD enzyme. Mesotrione is selective to maize due to rapid metabolism and relative high tolerance by the susceptible crop plant .
|
-
- HY-162893
-
|
|
Glucosidase
|
Metabolic Disease
|
|
SX29 is an orally active non-competitive α-glucosidase inhibitor with an IC50 value of 2.12 μM. SX29 exhibits hypoglycemic activity, and oral administration of SX29 can reduce blood glucose levels and improve glucose tolerance in diabetic mice .
|
-
- HY-160604
-
|
FPL 12924; PR 934-423; FPL 13592
|
iGluR
|
Neurological Disease
|
|
Remacemide (FPL 12924) is an orally active, non-competitive, low-affinity NMDA receptor antagonist. Remacemide shows neuroprotection activity in animal models of hypoxia and ischemic stroke. Remacemide is also an anticonvulsant, and can be used in Parkinson's disease and Huntington's disease research .
|
-
- HY-14335A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Ro 04-6790 dihydrochloride is a potent, competitive and selective 5-HT6 receptor antagonist with pKi values of 7.26, 7.35 for rat and human 5-HT6 receptors, respectively. Ro 04-6790 dihydrochloride has no affinity at other receptors .
|
-
- HY-14567
-
|
FUB-359
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Ciproxifan (FUB 359) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan displays low apparent affinity at other receptor subtypes. Ciproxifan can be used for the research of aging disorders and Alzheimer's disease .
|
-
- HY-10450
-
|
BMS-512148
|
SGLT
|
Metabolic Disease
Cancer
|
|
Dapagliflozin (BMS-512148), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin induces HIF1 expression and attenuates renal IR injury .
|
-
- HY-15289
-
|
FUB 359 maleate
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Ciproxifan maleate (FUB 359 maleate) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan maleate displays low apparent affinity at other receptor subtypes. Ciproxifan maleate can be used for the research of aging disorders and Alzheimer's disease .
|
-
- HY-16343C
-
|
|
Others
|
Metabolic Disease
|
|
NB-598 Maleate is a potent and competitive inhibitor of squalene epoxidase (SE), and suppresses triglyceride biosynthesis through the farnesol pathway. NB-598 (Maleate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-16343
-
|
|
Others
|
Metabolic Disease
|
|
NB-598 is a potent and competitive inhibitor of squalene epoxidase (SE), and suppresses triglyceride biosynthesis through the farnesol pathway. NB-598 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-16343A
-
|
|
Others
|
Metabolic Disease
|
|
NB-598 hydrochloride is a potent and competitive inhibitor of squalene epoxidase (SE), and suppresses triglyceride biosynthesis through the farnesol pathway. NB-598 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-15473
-
|
ML120B
|
IKK
|
Cancer
|
|
MLN120B (ML120B) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC50 of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis .
|
-
- HY-10255A
-
|
SU 11248
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
|
-
- HY-B0002A
-
|
GR 38032 hydrochloride dihydrate; SN 307 hydrochloride dihydrate
|
5-HT Receptor
|
Neurological Disease
|
|
Ondansetron (GR 38032) hydrochloride dehydrate is an orally active, highly selective and competitive 5-HT3 receptor antagonist (crosses the blood-brain barrier). Ondansetron hydrochloride dehydrate can be used in studies of preventing nausea and vomiting associated with cancer chemotherapy, radiation therapy and surgery .
|
-
- HY-15779
-
|
|
SphK
Apoptosis
|
Cancer
|
|
K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity .
|
-
- HY-15779A
-
|
|
SphK
Apoptosis
|
Cancer
|
|
K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 μM and a Ki of 6.4 μM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity .
|
-
- HY-15834A
-
|
SKF-108566J
|
Angiotensin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Eprosartan mesylate (SKF-108566J) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan mesylate binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
|
-
- HY-13418
-
|
Compound C dihydrochloride; BML-275 dihydrochloride
|
Organoid
AMPK
TGF-β Receptor
Autophagy
|
Cancer
|
|
Dorsomorphin (Compound C) dihydrochloride is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).
|
-
- HY-17443B
-
|
EI546 sodium tetrahydrate; LY544349 sodium tetrahydrate; ONO5046 sodium tetrahydrate
|
Elastase
SARS-CoV
|
Cancer
|
|
Sivelestat (EI546) sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) sodium tetrahydrate has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19 .
|
-
- HY-10917
-
|
|
c-Fms
|
Inflammation/Immunology
Cancer
|
|
GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling .
|
-
- HY-19533
-
|
|
Adenosine Receptor
|
Cancer
|
|
SCH 58261 is a potent, selective and competitive antagonist of adenosine A2A receptor with an IC50 of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively .
|
-
- HY-16569S
-
-
- HY-B0574S1
-
|
|
COX
|
Inflammation/Immunology
|
|
Mefenamic Acid-d3 is the deuterium labeled Mefenamic acid. Mefenamic acid is a non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively.
|
-
- HY-16569S1
-
-
- HY-100530
-
|
|
PKA
|
Neurological Disease
|
|
Rp-cAMPS triethylammonium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 μM and 4.5 μM, respectively) antagonist. Rp-cAMPS triethylammonium salt is resistant to hydrolysis by phosphodiesterases .
|
-
- HY-14903
-
|
TZP-101
|
GHSR
Adrenergic Receptor
|
Metabolic Disease
|
|
Ulimorelin (TZP-101) is a ghrelin receptor (GRLN) agonist with an EC50 of 29 nM and a Ki of 16 nM. Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition .
|
-
- HY-N7136
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
α-Terpinyl acetate is a monoterpene ester isolated from Laurus nobilis L. essential oil. α-Terpinyl acetate is a competitive P450 2B6 substrate which binding to the active site of P450 2B6 with a Kd value of 5.4?μM .
|
-
- HY-N7389B
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
GDP-α-D-mannose disodium is the donor substrate for mannosyltransferases and the precursor of GDP-β-L-fucose. GDP-α-D-mannose disodium gives a competitive inhibition with respect to GTP (Ki 14.7 μM) and an uncompetitive inhibition with respect to mannose-1-P (Ki 115 μM) .
|
-
- HY-136128
-
|
|
Potassium Channel
|
Cancer
|
|
H3B-120 is a highly selective, competitive and allosteric carbamoyl phosphate synthetase 1 (CPS1) inhibitor with an IC50 of 1.5 μM and a Ki of 1.4 μM. H3B-120 has anti-cancer activity .
|
-
- HY-101332
-
|
(2S)-α-Ethylglutamic acid; (2S)-α-EGLU
|
mGluR
|
Neurological Disease
|
|
EGLU ((2S)-α-Ethylglutamic acid; (2S)-α-EGLU) is a potent and competitive mGluR-2 receptor antagonist. EGLU interacts with (lS,3S)-ACPD-sensitive site with a Kd value of 66 μM. EGLU is an antidepressant agent .
|
-
- HY-13816
-
|
|
CDK
ATM/ATR
|
Cancer
|
|
NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with Kis of 2.5 μM and 1.3 μM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner .
|
-
- HY-111538
-
|
|
MAGL
|
Cancer
|
|
MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL, with an IC50 of 80 nM. MAGL-IN-1 exhibits anti-proliferative effects against human breast, colorectal, and ovarian cancer cells. MAGL-IN-1 blocks MAGL in cell-based as well as in vivo assays .
|
-
- HY-15473A
-
|
ML120B dihydrochloride
|
IKK
|
Inflammation/Immunology
Cancer
|
|
MLN120B dihydrochloride (ML120B dihydrochloride) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC50 of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis .
|
-
- HY-100706
-
|
|
DNA-PK
|
Cancer
|
|
AMA-37, an Arylmorpholine analog, is ATP-competitive DNA-PK inhibitor, with IC50 values of 0.27 μM (DNA-PK), 32 μM (p110α), 3.7 μM (p110β), and 22 μM (p110γ), respectively .
|
-
- HY-N8122
-
|
|
Akt
|
Cancer
|
|
24-Methylenecycloartanyl ferulate is a γ-oryzanol compound. 24-Methylenecycloartanyl ferulate promotes parvin-beta expression in human breast cancer cells. 24-Methylenecycloartanyl ferulate is a potential ATP-competitive Akt1 inhibitor (EC50= 33.3μM) .
|
-
- HY-101043
-
|
|
Sigma Receptor
iGluR
|
Neurological Disease
|
|
4-PPBP maleate is a potent σ 1 receptor ligand and agonist. 4-PPBP maleate is a non-competitive, selective NR1a/2B NMDA receptors (expressed in Xenopus oocytes) antagonist. 4-PPBP maleate provides neuroprotection .
|
-
- HY-10512S
-
-
- HY-113329
-
|
Taurocyamine
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Guanidinoethyl sulfonate (Taurocyamine), a transport antagonist of taurine, induces much urinary taurine excretion with a resulting decrease in the tissue taurine content and readily produces taurine-deficient fetal rats in pregnant rats . Guanidinoethyl sulfonate, a structural analogue of taurine, acts as a competitive inhibitor of taurine transport .
|
-
- HY-146387
-
|
|
Sirtuin
|
Neurological Disease
Cancer
|
|
SIRT5 inhibitor 3 (compound 46) is a potent and competitive SIRT5 inhibitor with an IC50 value of 5.9 μM. SIRT5 inhibitor 3 can inhibit SIRT5 desuccinylation. SIRT5 inhibitor 3 can be used for researching cancer and neurodegenerative diseases .
|
-
- HY-13966S2
-
|
2-DG-13C; 2-Deoxy-D-arabino-hexose-13C; D-Arabino-2-deoxyhexose-13C
|
Isotope-Labeled Compounds
Apoptosis
Hexokinase
HSV
|
Cancer
|
|
2-Deoxy-D-glucose- 13C is the 13C labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1][2].
|
-
- HY-113038A
-
|
2-Hydroxyglutarate disodium; 2-Hydroxyglutaric acid disodium; 2-Hydroxypentanedioic acid disodium
|
Histone Demethylase
Endogenous Metabolite
|
Cancer
|
|
α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases .
|
-
- HY-136990
-
|
|
Others
|
Cancer
|
|
GLPG0259 is a ATP-competitive inhibitor of MAPK-activated protein kinase 5 (MK5) with oral activity. GLPG0259 reduces inflammation and bone destruction in a mouse model of collagen-induced arthritis. GLPG0259 also inhibited the metastasis of prostate cancer (PCa) cells .
|
-
- HY-B0334AS1
-
|
CP45899-d2 sodium
|
Bacterial
Antibiotic
|
Infection
|
|
Sulbactam-d2 (sodium) is the deuterium labeled Sulbactam sodium[1]. Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex[2][3].
|
-
- HY-P4522
-
|
|
Endogenous Metabolite
|
Others
|
|
Bz-Ala-Arg is a dipeptide. Bz-Ala-Arg is also a spectrophotometric substrate (0.4 M pyridine formate, pH 4.25) of human pancreatic carboxypeptidase B and plasma carboxypeptidase N. Bz-Ala-Arg can be used to screen competitive inhibitors of these two enzymes .
|
-
- HY-156029
-
|
|
Others
|
Cancer
|
|
IA1-8H2 is a non-covalent, non-competitive inhibitor of PHPT1 (IC50: 3.4 μM). IA1-8H2 can be used for research of lung cancer, hepatocarcinoma, and renal cancer .
|
-
- HY-157220
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
Tolvaptan phosphate ester sodium, a prodrug of Tolvaptan (HY-17000), can be used in the study of cardiac edema. Tolvaptan is a selective, competitive and orally active vasopressin receptor 2 (V2R) antagonist with an IC50 of 1.28 μM for the inhibition of arginine vasopressin (AVP)-induced platelet aggregation .
|
-
- HY-157489
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-47 (compound 8H) is a non-competitive α-glucosidase (α-glucosidase) inhibitor with IC50 value is 38.2 μM and Ki value is 38.2 μM. α-Glucosidase-IN-47 can be used in diabetes research. .
|
-
- HY-B0199AS
-
|
RS 61443-d4 hydrochloride; TM-MMF-d4 hydrochloride
|
Bacterial
Endogenous Metabolite
Isotope-Labeled Compounds
|
Cancer
|
|
Mycophenolate Mofetil-d4 hydrochloride is deuterated labeled Mycophenolate mofetil hydrochloride (HY-B0199A). Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD) type I/II with IC50s of 39 nM and 27 nM, respectively.
|
-
- HY-N0471R
-
|
|
mAChR
|
Neurological Disease
|
|
L-Hyoscyamine (Standard) is the analytical standard of L-Hyoscyamine. This product is intended for research and analytical applications. L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205) .
|
-
- HY-139158
-
|
|
HIV
|
Infection
|
|
Ainuovirine is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI). Ainuovirine inhibits HIV replication by non-competitively binding to HIV reverse transcriptase and blocking the reverse transcription process of viral RNA. Ainuovirine can be used for human immunodeficiency virus (HIV) type 1 infection .
|
-
- HY-14567A
-
|
FUB-359 hydrochloride
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Ciproxifan (FUB 359) hydrochloride is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan hydrochloride displays low apparent affinity at other receptor subtypes. Ciproxifan hydrochloride can be used for the research of aging disorders and Alzheimer's disease .
|
-
- HY-129808
-
|
|
Others
|
Cardiovascular Disease
Cancer
|
|
VPC12249 is a competitive dual LPA1/LPA3 antagonist with Ki values of 137nM and 428 nM, respectively. VPC12249 inhibits calcium mobilization in HEK293T cells with a Ki value of ~130 nM. VPC12249 is promising for research of ovarian cancer and hypertensive diseases .
|
-
- HY-134525
-
|
|
iGluR
|
Others
|
|
Ro 8-4304 is a non-competitive, voltage-independent and state-dependent antagonist for NMDA receptor. Ro 8-4304 inhibits 10 μM NMDA-induced currents and 100 μM NMDA-induced currents with IC50s of 2.3 μM and 0.36 μM .
|
-
- HY-10262
-
|
|
IGF-1R
Insulin Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
BMS-536924 is an orally active, competitive and selective insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IR) inhibitor with IC50s of 100 nM and 73 nM, respectively. BMS-536924 has anti-cancer activity .
|
-
- HY-17000
-
|
OPC-41061
|
Vasopressin Receptor
Autophagy
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Tolvaptan is a selective, competitive and orally active vasopressin receptor 2 (V2R) antagonist with an IC50 of 1.28 μM for the inhibition of arginine vasopressin (AVP)-induced platelet aggregation. Tolvaptan induces cell apoposis and affects cell cycle. Tolvaptan can be used for the research of hyponatremia .
|
-
- HY-10253
-
AG1024
5 Publications Verification
Tyrphostin AG 1024
|
IGF-1R
Insulin Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
AG1024 (Tyrphostin AG 1024) is a reversible, competitive and selective IGF-1R inhibitor with an IC50 of 7 μM. AG1024 inhibits phosphorylation of IR (IC50=57 μM). AG1024 induces apoptosis and has anti-cancer activity .
|
-
- HY-18086
-
|
SC 204330
|
Pim
|
Cancer
|
|
TCS PIM-1 1 (SC 204330) is a potent, selective and ATP-competitive Pim-1 kianse inhibitor with an IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2 (IC50s >20000 nM) .
|
-
- HY-12335A
-
|
|
Histone Methyltransferase
|
Inflammation/Immunology
Cancer
|
|
UNC0379 TFA is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM, KD value of 18.3 μM. UNC0379 TFA can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma .
|
-
- HY-103392
-
|
BCX2600
|
Cytochrome P450
|
Neurological Disease
|
|
Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediatated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59±0.07 and 0.516±0.065 μM and IC50 of 1.58 and 3.29 μM, respectively.
|
-
- HY-101037
-
|
N-Methylglycine; Sarcosin
|
Endogenous Metabolite
GlyT
|
Cancer
|
|
Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia .
|
-
- HY-122629
-
|
|
DAPK
|
Others
|
|
DRAK2-IN-1, compound 16, is a potent, selective and ATP-competitive DRAK2 inhibitor with IC50and Kivalues of 3 nM and 0.26 nM, respectively.
DRAK2-IN-1 also has inbitory effect on DRAK1 (IC50=51 nM) .
|
-
- HY-B0574S2
-
|
|
Isotope-Labeled Compounds
COX
|
Inflammation/Immunology
|
|
Mefenamic acid- 13C6 is the 13C-labeled Mefenamic acid. Mefenamic acid is a non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively.
|
-
- HY-10805S
-
-
- HY-N0368
-
-
- HY-125833
-
|
|
Cytochrome P450
Aryl Hydrocarbon Receptor
Apoptosis
|
Cancer
|
|
Alpha-Naphthoflavone is an orally active flavonoid that is a potent, competitive inhibitor of aromatase< b>aromatase. < b > IC < sub > 50 < / sub > < / b > and < b > K < sub > I < / sub > < / b > value were 0.5 and 0.2 microns. Alpha-Naphthoflavone can inhibit cell proliferation and induce apoptosis .
|
-
- HY-136532
-
ZT-1a
1 Publications Verification
|
Others
|
Neurological Disease
|
|
ZT-1a is a potent, non-ATP-competitive and selective SPAK inhibitor. ZT-1a inhibits SPAK activity with IC50s of 44.3, 35.0, 46.7 μM at ATP concentrations of 0.01, 0.1 and 1 mM, respectively .
|
-
- HY-B0873
-
|
|
Cytochrome P450
ROS Kinase
|
Others
|
|
Uniconazole, a plant growth retardant, is a potent inhibitor of abscisic acid (ABA) catabolism with an IC50 of 68 nM against ABA 8’-hydroxylase. Uniconazole is a potent competitive inhibitor of CYP707A3 activity with a Ki of 8 nM. Uniconazole evidently inhibits gibberellin biosynthesis, and brassinosteroid biosynthesis is also inhibited to some extent .
|
-
- HY-135780
-
-
- HY-102062
-
|
N-omega-Propyl-L-arginine
|
NO Synthase
|
Neurological Disease
|
|
Nω-Propyl-L-arginine (N-omega-Propyl-L-arginine) is a potent, competitive, and highly selective inhibitor of neuronal nitric oxide synthase (nNOS), with a Ki of 57 nM. Nω-Propyl-L-arginine displays a 149-fold selectivity for nNOS over endothelial NOS (eNOS) .
|
-
- HY-P1293A
-
|
|
iGluR
|
Neurological Disease
|
|
Conantokin G TFA, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G TFA inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G TFA has neuroprotective properties .
|
-
- HY-100530B
-
-
- HY-100530C
-
|
|
PKA
Phosphodiesterase (PDE)
|
Neurological Disease
Metabolic Disease
|
|
Sp-cAMPS sodium salt, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS sodium salt is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS sodium salt binds the PDE10 GAF domain with an EC50 of 40 μM .
|
-
- HY-P2477
-
|
|
PD-1/PD-L1
|
Inflammation/Immunology
|
|
Human PD-L1 inhibitor IV, a polypeptide, is a competitive human PD-1 protein inhibitor with a Kd value of 1.38 μM. Human PD-L1 inhibitor IV inhibits the interaction of hPD-1/hPD-L1 .
|
-
- HY-30008
-
|
|
iGluR
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Cycloleucine is a specific inhibitor of S-adenosyl-methionine mediated methylation. Cycloleucine is antagonist of NMDA receptor associated glycine receptor, with a Ki of 600 μM. Cycloleucine is also a competitive inhibitor of ATP: L-methionine-S-adenosyl transferase in vitro. Cycloleucine has anxiolytic and cytostatic effects .
|
-
- HY-102062A
-
|
N-omega-Propyl-L-arginine hydrochloride
|
NO Synthase
|
Neurological Disease
|
|
Nω-Propyl-L-arginine (N-omega-Propyl-L-arginine) hydrochloride is a potent, competitive, and highly selective inhibitor of neuronal nitric oxide synthase (nNOS), with a Ki of 57 nM. Nω-Propyl-L-arginine hydrochloride displays a 149-fold selectivity for nNOS over endothelial NOS (eNOS) .
|
-
- HY-15003
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
ATH686 is a potent, selective and ATP-competitive FLT3 inhibitor. ATH686 target mutant FLT3 protein kinase activity and inhibit the proliferation of cells harboring FLT3 mutants via induction of apoptosis and cell cycle inhibition. ATH686 has antileukemic effects .
|
-
- HY-B0461S
-
|
|
mAChR
|
Neurological Disease
|
|
Trospium-d8 (chloride) is the deuterium labeled Trospium chloride. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors[1][2].
|
-
- HY-D0145S
-
|
Resorufin ethyl ether-d5
|
Isotope-Labeled Compounds
Cytochrome P450
NO Synthase
|
Others
|
|
7-Ethoxyresorufin-d5 is deuterium labeled 7-Ethoxyresorufin. 7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase[1][2].
|
-
- HY-17423B
-
|
|
HIV
Reverse Transcriptase
Telomerase
Apoptosis
|
Infection
Cancer
|
|
Abacavir monosulfate is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir monosulfate can inhibits the replication of HIV. Abacavir monosulfate shows anticancer activity in prostate cancer cell lines. Abacavir monosulfate can trespass the blood-brain-barrier and suppresses telomerase activity .
|
-
- HY-B0267C
-
|
Aroxybutynin
|
mAChR
|
Neurological Disease
|
|
(R)-Oxybutynin (Aroxybutynin) is the racemic isomer of Oxybutynin and an orally active muscarinic receptor antagonist. (R)-Oxybutynin has antispasmodic, antimuscarinic, and anticholinergic activities and competitively antagonizes carbachol-induced contractions. (R)-Oxybutynin can be used to study urinary incontinence caused by neurogenic bladder dysfunction .
|
-
- HY-12182A
-
|
|
Prostaglandin Receptor
|
Cancer
|
|
ONO-8711 dicyclohexylamine is a selective and orally active EP1 competitive antagonist with Ki value of 0.6 nM and 1.7 nM for human and mouse EP1 respectively. ONO-8711 dicyclohexylamine effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer .
|
-
- HY-15141G
-
|
Antibiotic AM-2282; STS; AM-2282
|
PKC
|
Infection
Cancer
|
|
Staurosporine (AM-2282) (GMP) is Staurosporine (HY-15141) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Staurosporine is a potent, ATP-competitive and non-selective inhibitor of protein kinases .
|
-
- HY-114203
-
-
- HY-107524
-
|
|
EAAT
|
Neurological Disease
|
|
(±)-HIP-B is a non-competitive excitatory amino acid transporter (EAAT) blocker that effectively blocks Glu uptake (IC50=17-18 μM). (±)-HIP-B is also a lead compound against ischemia-induced neuronal degeneration. (±)-HIP-B can be used in the study of neurological diseases .
|
-
- HY-N3136
-
|
|
Histamine Receptor
|
Others
|
|
Onitin is a natural product, that can be isolated from Onychium siliculosum. Onitin is also a non-competitive antagonist of histamine. Onitin shows activity in blocking the peristaltic reflex of the guinea-pig ileum, in inhibition of the responses of guinea-pig ileum to histamine and of inhibition of the responses of guinea-pig tracheal muscle to histamine .
|
-
- HY-114730
-
|
|
IKK
|
Inflammation/Immunology
|
|
CGA-JK3 is CGA-JK3 is an ATP-competitive inhibitor of IKKβ-catalyzed kinase activity. CGA-JK3 inhibits IκBα phosphorylation in LPS (HY-D1056) - induced RAW 264.7 cells .
|
-
- HY-161029
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
T14-A24 is an orally active, reversible, competitive, and selective AChE inhibitor (Ki=22 nM, IC50=6 nM). T14-A24 has benign BBB penetration, remarkable neuroprotective effect, and safe toxicological profile .
|
-
- HY-12866R
-
|
|
Trk Receptor
Apoptosis
|
Cancer
|
|
Larotrectinib (Standard) is the analytical standard of Larotrectinib. This product is intended for research and analytical applications. Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
- HY-17572AR
-
|
|
Oxytocin Receptor
Vasopressin Receptor
|
Endocrinology
Cancer
|
|
Atosiban (acetate) (Standard) is the analytical standard of Atosiban (acetate). This product is intended for research and analytical applications. Atosiban acetate (RW22164 acetate;RWJ22164 acetate) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research .
|
-
- HY-128041
-
|
Hydroxyfarnesyl phosphate
|
Others
|
Others
|
|
α-hydroxy Farnesyl phosphonic acid is a nonhydrolyzable analog of farnesyl pyrophosphate which acts as a competitive inhibitor of farnesyl transferase (FTase). At concentrations greater than 1 μM, α-hydroxy farnesyl phosphonic acid inhibits the processing of Ras in Ha-ras-transformed NIH3T3 cells.
|
-
- HY-122646
-
|
|
Deubiquitinase
MDM-2/p53
|
Cancer
|
|
USP7-IN-2 (compound 4) is a non-competitive USP7 inhibitor with an IC50 of 6 nM. USP7-IN-2 causes degradation of MDM2, stabilization of p53 and induction of p21 in multiple cell lines, and can be utilized in cancer research .
|
-
- HY-103430
-
|
|
Dopamine Receptor
5-HT Receptor
Adenylate Cyclase
|
Neurological Disease
|
|
SKF-83566 hydrobromide is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM) . SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM . SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta . SKF-83566 can be used for the research of parkinson’s disease and nicotine craving alleviation .
|
-
- HY-103430A
-
|
|
Dopamine Receptor
5-HT Receptor
Adenylate Cyclase
|
Neurological Disease
|
|
SKF-83566 is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM) . SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM . SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta . SKF-83566 can be used for research of parkinson’s disease and nicotine craving alleviation .
|
-
- HY-B0879AR
-
|
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
SARS-CoV
Parasite
Apoptosis
|
Infection
Cardiovascular Disease
Cancer
|
|
Suramin (sodium salt) (Standard) is the analytical standard of Suramin (sodium salt). This product is intended for research and analytical applications. Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor . Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM) . Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM) . Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor . Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent .
|
-
- HY-16638
-
|
PDDF
|
Thymidylate Synthase
|
Metabolic Disease
|
|
CB 3717 is a potent inhibitor of human thymidylate synthetase, competitively binding with 5,10-methylenetetrahydrofolate (Ki = 4.9 X 10(-9) M). It also competitively inhibits human dihydrofolate reductase with dihydrofolate (Ki = 2.3 X 10(-8) M). In WI-L2 human lymphoblastoid cells, CB 3717 treatment led to a significant decrease in cellular dTTP levels and a notable increase in dUMP levels, indicating a disruption in nucleotide metabolism. The growth-inhibitory effect of CB 3717 was reversed by thymidine supplementation, demonstrating that thymidylate synthetase became rate-limiting in the presence of this compound. Delayed thymidine supplementation beyond 8 hours resulted in severe cytotoxicity, underscoring the critical timing of nucleotide rescue strategies in CB 3717-treated cells .
|
-
- HY-11005
-
BX-912
4 Publications Verification
|
PDK-1
Apoptosis
|
Cancer
|
|
BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis .
|
-
- HY-B0371A
-
|
|
Adrenergic Receptor
|
Metabolic Disease
Endocrinology
|
|
Terazosin hydrochloride dihydrate is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin hydrochloride dihydrate works by relaxing blood vessels and the opening of the bladder. Terazosin hydrochloride dihydrate has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment .
|
-
- HY-18637
-
|
|
Deubiquitinase
Apoptosis
|
Neurological Disease
|
|
LDN-57444 is a reversible, competitive and site-directed inhibitor of ubiquitin C-terminal hydrolase L1 (UCH-L1), with an IC50 of 0.88 μM and a Ki of 0.40 μM; LDN-57444 also suppresses UCH-L3 activity, with an IC50 of 25 μM.
|
-
- HY-15658
-
GSK2801
2 Publications Verification
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
GSK2801 is a potent, selective, orally active and cell active acetyl-lysine competitive BAZ2A and BAZ2B bromodomains inhibitor with Kd values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for BAZ2A/B over BRD4 .
|
-
- HY-10119
-
|
SCH 530348
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-10403
-
-
- HY-101920
-
|
|
Autophagy
PI3K
|
Neurological Disease
Cancer
|
|
Autophinib is a potent, selective autophagy inhibitor with IC50s of 90 nM and 40 nM for starvation- and Rapamycin-induced autophagy, respectively. Autophinib is also an ATP competitive Vacuolar Protein Sorting 34 (VPS34) inhibitor with an IC50 of 19 nM. Autophinib inhibits autophagy induced by starvation or Rapamycin by targeting VPS34 .
|
-
- HY-111383
-
-
- HY-N1919
-
|
Raubasine
|
Adrenergic Receptor
Cholinesterase (ChE)
|
Neurological Disease
Endocrinology
|
|
Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity .
|
-
- HY-13965
-
|
ML161
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM . Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo .
|
-
- HY-121515
-
|
|
Phosphatase
|
Metabolic Disease
|
|
DPM-1001 is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM. DPM-1001 is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 has anti-diabetic property .
|
-
- HY-23460
-
|
4-Ethynyl-L-phenylalanine
|
Tryptophan Hydroxylase
|
Neurological Disease
|
|
p-Ethynylphenylalanine (4-Ethynyl-L-phenylalanine) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a Ki of 32.6 μM . p-Ethynylphenylalanine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-W009156
-
-
- HY-B1866
-
|
|
Androgen Receptor
|
Endocrinology
|
|
Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive androgen receptor (AR) antagonist with a Ki of 100 μM. Linuron shows reproductive toxicity in animals that acts as an endocrine disruptor .
|
-
- HY-P1115
-
|
|
Akt
|
Others
|
|
AKTide-2T is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position .
|
-
- HY-113468AS
-
|
3-Methoxy-L-tyrosine-d3; 3-O-Methyl-L-DOPA-d3
|
Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
3-O-Methyldopa-d3 is deuterium labeled 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine[1].
|
-
- HY-23460A
-
|
4-Ethynyl-L-phenylalanine hydrochloride
|
Tryptophan Hydroxylase
|
Neurological Disease
|
|
p-Ethynylphenylalanine hydrochloride (4-Ethynyl-L-phenylalanine hydrochloride) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a Ki of 32.6 μM . p-Ethynylphenylalanine (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-137472
-
|
|
GSK-3
|
Neurological Disease
|
|
SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC50 of 12 nM for human GSK-3β. SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD) .
|
-
- HY-U00302
-
|
|
mAChR
|
Inflammation/Immunology
|
|
CHF5407 is a selective, long-acting and competitive muscarinic M3 receptor antagonist. CHF5407 shows subnanomolar affinities for human muscarinic M1 (hM1), M2 (hM2) and M3 (hM3) receptors. CHF5407 shows a prolonged antibronchospastic activity .
|
-
- HY-121515A
-
|
|
Phosphatase
|
Metabolic Disease
|
|
DPM-1001 trihydrochloride is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM. DPM-1001 trihydrochloride is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 trihydrochloride has anti-diabetic property .
|
-
- HY-137506
-
-
- HY-117743
-
|
SKF-108566J free base
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
|
-
- HY-108913
-
|
|
Beta-lactamase
Antibiotic
|
Infection
|
|
Nitrocefin is a chromogenic β-lactamase substrate that undergoes a distinctive color change from yellow to red as the amide bond in the β-lactam ring is hydrolyzed by β-lactamase. Nitrocefin is used in competitive inhibition studies in developmental work on β-lactamase-resistant antibiotics .
|
-
- HY-Y0413
-
|
Diacetyl monoxime; DAM
|
Na+/K+ ATPase
Myosin
|
Metabolic Disease
|
|
Biacetyl monoxime (Diacetyl monoxime), a myosin ATPase inhibitor, is a skeletal and cardiac muscle contraction inhibitor. Biacetyl monoxime is also a well-characterized non-competitive inhibitor of chemical and motile activity of skeletal muscle myosin-II. Biacetyl monoxime induces sarcoplasmic reticulum Ca 2+ release .
|
-
- HY-A0230
-
|
SCH 33844
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Spirapril is a potent and cross the blood-brain barrier angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril competitively binds to ACE and prevents the conversion of angiotensin I to angiotensin II. Spirapril is an orally active proagent of Spiraprilat and can be used for the research of hypertension, congestive heart failure .
|
-
- HY-N1919A
-
|
Raubasine hydrochloride
|
Adrenergic Receptor
Cholinesterase (ChE)
|
Neurological Disease
Endocrinology
|
|
Ajmalicine (Raubasine) hydrochloride is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine hydrochloride is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine hydrochloride also can be used as anti-hypertensive, and serpentine, with sedative activity .
|
-
- HY-106840A
-
|
|
Cholecystokinin Receptor
|
Neurological Disease
Metabolic Disease
|
|
L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors .
|
-
- HY-150207
-
|
|
PARP
|
Inflammation/Immunology
|
|
RBN-3143 is a potent and NAD+-competitive catalytic PARP14 inhibitor with an IC50 value of 4 nM. RBN-3143 inhibits PARP14-mediated ADP-ribosylation and stabilizes PARP14 in cell lines. RBN-3143 can be used in research of lung inflammation .
|
-
- HY-120041
-
|
|
IRAK
|
Cancer
|
|
ND-2158 is a competitive IRAK4 inhibitor, with the Ki of 1.3 nM. ND-2158 suppresses LPS-induced TNF production in human white blood cells, alleviated collagen-induced arthritis, and blocked gout formation in mouse models. ND-2158 has antitumor activity in vivo .
|
-
- HY-N8382
-
|
|
Cytochrome P450
|
Neurological Disease
|
|
Chalepensin, a furanocoumarin, is a competitive CYP2A6 inhibitor. Chalepensin also inhibits human CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to different extents .
|
-
- HY-N9933
-
|
TβMCA
|
FXR
Apoptosis
|
Metabolic Disease
Cancer
|
|
Tauro-β-muricholic acid (TβMCA) is a trihydroxylated bile acid. Tauro-β-muricholic acid is a competitive and reversible FXR antagonist (IC50 = 40 μM). Tauro-β-muricholic acid has antiapoptotic effect. Tauro-β-muricholic acid inhibits bile acid-induced hepatocellular apoptosis by maintaining the mitochondrial membrane potential .
|
-
- HY-19881
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
ABT-288 is a competitive, potent and selective histamine H3 receptor (H3R) antagonist. ABT-288 has Ki values of 1.9 and 8.2 nM for human and rat H3Rs, respectively. ABT-288 can be used in cognitive impairment research. .
|
-
- HY-160564
-
|
|
EGFR
|
Cancer
|
|
ZNL-0056 is an orally active ATP-competitive inhibitor that targets both the Cys797 and Cys775 in the ATP binding site of EGFR. ZNL-0056 selectively inhibits EGFR and its downstream signaling in H3255 cells. ZNL-0056 can be used for the research of cancer .
|
-
- HY-112349
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
SB 203580 sulfone is an analog of p38 MAP kinase inhibitor SB 203580, which inhibits the IL-1 production in monocytes with an IC50 of 0.2 μM and binds competitively with CSAID binding proteins (CSBP), inhibits it mediated stress response signaling with an IC50 of 0.03 μM .
|
-
- HY-160624
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
CD 10899 is a hydroxylated metabolite of Volasertib (HY-12137). CD 10899 is pharmacologically active against Polo-like kinase 1 (PLK1) (IC50: 6 nM). Volasertib is an orally active, highly potent and ATP-competitive PLK1 inhibitor. CD 10899 can be used for research of cancer .
|
-
- HY-19010A
-
|
SKF 94482 hydrochloride
|
Histamine Receptor
|
Neurological Disease
|
|
BMY-25368 hydrochloride is a histamine H2 receptor antagonist that acts as a gastric acid secretion inhibitor. BMY-25368 hydrochloride competitively antagonizes gastric secretion stimulated by histamine and also antagonizes gastric secretion stimulated by Pentagastrin (HY-A0261), Bethanechol (HY-B0406), and food .
|
-
- HY-B0574R
-
|
|
COX
|
Inflammation/Immunology
|
|
Mefenamic acid (Standard) is the analytical standard of Mefenamic acid. This product is intended for research and analytical applications. Mefenamic acid is a non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively.
|
-
- HY-121094
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Androgen receptor allosteric antagonist 1(compound D36)is a a llosteric, competitive androgen receptor (AR) antagonist with the Ki of 9 μM. Androgen receptor allosteric antagonist 1 inhibits R1881-mediated transcription and proliferation and can be used for study of prostate cancer .
|
-
- HY-W653723R
-
|
|
Androgen Receptor
|
Endocrinology
|
|
N-Nitrosodicyclohexylamine (Standard) is the analytical standard of N-Nitrosodicyclohexylamine. This product is intended for research and analytical applications. N-Nitrosodicyclohexylamine (NDCHA) is a N-nitrosocompound with anti-androgenic activities. N-Nitrosodicyclohexylamine shows the competitive binding to androgen receptor (AR) against 5α-dihydrotestosterone and decreased the level of AR protein .
|
-
- HY-138813A
-
|
(E/Z)-SU-12662 hydrochloride
|
Others
|
Cancer
|
|
(E/Z)-N-Desethylsunitinib hydrochloride ((E/Z)-SU-12662 hydrochloride) is a compound with potential anti-tumor activity that inhibits VEGF-R2 and PDGF-Rβ tyrosine kinases. (E/Z)-N-Desethylsunitinib hydrochloride is the main active metabolite of sunitinib and has the ability to competitively inhibit ATP .
|
-
- HY-10014
-
R547
2 Publications Verification
|
CDK
GSK-3
Apoptosis
|
Cancer
|
|
R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively .
|
-
- HY-12062
-
|
|
MEK
|
Cancer
|
|
PD318088 is a potent, allosteric and non-ATP competitive MEK1/2 inhibitor, an analog of PD184352 (HY-50295). PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. PD318088 can be used for cancer research .
|
-
- HY-50847
-
|
|
PI3K
Autophagy
|
Cancer
|
|
ZSTK474 is an ATP-competitive pan-class I PI3K inhibitor with IC50s of 16 nM, 44 nM, 4.6 nM and 49 nM for PΙ3Κα, PI3Kβ, PI3Kδ and PI3Kγ, respectively.
|
-
- HY-15517
-
KN-92
5 Publications Verification
|
Others
|
Cancer
|
|
KN-92 is an inactive derivative of KN-93, without CaM kinase inhibitory activity. KN-92 is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 is a cell-permeable, reversible and competitive CaMKII inhibitor .
|
-
- HY-15517A
-
|
|
Others
|
Cancer
|
|
KN-92 phosphate is an inactive derivative of KN-93, without CaM kinase inhibitory activity. KN-92 phosphate is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 is a cell-permeable, reversible and competitive CaMKII inhibitor .
|
-
- HY-17423A
-
|
Abacavir Hemisulfate; ABC sulfate
|
Reverse Transcriptase
HIV
Telomerase
Apoptosis
|
Infection
|
|
Abacavir sulfate (Abacavir Hemisulfate) is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir sulfate can inhibits the replication of HIV. Abacavir sulfate shows anticancer activity in prostate cancer cell lines. Abacavir sulfate can trespass the blood-brain-barrier and suppresses telomerase activity .
|
-
- HY-13038A
-
|
R788
|
Syk
FLT3
|
Inflammation/Immunology
Cancer
|
|
Fostamatinib (R788) is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-B0305A
-
|
HOE 760
|
Histamine Receptor
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Roxatidine Acetate Hydrochloride is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine Acetate Hydrochloride has antisecretory potency against gastric acid secretion. Roxatidine Acetate Hydrochloride can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine Acetate Hydrochloride has antitumor activity .
|
-
- HY-B0488
-
|
L631529; MK401
|
Parasite
|
Infection
|
|
Clorsulon (L631529; MK401) is an orally active flukicidal agent against liver flukes (Fasciola hepatica and Fasciola gigantica) infections in calves and sheep. Clorsulon is also a competitive inhibitor of both 3-phosphoglycorate and ATP andinhibits glucose utilization and acetate and propionate formation by mature Fasciola hepatica in vitro .
|
-
- HY-15141
-
|
Antibiotic AM-2282; STS; AM-2282
|
PKC
PKA
Apoptosis
Bacterial
Fungal
Antibiotic
|
Infection
Cancer
|
|
Staurosporine is a potent, ATP-competitive and non-selective inhibitor of protein kinases with IC50s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase respectively. Staurosporine also inhibits TAOK2 with an IC50 of 3 μM. Staurosporine is an apoptosis inducer .
|
-
- HY-13859
-
|
L-FMAU
|
HBV
DNA/RNA Synthesis
Orthopoxvirus
|
Infection
|
|
Clevudine (L-FMAU), a nucleoside analog of the unnatural L-configuration, has potent anti-HBV activity with long half-life, low toxicity. Clevudine is a non-competitive inhibitor that is not incorporated into the viral DNA but rather binds to the polymerase. Clevudine is active against cowpox virus respiratory infection in mice .
|
-
- HY-B0876
-
|
4-Methylpyrazole
|
Cytochrome P450
|
Metabolic Disease
|
|
Fomepizole (4-Methylpyrazole) is a potent cytochrome P450 (CYP2E1) inhibitor. Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole has the potential for an antidote for ethylene glycol or methanol poisoning .
|
-
- HY-101870B
-
|
INCB053914 phosphate
|
Pim
|
Cancer
|
|
Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
|
-
- HY-16214
-
|
LDHA Inhibitor FX11
|
Lactate Dehydrogenase
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
FX-11 is a potent, selective, reversible and competitive lactate dehydrogenase A (LDHA) inhibitor, with a Ki of 8 μM. FX-11 reduces ATP levels and induces oxidative stress, ROS production and cell death. FX-11 shows antitumor activity in lymphoma and pancreatic cancer xenografts .
|
-
- HY-B0574S
-
|
|
COX
|
Inflammation/Immunology
|
|
Mefenamic acid-d4 is a deuterium labeled Mefenamic acid. Mefenamic acid is a non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively[1][2].
|
-
- HY-10163S1
-
|
BIBR 953-d3; BIBR 953ZW-d3
|
Thrombin
|
Cardiovascular Disease
|
|
Dabigatran-d3 is the deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
|
-
- HY-15010
-
|
|
Oxytocin Receptor
Vasopressin Receptor
|
Endocrinology
|
|
L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM) .
|
-
- HY-107642
-
|
|
Motilin Receptor
|
Metabolic Disease
|
|
MA-2029 is a selective, orally active, and competitive motilin receptor antagonist (IC50=4.9 nM). MA-2029 is selective for the motilin receptor over various other receptors and ion channels. MA-2029 may be useful for gastrointestinal disorders associated with disturbed gastrointestinal motility .
|
-
- HY-50688
-
|
|
CXCR
|
Inflammation/Immunology
|
|
SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC50s of 3.7 nM and 70 nM, respectively .
|
-
- HY-107597
-
Halicin
1 Publications Verification
SU3327
|
JNK
|
Metabolic Disease
Inflammation/Immunology
|
|
Halicin (SU3327) is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. Halicin also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. Halicin shows less active against p38α and Akt kinase .
|
-
- HY-13333
-
|
BAG 956
|
PI3K
|
Cancer
|
|
NVP-BAG956 is an ATP-competitive PI3K inhibitor with IC50s of 34, 56, 112 and 444 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
|
-
- HY-10119A
-
|
SCH 530348 sulfate
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-110150
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
UNC3230 is a potent, selective and ATP-competitive PIP5K1C inhibitor with an IC50 of ~41 nM. UNC3230 also inhibits PIP4K2C and does not inhibit any of the other lipid kinases that regulate phosphoinositide levels. UNC3230 has antinociceptive and anticancer effects .
|
-
- HY-100429
-
CAN508
1 Publications Verification
|
CDK
|
Cancer
|
|
CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity .
|
-
- HY-112390A
-
|
|
Syk
5-HT Receptor
|
Inflammation/Immunology
|
|
Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect .
|
-
- HY-P1297
-
|
|
CRFR
|
Neurological Disease
|
|
CRF(6-33)(human) is a CRF binding protein (CRF-BP) ligand inhibitor. CRF(6-33)(human) competitively binds the CRF-BP but not the post-synaptic CRF receptors. CRF(6-33)(human) has anti-obesity effect .
|
-
- HY-10255
-
|
SU 11248 Malate
|
PDGFR
VEGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
|
-
- HY-B1558A
-
|
MCI-2016
|
Monoamine Oxidase
|
Neurological Disease
|
|
Bifemelane hydrochloride (MCI-2016) is a potent, selective and competitive inhibitor of monoamine oxidase A (MAO-A), with a Ki of 4.20 μM. Bifemelane hydrochloride also inhibits MAO-B noncompetitively with a Ki of 46.0 μM. Bifemelane hydrochloride has a potent antidepressant activity and can be used for the research of cognitive and emotional disturbances related to cerebrovascular disease .
|
-
- HY-107365
-
|
|
PI3K
mTOR
|
Cancer
|
|
PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar Kd toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity .
|
-
- HY-105327
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
P11149 is a competitive, BBB-penetarated weakly, orally active and selective inhibitor of AChE. P11149 exhibits an IC50 of 1.3 μM for rat BChE/AChE. P11149, a Galanthamine derivative, demonstrates central cholinergic activity, behavioral efficacy and safety. P11149 is used in the study for Alzheimer's disease .
|
-
- HY-P2244
-
|
|
YAP
|
Cancer
|
|
YAP-TEAD-IN-1 is a potent and competitive inhibitor of?YAP–TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd=40 nM) .
|
-
- HY-139481
-
|
|
Btk
|
Infection
Cancer
|
|
TL-895 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor with an IC50 and a Ki of 1.5 nM and 11.9 nM, respectively . TL-895 is used be for JAKi-relapsed/refractory myelofibrosis, acute myeloid leukemia, COVID-19 and cancer research .
|
-
- HY-101870
-
|
INCB053914
|
Pim
|
Cancer
|
|
Uzansertib (INCB053914) is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
|
-
- HY-B0251S
-
|
Epoxymexrenone-d3
|
Mineralocorticoid Receptor
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Eplerenone-d3 is the deuterium labeled Eplerenone. Eplerenone (Epoxymexrenone) is a selective, competitive and oreally active aldosterone antagonist with an IC50 of 138 nM. Eplerenone has low affinity for progesterone, androgen, estrogen and glucocorticoid receptors. Eplerenone can be used for hypertension and heart failure after myocardial infarction reserch[1][2].
|
-
- HY-115741
-
|
|
Others
|
Neurological Disease
Cancer
|
|
3BrB-PP1 is an ATP-competitive analog. 3BrB-PP1 can specifically inhibit the activity of protein kinase with mutations in the ATP-binding pocket (mutation of Thr97 within Sty1’s ATP-binding pocket) .
|
-
- HY-10163S
-
|
BIBR 953-d4; BIBR 953ZW-d4
|
Isotope-Labeled Compounds
Thrombin
|
Cardiovascular Disease
|
|
Dabigatran-d4 is deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
|
-
- HY-147040
-
|
|
c-Met/HGFR
|
Cancer
|
|
ABN401 is a highly potent and selective ATP-competitive c-MET inhibitor with an IC50 value of 10 nM. ABN401 has cytotoxic activity against MET-addicted cancer cells. ABN401 can inhibit c-MET phosphorylation in tumor tissues. ABN401 can be used for researching anticancer .
|
-
- HY-B0305
-
|
|
Histamine Receptor
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Roxatidine acetate is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine acetate has antisecretory potency against gastric acid secretion. Roxatidine acetate can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine acetate has antitumor activity .
|
-
- HY-13966S4
-
|
2-DG-13C-1; 2-Deoxy-D-arabino-hexose-13C-1; D-Arabino-2-deoxyhexose-13C-1
|
Isotope-Labeled Compounds
Apoptosis
Hexokinase
HSV
|
Cancer
|
|
2-Deoxy-D-glucose- 13C-1 is the 13C labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1][2].
|
-
- HY-151627
-
-
- HY-112390
-
|
|
5-HT Receptor
Syk
|
Inflammation/Immunology
|
|
Syk Inhibitor II dihydrochloride is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride shows less potent against other kinases and has anti-allergic effect .
|
-
- HY-148757
-
|
|
CaMK
|
Metabolic Disease
|
|
TIM-063 is a selective and cell-permeable CaMKK inhibitor, ATP competitive inhibitor, can directly target the catalytic domain of CaMKK, with the Ki values of 0.35 μM and 0.2 μM for CaMKKα and CaMKKβ, respectively, the IC50 values are 0.63 μM and 0.96 μM, respectively .
|
-
- HY-N4037
-
|
(-)-Homopterocarpin; 3,9-Dimethoxypterocarpan
|
Monoamine Oxidase
|
Inflammation/Immunology
|
|
Homopterocarpin is an isoflavonoid that can be isolated from Pterocarpus erinaceus. Homopterocarpin has hepatoprotective and antioxidant properties. Homopterocarpin is a competitive reversible inhibitor of human monoamine oxidase-B with an IC50 and a Ki of 0.72 and 0.21 μM for hMAO-B, respectively. Homopterocarpin can be used for the research of liver injury and oxidative stress .
|
-
- HY-P5305A
-
|
|
GABA Receptor
|
Metabolic Disease
|
|
GAD65(247-266) epitope TFA is the T cell epitopes of islet antigens，binding to I-A g7 (type I diabetes-associated molecule) competitively with poor affinity. GAD65 refers to Glutamic Acid Decarboxylase 65，involved in the conversion of glutamate to gamma-aminobutyric acid (GABA) .
|
-
- HY-149515
-
|
|
Monoamine Oxidase
|
Cancer
|
|
MAO-IN-3 (Compound 5) is a reversible and competitive MAO inhibitor (Ki: 0.6 and 0.2 μM for MAO A and MAO B). MAO-IN-3 inhibits LN-229 glioblastoma cell proliferation with an IC50 of 0.8 μM. MAO-IN-3 can be used for cancer research .
|
-
- HY-123206
-
|
|
5-HT Receptor
|
Inflammation/Immunology
|
|
R-96544 (free base) is a potent, selective and competitive 5-HT2 receptor antagonist. R-96544 (free base) inhibits platelet aggregation induced by serotonin, and inhibits 5-HT2A receptor-mediated contraction of guinea pig trachea .
|
-
- HY-157068
-
|
|
Ferroptosis
|
Cancer
|
|
icFSP1 is a potent ferroptosis suppressor protein-1 (FSP1) inhibitor. icFSP1 does not competitively inhibit FSP1 enzyme activity, but instead triggers subcellular relocalization of FSP1 from the membrane and FSP1 condensation before ferroptosis induction, in synergism with GPX4 inhibition .
|
-
- HY-10337R
-
|
|
VEGFR
Autophagy
|
Cancer
|
|
Brivanib (Standard) is the analytical standard of Brivanib. This product is intended for research and analytical applications. Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β .
|
-
- HY-14281R
-
|
|
Others
|
Endocrinology
Cancer
|
|
Trilostane (Standard) is the analytical standard of Trilostane. This product is intended for research and analytical applications. Trilostane (Win 24540) is a competitive and orally active 3-β-hydroxysteroiddehydrogenase (3β-HSD) inhibitor. Trilostane is a synthetic nonhormonal steroid. Trilostane can be used for the research of breast cancer and prostate cancer .
|
-
- HY-A0166R
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Cilastatin (Standard) is the analytical standard of Cilastatin. This product is intended for research and analytical applications. Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct .
|
-
- HY-N0301R
-
|
|
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Thiocolchicoside (Standard) is the analytical standard of Thiocolchicoside. This product is intended for research and analytical applications. Thiocolchicoside is a competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties .
|
-
- HY-125221
-
|
|
ROCK
|
Cancer
|
|
DJ4 is a ATP-competitive inhibitor of ROCK1/2 (IC50 values:5 and 50 nM) and MRCKα/β (IC50 values:10 and 100 nM). DJ4 blocks stress fiber formation and induces cell apoptosis. DJ4 can be used for study of cancer .
|
-
- HY-112390C
-
|
|
5-HT Receptor
Syk
|
Inflammation/Immunology
|
|
Syk Inhibitor II hydrochloride is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II hydrochloride inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II hydrochloride shows less potent against other kinases and has anti-allergic effect .
|
-
- HY-P4522A
-
|
|
Endogenous Metabolite
|
Others
|
|
Bz-Ala-Arg TFA is a dipeptide. Bz-Ala-Arg TFA is also a spectrophotometric substrate (0.4 M pyridine formate, pH 4.25) of human pancreatic carboxypeptidase B and plasma carboxypeptidase N. Bz-Ala-Arg TFA can be used to screen competitive inhibitors of these two enzymes .
|
-
- HY-B0461R
-
|
|
mAChR
|
Neurological Disease
|
|
Trospium (chloride) (Standard) is the analytical standard of Trospium (chloride). This product is intended for research and analytical applications. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
|
-
- HY-111260
-
|
|
CDK
GSK-3
Apoptosis
|
Cancer
|
|
R547 mesylate is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively .
|
-
- HY-120418
-
|
|
Others
|
Others
|
|
L-687306 is a high affinity muscarinic M1 receptor partial agonist with activity as a partial agonist of M1 receptors in rat ganglia and as a high affinity competitive antagonist at guinea pig cardiac M2 and ileal M3 muscarinic receptors, useful for studying the receptor reserve of muscarinic receptors.
|
-
- HY-107339A
-
|
Harmonyl hydrochloride
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Deserpidine hydrochloride (Harmonyl hydrochloride) is an antihypertensive compound that competitively inhibits the activity of angiotensin converting enzyme (ACE). Deserpidine hydrochloride competes with angiotensin I for ACE, preventing the conversion of angiotensin I to angiotensin II, thereby lowering blood pressure. Deserpidine hydrochloride can also reduce angiotensin II-induced aldosterone secretion from the adrenal cortex .
|
-
- HY-10229
-
|
AMG 706 Diphosphate
|
c-Kit
VEGFR
|
Cancer
|
|
Motesanib Diphosphate (AMG 706 Diphosphate) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is approximately 10-fold more selective for VEGFR than PDGFR and Ret.
|
-
- HY-13038
-
|
R788(Disodium)
|
Syk
FLT3
|
Inflammation/Immunology
Cancer
|
|
Fostamatinib Disodium (R788 Disodium) is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-12041
-
|
|
JNK
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
|
SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 induces the transformation of bladder cancer cells from autophagy to apoptosis .
|
-
- HY-10044
-
|
WYE-125132
|
mTOR
Apoptosis
|
Cancer
|
|
WYE-132 (WYE-125132) is a highly potent, ATP-competitive, and specific mTOR kinase inhibitor (IC50: 0.19±0.07 nM; >5,000-fold selective versus PI3Ks). WYE-132 (WYE-125132) inhibits mTORC1 and mTORC2.
|
-
- HY-13454
-
|
|
PKD
|
Cancer
|
|
CID 2011756 is an ATP competitive PKD inhibitor, with an IC50 of 3.2 μM for PKD1 in cell free assay, and also shows cellular pan-PKD inhibitory activity against PKD2 and PKD3 (IC50, 0.6 and 0.7 μM, respectively). CID 2011756 also has antitumor activity.
|
-
- HY-14722A
-
|
|
JAK
|
Cancer
|
|
NVP-BSK805 dihydrochloride is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively .
|
-
- HY-13038B
-
|
R788 disodium hexahydrate
|
Syk
FLT3
|
Inflammation/Immunology
Cancer
|
|
Fostamatinib (R788) disodium hexahydrate is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-15945
-
DBeQ
3 Publications Verification
JRF 12
|
p97
Autophagy
Apoptosis
|
Cancer
|
|
DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC50 value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4 with an IC50 of 11.5 μM.
|
-
- HY-B0607
-
|
NTBC; Nitisone; SC0735
|
HPPD
|
Metabolic Disease
|
|
Nitisinone is an orally active, competitive and reversible 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) inhibitor with an IC50 of 173 nM. Nitisinone promotes tyrosine accumulation in a dose-dependent manner. nitisinone can be used in studies of hereditary tyrosinemia type 1 (HT-1) (a rare genetic disorder) and albinism .
|
-
- HY-15908
-
BCA
5 Publications Verification
Disodium bicinchoninate
|
Beta-secretase
|
Neurological Disease
Cancer
|
|
BCA (Disodium bicinchoninate) is an orally active and non-competitive Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 value of 28 µM, a Ki value of 43 µM. BCA shows anticancer activity. BCA has the potential for the research of Alzheimer's disease (AD) .
|
-
- HY-N0192
-
Arbutin
1 Publications Verification
β-Arbutin
|
Tyrosinase
Endogenous Metabolite
|
Cancer
|
|
Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase, with Ki app values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents . Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties .
|
-
- HY-16071
-
AT13148
2 Publications Verification
|
Akt
PKA
ROCK
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
AT13148 is an orally active and ATP-competitive, multi-AGC kinase inhibitor with IC50s of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively.
|
-
- HY-B1295
-
-
- HY-15703
-
QNZ46
1 Publications Verification
|
iGluR
|
Neurological Disease
|
|
QNZ46 is a NR2C/NR2D-selective NMDA receptor non-competitive antagonist (IC50 values are 3, 6, 229, and >300, >300 μM for NR2D, NR2C, NR2A, NR2B, and GluR1, respectively).
|
-
- HY-19928
-
|
EW-7197; TEW-7197
|
TGF-β Receptor
|
Cancer
|
|
Vactosertib (EW-7197) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib has potently antimetastatic activity and anticancer effect .
|
-
- HY-A0030
-
|
|
mAChR
|
Neurological Disease
Metabolic Disease
|
|
Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .
|
-
- HY-100125
-
|
SR1368
|
COX
|
Inflammation/Immunology
|
|
Timegadine, a new antiinflammatory agent, is found to be a potent, competitive inhibitor of cyclo-oxygenase (COX) and lipo-oxygenase, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates, and in washed rabbit platelets.
|
-
- HY-19928A
-
|
EW-7197 Hydrochloride; TEW-7197 Hydrochloride
|
TGF-β Receptor
|
Cancer
|
|
Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect .
|
-
- HY-17462
-
|
(+)-Adrenosterone
|
Androgen Receptor
Endogenous Metabolite
|
Endocrinology
Cancer
|
|
Adrenosterone ((+)-Adrenosterone) is a competitive hydroxysteroid (11-beta) dehydrogenase 1 (HSD11β1) inhibitor.
Adrenosterone is a steroid hormone with weak androgenic effect. Adrenosterone is a dietary supplement that can decrease fat and increase muscle mass. Adrenosterone acts as a suppressor of metastatic progression of human cancer cells .
|
-
- HY-107526
-
|
(Rac)-NFPS
|
GlyT
|
Neurological Disease
|
|
NFPS is a selective, non-competitive glycine transporter-1 (GlyT1) inhibitor with IC50s of 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively . NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion .
|
-
- HY-135111
-
|
|
Drug Metabolite
|
Infection
Metabolic Disease
Cancer
|
|
4-Desmethoxy Omeprazole is the active metabolite of Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .
|
-
- HY-135892
-
|
|
MAP4K
|
Inflammation/Immunology
|
|
GNE-1858 is a potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA, respectively .
|
-
- HY-P2244A
-
|
|
YAP
|
Cancer
|
|
YAP-TEAD-IN-1 TFA is a potent and competitive peptide inhibitor of?YAP-TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 TFA is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd= 40 nM) .
|
-
- HY-70053
-
|
|
mAChR
|
Neurological Disease
Metabolic Disease
|
|
Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB) .
|
-
- HY-W015445
-
|
|
p38 MAPK
|
Metabolic Disease
|
|
SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation .
|
-
- HY-14722C
-
|
|
JAK
|
Cancer
|
|
NVP-BSK805 trihydrochloride trihydrochloride is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively .
|
-
- HY-14722
-
|
|
JAK
|
Cancer
|
|
NVP-BSK805 is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively .
|
-
- HY-108847
-
|
|
TNF Receptor
Bacterial
|
Inflammation/Immunology
Cancer
|
|
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis .
|
-
- HY-15999A
-
|
PRT062070 hydrochloride; PRT2070 hydrochloride
|
Syk
JAK
|
Cancer
|
|
Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with IC50s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK and Tyk2, JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies .
|
-
- HY-P1115A
-
|
|
Akt
|
Others
|
|
AKTide-2T TFA is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T TFA mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position .
|
-
- HY-P1264
-
|
|
nAChR
|
Neurological Disease
|
|
α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC50 of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM .
|
-
- HY-P1380A
-
|
|
Apoptosis
|
Cancer
|
|
Difopein (TFA), a specific and competitive inhibitor of 14-3-3 protein (a highly conserved eukaryotic regulatory molecule), blocking the ability of 14-3-3 to bind to target proteins and inhibits 14-3-3/Ligand interactions. Difopein (TFA) leads to induction of apoptosis and enhances the ability of cisplatin to kill cells .
|
-
- HY-120994
-
|
|
PKA
|
Neurological Disease
Inflammation/Immunology
|
|
Rp-8-CPT-cAMPS sodium, a cAMP analog, is a potent and competitive antagonist of cAMP-induced activation of cAMP-dependent PKA I and II. Rp-8-CPT-cAMPS sodium preferentially selects site A of RI compares to site A of RII and site B of RII compares to site B of RI .
|
-
- HY-120994A
-
|
|
PKA
|
Neurological Disease
Inflammation/Immunology
|
|
Rp-8-CPT-cAMPS, a cAMP analog, is a potent and competitive antagonist of cAMP-induced activation of cAMP-dependent PKA I and II. Rp-8-CPT-cAMPS preferentially selects site A of RI compares to site A of RII and site B of RII compares to site B of RI .
|
-
- HY-P1178
-
|
|
Trk Receptor
|
Neurological Disease
|
|
Cyclotraxin B, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects .
|
-
- HY-131760
-
|
2'-Amino-2'-deoxyadenosine-5'-triphosphate, 2′-Amino-2′-deoxy-ATP
|
Others
|
Metabolic Disease
|
|
2'-NH2-ATP (2'-Amino-2'-deoxyadenosine-5'-triphosphate), an adenosine derivative, is a weak competitive inhibitor of ATP, with a Ki of 2.3 mM. 2'-NH2-ATP can be used in nucleic acid labeling .
|
-
- HY-105692
-
|
|
PARP
|
Neurological Disease
|
|
DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. DR2313 exhibits neuroprotective effects on ischemic injuries in vitro and in vivo .
|
-
- HY-135780A
-
-
- HY-B2152
-
|
Hemicholinium dibromide
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Hemicholinium 3 is a competitive inhibitor of the high affinity choline transporter (HACU) with a Ki value of 25 nM. Hemicholinium 3, a neuromuscular blocking agent which inhibits the synthesis and the release of acetylcholine (ACh) . Hemicholinium 3 inhibits the Epibatidine-evoked contraction and [ 3H]acetylcholine release with IC50s of 897 nM and 693 nM, respectively .
|
-
- HY-115750
-
|
|
NO Synthase
|
Neurological Disease
|
|
Nω-allyl-L-arginine is a competitive and reversible inhibitor of bovine brain nitric oxide synthase (nNOS). Nω-allyl-L-arginine can inactivate nNOS in a time-dependent manner. Nω-allyl-L-arginine also is a substrate, producing L-arginine, acrolein, and H2O .
|
-
- HY-100743
-
|
2-Amino-4-phosphonobutyric acid
|
Others
|
Neurological Disease
Metabolic Disease
|
|
DL-AP4 (2-Amino-4-phosphonobutyric acid) is a glutamate antagonist. DL-AP4 behaves as a competitive inhibitor of glutamate binding with an apparent Kd of 66 μM. DL-AP4 can be used for the research of central nervous system and visual system .
|
-
- HY-W129596
-
|
|
Virus Protease
|
Infection
|
|
Policresulen is a potent inhibitor of DENV2 NS2B/NS3 protease (IC50 of 0.48 μg/mL). Policresulen inhibits DENV2 replication in BHK-21 cells with IC50 of 4.99 μg/mL. Policresulen acts as a competitive inhibitor of the protease, and slightly affects the protease stability .
|
-
- HY-50848
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
BW A868C, a hydantoin compound, is a BW245C structural analogue. BW A868C is a selective and potent competitive prostaglandin D2 (PGD2) antagonist. BW A868C has no effect on other prostaglandin receptors (IP, EP1, EP2, TP and FP) .
|
-
- HY-146333
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
TRAP-6-IN-1 (Compound 8) is a dual collagen and TRAP-6 inhibitor with IC50 values of 17.12 µM and 11.88 µM against collagen and TRAP-6, respectively. TRAP-6-IN-1 inhibits agonist-induced platelet aggregation in a non-competitive manner .
|
-
- HY-147707
-
|
|
Cannabinoid Receptor
|
Others
|
|
Hexyl resorcinol derivative 29 has been proved to be a CB2 selective competitive antagonist / reverse agonist with good potency. Olivanol and 5- (2-methyloctane-2-yl) resorcinol derivatives 23 and 24 showed significant antinociceptive activity. Compound 24 was shown to activate cannabinoid and TRPV1 receptors.
|
-
- HY-124953
-
|
|
MAP3K
Apoptosis
|
Cancer
|
|
7,3',4'-Trihydroxyisoflavone, a major metabolite of Daidzein, is an ATP-competitive inhibitor of Cot (Tpl2/MAP3K8) and MKK4. 7,3',4'-Trihydroxyisoflavone has anticancer, anti-angiogenic, chemoprotective, and free radical scavenging activities .
|
-
- HY-B0876A
-
|
4-Methylpyrazole hydrochloride
|
Cytochrome P450
|
Metabolic Disease
|
|
Fomepizole (4-Methylpyrazole) hydrochloride is a potent and orally active cytochrome P450 (CYP2E1) inhibitor. Fomepizole hydrochloride is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole hydrochloride blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole hydrochloride has the potential for an antidote for ethylene glycol or methanol poisoning .
|
-
- HY-150555
-
|
|
Potassium Channel
|
Others
|
|
P-CAB agent 1 (compound B19) is a highly potent potassium-competitive acid blocker agent with an IC50 value of 60.50 nM for H +/K +-ATPase. P-CAB agent 1 has acceptable oral absorption in rats. P-CAB agent 1 can be used for researching acid-related disorders (ARDs) .
|
-
- HY-150061
-
|
|
PI3K
mTOR
|
Cancer
|
|
NVP-BBD130 is a potent, stable, ATP-competitive and orally active dual PI3K and mTOR inhibitor . NVP-BBD130 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-122936
-
|
|
Histone Methyltransferase
Keap1-Nrf2
Sirtuin
|
Cardiovascular Disease
Cancer
|
|
Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research .
|
-
- HY-112346
-
|
|
CDK
Apoptosis
|
Cancer
|
|
RGB-286147 is a selective and ATP-competitive CDK and CDK-related kinases (CRK) inhibitor with IC50 values ranging from 9-839 nM. RGB-286147 shows less active against other non-CDK/CRK kinases. RGB-286147 induces cell apoptosis, and exhibits anti-tumor activity .
|
-
- HY-110005
-
|
|
PKA
Phosphodiesterase (PDE)
|
Neurological Disease
Metabolic Disease
|
|
Sp-cAMPS triethylamine, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS triethylamine is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS triethylamine binds the PDE10 GAF domain with an EC50 of 40 μM .
|
-
- HY-117359
-
|
|
PAI-1
Apoptosis
|
Cancer
|
|
UCD38B hydrochloride is a cell permeant, competitive enzymatic uPA inhibitor with an IC50 value of 7 μM. UCD38B hydrochloride targets intracellular uPA causing mistrafficking of uPA into perinuclear mitochondria, reducing the mitochondrial membrane potential, and followed by the release of apoptotic inducible factor (AIF). UCD38B hydrochloride induces apoptosis .
|
-
- HY-P99639
-
|
APL-501; CBT-501; GB-226
|
PD-1/PD-L1
|
Cancer
|
|
Geptanolimab (CBT-501) is a humanized IgG4k monoclonal antibody against programmed death-1 (PD-1). Siplizumab inhibits the binding of PD-L1/L2 to PD-1 through a competitive action. Siplizumab can be used in research of cancer .
|
-
- HY-108483
-
|
|
Neurokinin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
RP 67580 is a non-peptide antagonist of substance P (SP), competitively inhibits the binding of [3H]SP to neurokinin receptor 1 (NK1 receptor) in rat brain membranes with a Ki value of 4.16 nM. RP 67580 is a specific antagonist of NK1 receptors and can be used in the research of pain and neurogenic inflammation .
|
-
- HY-100834A
-
|
5,7-DCKA sodium
|
iGluR
|
Neurological Disease
|
|
5,7-Dichlorokynurenic acid (sodium) is the sodium form of 5,7-Dichlorokynurenic acid (HY-100834). 5,7-Dichlorokynurenic acid is a selective and competitive antagonist of the glycine site on the NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid, a derivative of kynurenic acid, reduces NMDA-induced neuron injury in rat cortical cell cultures .
|
-
- HY-163174
-
|
|
Others
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
|
|
II399 is a potent, selective NNMT bisubstrate inhibitor containing an unconventional SAM mimic, with a Ki of 5.9 nM. II399 exhibits an explicit pattern of competitive inhibition for NAM. II399 occupies both the substrate and cofactor binding pockets. II399 has the potential for the research of cancers, metabolic, cardiovascular, and neurodegenerative diseases .
|
-
- HY-134101
-
-
- HY-106103
-
|
MK-678; L-363586
|
Somatostatin Receptor
|
Neurological Disease
Metabolic Disease
|
|
Seglitide (MK-678) is a potent, orally active somatostatin receptor 2 (SSTR2) agonist, and also a competitive antagonist of SSTR14, SSTR25, and SSTR28. Seglitide has antihypertensive effects and can inhibit plasma glucagon and growth hormone. Seglitide can be used for research on diabetes .
|
-
- HY-106103A
-
|
MK 678 acetate; L 36358 acetate
|
Somatostatin Receptor
|
Neurological Disease
Metabolic Disease
|
|
Seglitide acetate (MK 678; L 36358 acetate) is a potent, orally active somatostatin receptor 2 (SSTR2) agonist, and also a competitive antagonist of SSTR14, SSTR25, and SSTR28. Seglitide acetate has antihypertensive effects and can inhibit plasma glucagon and growth hormone. Seglitide acetate can be used for research on diabetes .
|
-
- HY-121383R
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Labetalol (Standard) is the analytical standard of Labetalol. This product is intended for research and analytical applications. Labetalol (AH5158) is an orally active selective α1- and non-selective β-adrenergic receptors competitive antagonist. Labetalol, an anti-hypertensive agent, can be used for the research of cardiovascular disease, such as hypertension in pregnancy .
|
-
- HY-W685943
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Heptaminol is a fatty amine with pressor properties and a potential antihypotension agent. Heptaminol is also a competitive inhibitor of norepinephrine uptake and an inhibitor of nicotine-induced catecholamine release (IC50: 650 μM). Heptaminol does not inhibit norepinephrine release induced by 59 mM K + but rather inhibits high-affinity Na +-dependent norepinephrine uptake .
|
-
- HY-19010
-
|
SKF 94482
|
Histamine Receptor
|
Neurological Disease
|
|
BMY-25368 (SKF 94482) is a histamine H2 receptor antagonist that acts as a gastric acid secretion inhibitor. BMY-25368 competitively antagonizes gastric secretion stimulated by histamine and also antagonizes gastric secretion stimulated by Pentagastrin (HY-A0261), Bethanechol (HY-B0406), and food .
|
-
- HY-161913
-
|
|
Dopamine Transporter
|
Neurological Disease
|
|
AC-4-248 is an atypical non-competitive dopamine transporter (DAT) inhibitor and reduces the potency of cocaine to inhibit DAT. AC-4-248 is a non-selective inhibitor of SLC6 transporters with IC50 values for hDAT, hSERT, and hNET of 45.5 μM, 96.2 μM, and 250 μM, respectively .
|
-
- HY-10583R
-
|
|
ROCK
Organoid
|
Cancer
|
|
Y-27632 (dihydrochloride) (Standard) is the analytical standard of Y-27632 (dihydrochloride). Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor (ROCK-I Ki=220 nM; ROCK-II Ki=300 nM). Y-27632 dihydrochloride shows antiepileptic effects .
|
-
- HY-N0471AR
-
|
|
mAChR
|
Neurological Disease
|
|
L-Hyoscyamine (sulfate) (Standard) is the analytical standard of L-Hyoscyamine (sulfate). This product is intended for research and analytical applications. L-Hyoscyamine sulfate (Daturine sulfate), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine sulfate is a levo-isomer to Atropine (HY-B1205) .
|
-
- HY-P10630
-
|
|
Amyloid-β
|
Neurological Disease
|
|
Pep63 is a neuroprotective peptide (VFQVRARTVA). Pep63 has a neuroprotective effect on synaptic plasticity and memory. Pep63 can competitively bind with Aβ1-42 oligomers, and can block Aβ fiber formation. Pep63 can be used for Alzheimer’s disease (AD) research .
|
-
- HY-119097
-
|
|
mGluR
|
Neurological Disease
|
|
LY456066 is a selective non-competitive metabotropic glutamate receptors (mGluR1) antagonist with an IC50 value of 52.0 nM. LY456066 is effective in rodent models of anxiolysis and nociception. LY456066 reduces hyperalgesia and the amount of licking and flinching following formalin injection, which is promising for research of analgesics for chronic pain .
|
-
- HY-10163R
-
|
|
Thrombin
|
Cardiovascular Disease
Cancer
|
|
Dabigatran (Standard) is the analytical standard of Dabigatran. This product is intended for research and analytical applications. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM) .
|
-
- HY-15086
-
|
CGS 19755
|
iGluR
|
Neurological Disease
|
|
Selfotel (CGS 19755) is a selective and competitive antagonist at N-methyl-D-aspartate (NMDA)-preferring receptor. CGS 19755 inhibits the binding of [3H]-3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid to NMDA-type receptors with an IC50 of 50 nM .
|
-
- HY-168108
-
|
|
Fungal
|
Infection
|
|
Antifungal agent 115 (compound 8n) is a non-competitive chitin synthase (CHS) inhibitor with an IC50 of 93 μM. Antifungal agent 115 demonstrates good selectivity and broad-spectrum antifungal activity, exhibiting significant efficacy against drug-resistant fungi. Antifungal agent 115 can be utilized in fungi infection research .
|
-
- HY-100815
-
|
|
Others
|
Neurological Disease
|
|
(R)-AMPA is an inactive AMPA receptor ligand that inhibits the release of excitatory amino acids from neurons. (R)-AMPA is inactive in experiments that enhance the release of [3H]D-aspartate induced by electrical stimulation. (R)-AMPA is inhibited by competitive and noncompetitive AMPA receptor selective antagonists in response to AMPA and glutamate .
|
-
- HY-12059
-
AT7867
4 Publications Verification
|
Akt
PKA
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
AT7867 is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
|
-
- HY-12059A
-
|
|
Akt
PKA
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
|
-
- HY-B0290
-
-
- HY-13418A
-
|
Compound C; BML-275
|
Organoid
AMPK
TGF-β Receptor
Autophagy
|
Cancer
|
|
Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599) .
|
-
- HY-B0113S
-
|
H 16868-d3
|
Proton Pump
Bacterial
Autophagy
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole-d3 is deuterium labeled Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].
|
-
- HY-B1205
-
|
Tropine tropate; DL-Hyoscyamine
|
mAChR
Endogenous Metabolite
|
Cardiovascular Disease
Neurological Disease
|
|
Atropine (Tropine tropate) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine inhibits ACh-induced relaxations in human pulmonary veins. Atropine can be used for research of anti-myopia and bradycardia .
|
-
- HY-10406
-
|
SCIO-469
|
p38 MAPK
|
Cancer
|
|
Talmapimod (SCIO-469) is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs .
|
-
- HY-12481
-
|
|
PI3K
Autophagy
|
Cancer
|
|
SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity .
|
-
- HY-14166
-
|
L 663536
|
FLAP
Leukotriene Receptor
PPAR
Apoptosis
|
Cancer
|
|
MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis .
|
-
- HY-B0290A
-
|
ONO-1078 hemihydrate
|
Leukotriene Receptor
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Pranlukast hemihydrate is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [ 3H]LTE4, [ 3H]LTD4, and [ 3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
|
-
- HY-18955
-
|
|
MEK
Aurora Kinase
Apoptosis
|
Cancer
|
|
BI-847325 is an ATP competitive dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively. BI-847325 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-10228
-
|
AMG 706
|
c-Kit
VEGFR
|
Cancer
|
|
Motesanib (AMG 706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is appr 10-fold more selective for VEGFR than PDGFR and Ret.
|
-
- HY-15785
-
|
TAS-116
|
HSP
|
Cancer
|
|
Pimitespib (TAS-116) is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94 . Pimitespib demonstrates less ocular toxicity .
|
-
- HY-13302
-
|
|
VEGFR
FGFR
|
Cancer
|
|
CP-547632 is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy .
|
-
- HY-10195BS
-
|
|
Isotope-Labeled Compounds
PKC
|
Metabolic Disease
|
|
Ruboxistaurin-d6 (hydrochloride) is the deuterium labeled Ruboxistaurin hydrochloride. Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC50 of 5.9 nM[1][2].
|
-
- HY-112179
-
|
|
Others
|
Inflammation/Immunology
|
|
GSK180 is a selective, competitive, and potent inhibitor of kynurenine-3-monooxygenase (KMO), a key enzyme of tryptophan metabolism (IC50, ~6 nM), but shows negligible activity against other enzymes on the tryptophan pathway. GSK180 rapidly changes levels of kynurenine pathway metabolites, and acts as a useful tool to probe the therapeutic potential of KMO inhibition .
|
-
- HY-113468AS1
-
|
3-Methoxy-L-tyrosine-d3 hydrate; 3-O-Methyl-L-DOPA-d3 hydrate
|
Isotope-Labeled Compounds
Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
3-O-Methyldopa-d3 (hydrate) is the deuterium labeled 3-O-Methyldopa. 3-O-Methyldopa (3-Methoxy-L-tyrosine) is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine[1].
|
-
- HY-17395S
-
|
TDT 067-d3 hydrochloride
|
Isotope-Labeled Compounds
Fungal
Bacterial
Antibiotic
|
Infection
|
|
Terbinafine-d3 (hydrochloride) is the deuterium labeled Terbinafine hydrochloride. Terbinafine hydrochloride (TDT 067 hydrochloride) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM[1][2]. Terbinafine hydrochloride also antibacterial activity against certain Gram-positive and Gram-negative bacteria[3].
|
-
- HY-17395AS
-
|
TDT 067-d7
|
Isotope-Labeled Compounds
Fungal
Bacterial
Antibiotic
|
Infection
|
|
Terbinafine-d7 is the deuterium labeled Terbinafine. Terbinafine (TDT 067) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM[1][2]. Terbinafine also antibacterial activity against certain Gram-positive and Gram-negative bacteria[3].
|
-
- HY-10255AS
-
|
SU 11248-d10
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib-d10 is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
|
-
- HY-15816A
-
|
BVD-523 hydrochloride; VRT752271 hydrochloride
|
ERK
|
Cancer
|
|
Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib hydrochloride inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .
|
-
- HY-124817
-
Col003
5 Publications Verification
|
HSP
|
Inflammation/Immunology
|
|
Col003 is a selective and potent inhibitor of Hsp47 and competitively binds to the collagen binding site on Hsp47 (IC50=1.8 μM). Col003 discourages the interaction of Hsp47 with collagen and inhibits collagen secretion by destabilizing the collagen triple helix. Col003 can be used for the investigation of fibrosis
|
-
- HY-101523
-
|
|
CDK
|
Cancer
|
|
Cdc7-IN-1 (Compound 13) is a highly potent, selective and ATP competitive inhibitor of Cdc7 kinase, with an IC50 value of 0.6 nM at 1 mM ATP and with slow off-rate characteristics. Cdc7-IN-1 potently inhibits Cdc7 activity in cancer cells, and effectively induces cell death .
|
-
- HY-101075
-
|
|
Phosphatase
|
Others
|
|
L-690330 is a competitive inhibitor of inositol monophosphatase (IMPase) with Kis of 0.27 and 0.19 μM for recombinant human and bovine IMPase, 0.30 and 0.42 μM for human and bovine frontal cortex IMPase, respectively. L-690330 exhibits 10-fold more sensitive than mouse and rat IMPase .
|
-
- HY-128694
-
|
SR27417
|
Platelet-activating Factor Receptor (PAFR)
|
Cardiovascular Disease
|
|
Foropafant (SR27417) highly potent, competitive, selective and orally active antagonist of platelet-activating factor (PAF) receptor, with a Ki value of 57 pM for [ 3H]PAF binding, at least 5-fold lower than that of unlabeled PAF itself. Foropafant potently inhibits PAF-induced aggregation of rabbit and human platelets .
|
-
- HY-122866
-
|
|
Ras
|
Cancer
|
|
ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM .
|
-
- HY-16018A
-
|
ABT-348 hydrochloride
|
Aurora Kinase
PDGFR
VEGFR
|
Cancer
|
|
Ilorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS) .
|
-
- HY-13302B
-
|
|
VEGFR
FGFR
|
Cancer
|
|
CP-547632 hydrochloride is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 hydrochloride has antitumor efficacy .
|
-
- HY-14561A
-
|
RX 781094 hydrochloride
|
Adrenergic Receptor
Imidazoline Receptor
|
Neurological Disease
Endocrinology
|
|
Idazoxan hydrochloride (RX 781094 hydrochloride) is an α2-adrenoceptor antagonist and is also a imidazoline receptors (IRs) antagonist competitively antagonized the centrally induced hypotensive effect of imidazoline-like agents (IMs). Idazoxan hydrochloride also improves motor symptoms in Parkinson’s disease, L-DOPA-induced dyskinesias, and experimental Parkinsonism .
|
-
- HY-106301
-
|
L-364,718; MK-329
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .
|
-
- HY-103353
-
|
|
Cathepsin
Parasite
|
Infection
Cancer
|
|
SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G .
|
-
- HY-103442
-
|
DAPH
|
EGFR
Amyloid-β
|
Neurological Disease
Cancer
|
|
CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca 2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease .
|
-
- HY-133146
-
|
|
Phosphatase
Apoptosis
|
Inflammation/Immunology
|
|
DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase-σ (PTPσ) inhibitor with an IC50 of 1.43 μM. DJ001 displays no inhibitory activity against other phosphatases, with only modest inhibitory activity against Protein Phosphatase 5. DJ001 promotes promote hematopoietic stem cell regeneration .
|
-
- HY-103195
-
NKY80
1 Publications Verification
|
Adenylate Cyclase
|
Metabolic Disease
|
|
NKY80 is a potent, selective and non-competitive adenylyl cyclase (AC) type V isoform inhibitor with IC50s of 8.3 µM, 132 µM and 1.7 mM for type V, III and II, respectively. NKY80 is a non-nucleoside quinazolinone and regulates the AC catalytic activity in heart and lung tissues .
|
-
- HY-10406A
-
|
SCIO-469 hydrochloride
|
p38 MAPK
|
Cancer
|
|
Talmapimod (SCIO-469) hydrochloride is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod hydrochloride shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs .
|
-
- HY-15271
-
WYE-687
3 Publications Verification
|
mTOR
PI3K
|
Cancer
|
|
WYE-687 is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
|
-
- HY-N4042
-
|
|
PI3K
ERK
|
Inflammation/Immunology
Cancer
|
|
Hirsutenone is an active botanical diarylheptanoid present in Alnus species and exhibits many biological activities, including anti-inflammatory, anti-tumor promoting and anti-atopic dermatitis effects. Hirsutenone attenuates adipogenesis by binding directly to PI3K and ERK1 in a non-ATP competitive manner. Hirsutenone can be used for the study of obesity .
|
-
- HY-116852
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Thiocolchicine, a derivative modified in the C Ring of Colchicine (HY-16569) with enhanced biological properties. Thiocolchicine is a potent inhibitor of tubulin polymerization (IC50=2.5 μM) and competitively binds to tubulin with a Ki of 0.7 μM. Thiocolchicine induces cell apoptosis . Thiocolchicine can be used as an ADC cytotoxin in ADC technology.
|
-
- HY-P1297A
-
|
|
CRFR
|
Neurological Disease
|
|
CRF(6-33)(human) TFA is a CRF binding protein (CRF-BP) ligand inhibitor. CRF(6-33)(human) TFA competitively binds the CRF-BP but not the post-synaptic CRF receptors. CRF(6-33)(human) TFA has anti-obesity effect .
|
-
- HY-W010342
-
|
|
Others
|
Cancer
|
|
6-Aminonicotinamide, a potent antimetabolite of nicotinamide, is competitive NADP +-dependent enzyme glucose-6-phosphate dehydrogenase (G6PD) inhibitor (Ki=0.46 μM). 6-Aminonicotinamide resultis ATP depletion and synergizes with DNA-crosslinking chemotherapy agents, such as Cisplatin, in killing cancer cells .
|
-
- HY-101075A
-
|
|
Phosphatase
|
Others
|
|
L-690330 hydrate is a competitive inhibitor of inositol monophosphatase (IMPase) with Kis of 0.27 and 0.19 μM for recombinant human and bovine IMPase, 0.30 and 0.42 μM for human and bovine frontal cortex IMPase, respectively. L-690330 hydrate exhibits 10-fold more sensitive than mouse and rat IMPase .
|
-
- HY-16018
-
|
ABT-348
|
Aurora Kinase
VEGFR
PDGFR
|
Cancer
|
|
Ilorasertib (ABT-348) is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib also is a potent VEGF, PDGF inhibitor. Ilorasertib has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS) .
|
-
- HY-131350
-
|
|
Proteasome
Parasite
|
Infection
|
|
LXE408 is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 has an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. LXE408 has a low propensity to cross the blood brain barrier. LXE408 has the potential for visceral leishmaniasis (VL) research .
|
-
- HY-110347
-
|
|
Mps1
|
Cancer
|
|
Mps1-IN-1 dihydrochloride is a potent and ATP-competitive Mps1 kinase inhibitor with an IC50 of 367 nM. Mps1-IN-1 dihydrochloride inhibit Mps1 mitotic kinase activity and abrogates spindle assembly checkpoint (SAC) function. Mps1-IN-1 dihydrochloride decreases the viability of both cancer and ‘normal’ cells .
|
-
- HY-112081
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
BAY-707 is a substrate-competitive, highly potent and selective inhibitor of MTH1(NUDT1) with an IC50 of 2.3 nM. BAY-707 has a good pharmacokinetic (PK) profile to other MTH1 compounds and is well-tolerated in mice, but shows a clear lack of in vitro or in vivo anticancer efficacy .
|
-
- HY-109184
-
|
AMG 397
|
Bcl-2 Family
|
Cancer
|
|
Murizatoclax (AMG 397) is a potent, selective and orally active inhibitor of myeloid leukemia 1 (MCL-1) inhibitor, with a Ki of 15 pM. Murizatoclax competitive binds to the BH3-binding groove of MCL1 with pro-apoptotic BCL-2 family members. Murizatoclax can be used for the research of cancer .
|
-
- HY-114038
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
SB-747651A is an ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor with an IC50 of 11 nM. SB-747651A also inhibits PRK2, RSK1, p70S6K and ROCK-II. SB-747651A can be used for inflammation research .
|
-
- HY-139409A
-
|
|
Others
|
Metabolic Disease
|
|
2-Deoxy-D-glucose 6-phosphate disodium, a derivative of 2-Deoxy-D-glucose, is produced in mammalian cells by the action of hexokinase on 2-DG. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase .
|
-
- HY-139466
-
|
|
SHP2
PKC
|
Metabolic Disease
|
|
PF-03622905 is a potent and ATP-competitive PKC inhibitor with IC50s of 5.6 nM, 14.5 nM, 13 nM, 37.7 nM, and 74.1 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCθ, respectively. PF-03622905 shows high specificity for PKC over other protein kinases .
|
-
- HY-110313
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
SB-747651A dihydrochloride is an ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor with an IC50 of 11 nM. SB-747651A dihydrochloride also inhibits PRK2, RSK1, p70S6K and ROCK-II. SB-747651A dihydrochloride can be used for inflammation research .
|
-
- HY-131592
-
|
|
Apoptosis
Keap1-Nrf2
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Tricetin is a potent competitive inhibitor of the Keap1-Nrf2 Protein Protein Interaction (PPI). Tricetin protects against 6-OHDA-induced neurotoxicity in Parkinson's disease model by activating Nrf2/HO-1 signaling pathway and preventing mitochondria-dependent apoptosis pathway .
|
-
- HY-145702
-
|
|
MEK
ERK
|
Cancer
|
|
MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2 .
|
-
- HY-144354S
-
|
|
Isotope-Labeled Compounds
ASCT
|
Cancer
|
|
S-Benzyl-DL-cysteine-2,3,3-d3 is a deuterium labeled Benzylcysteine. Benzylcysteine is an ASCT2 inhibitor that binds to ASCT2 with an apparent Ki of 780 μM. Benzylcysteine inhibit ASCT2 function based on a competitive mechanism, indicating that Benzylcysteine binds to the substrate-binding site of ASCT2[1].
|
-
- HY-B0371S
-
|
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Metabolic Disease
Endocrinology
|
|
Terazosin-d8 is deuterium labeled Terazosin. Terazosin is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin works by relaxing blood vessels and the opening of the bladder. Terazosin has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment[1][2][3].
|
-
- HY-102065
-
|
|
Prostaglandin Receptor
|
Others
|
|
SC-19220 is a competitive prostaglandinn E2 receptor antagonist. SC-19220 increases the bladder capacity and reduced the voiding efficiency of micturition (elicited by slow transvesical filling) of urethane-anesthetized rats. SC-19220 can restores the balance in bone marrow granulocyte and monocyte production after burn sepsis .
|
-
- HY-N10403
-
|
4-Hydroxy-17β-estradiol
|
Drug Metabolite
Endogenous Metabolite
|
Cancer
|
|
4-Hydroxyestradiol (4-Hydroxy-17β-estradiol) is an endogenous metabolite of Estradiol (HY-B0141). 4-Hydroxyestradiol is carcinogenic and shows mutagenic activity in breast epithelial cells. 4-Hydroxyestradiol inhibits the binding of Estradiol to the estrogen receptor in a competitive manner, with a Ki of 0.48 nM .
|
-
- HY-112390B
-
|
|
Syk
5-HT Receptor
|
Inflammation/Immunology
|
|
Syk Inhibitor II dihydrochloride dihydrate is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride dihydrate inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride dihydrate shows less potent against other kinases and has anti-allergic effect .
|
-
- HY-150029
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
CB1/2 agonist 3 (compound 52), a potent non-selective cannabinoid ligand, is a CB1/CB2 (cannabinoid receptor) competitive agonist. CB1/2 agonist 3 acts on hCB1 and hCB2 with Ki values of 5.9 nM and 3.5 nM, respectively .
|
-
- HY-147298
-
|
CYC140
|
Polo-like Kinase (PLK)
|
Cancer
|
|
Plogosertib (CYC140) is a selective, potent, and orally active ATP-competitive PLK1 inhibitor (IC50: 3 nM). Plogosertib is an anti-cancer agent with anti-proliferative activity. Plogosertib can be used in the research of several tumors, including esophageal, gastric, leukemia, non–small cell lung cancer, ovarian, and squamous cell cancers .
|
-
- HY-150560
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-11 is a highly permeable competitive α-glucosidase inhibitor with the IC50 value of 0.56 μM. α-Glucosidase-IN-11 binds to Trp residues in α-glucosidase and regulates protein folding. α-Glucosidase-IN-11 can be used to regulate blood glucose levels .
|
-
- HY-33838
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
eIF4A3-IN-8 is a selective ATP-competitive eukaryotic initiation factor 4A3 (eIF4A3) inhibitor. eIF4A3-IN-8 can serve as a valuable chemical probe to elucidate the detailed function of eIF4A3 and EJC (exon junction complex) .
|
-
- HY-151248
-
|
|
HDAC
|
Neurological Disease
|
|
HDAC2-IN-1 (Compound 17) is a brain penetrant, orally active, competitive HDAC2 inhibitor with an IC50 of 0.5 μM . HDAC2-IN-1 also inhibits HDAC1 and HDAC8 with IC50s of 1.61 μM and 0.98 μM, respectively .
|
-
- HY-P99345
-
|
TSR-042
|
PD-1/PD-L1
|
Cancer
|
|
Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively .
|
-
- HY-136026
-
|
BLU-5937
|
P2X Receptor
|
Inflammation/Immunology
|
|
Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with an IC50 of 25 nM against hP2X3 homotrimeric. Camlipixant shows potent anti-tussive effect and no taste alteration. Camlipixant can be used for the research of unexplained, refractory chronic cough .
|
-
- HY-10163S2
-
|
BIBR 953-13C6; BIBR 953ZW-13C6
|
Thrombin
|
Cardiovascular Disease
|
|
Dabigatran- 13C6 is the 13C labeled Dabigatran[1]. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[2][3].
|
-
- HY-B1729S
-
|
|
Antibiotic
|
Infection
|
|
Phenoxyethanol-d2 is the deuterium labeled Phenoxyethanol[1]. Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al[2].
|
-
- HY-B1729S1
-
|
|
Bacterial
|
Infection
|
|
Phenoxyethanol-d4 is the deuterium labeled Phenoxyethanol[1]. Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al[2].
|
-
- HY-107727
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
BMS-193885 (L-Lactic acid) is a potent, selective, and brain-penetrant neuropeptide Y1 receptor antagonist. BMS-193885 has a Ki value of 3.3 nM for the neuropeptide Y1 receptor, competitively acts on the neuropeptide Y binding site, and can reduce food intake and body weight through central Y1 inhibition .
|
-
- HY-155137
-
|
|
Monoamine Oxidase
Reactive Oxygen Species
|
Neurological Disease
|
|
CHBO4 is a potent, reversible, competitive, and selective hMAO-B inhibitor with an IC50 value of 0.031 μM in CHBO subseries and an Ki value of 0.010 ± 0.005 μM. CHBO4 reduce cell damage by scavenging intracellular reactive oxygen species (ROS). CHBO4 can be used for Parkinson's Disease (PD) research .
|
-
- HY-14166A
-
|
L 663536 sodium salt
|
PPAR
Apoptosis
Leukotriene Receptor
FLAP
|
Cancer
|
|
MK-886 (L 663536) sodium salt is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 sodium salt is also a non-competitive PPARα antagonist and can induce apoptosis .
|
-
- HY-149716
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
MEY-003 is an Autotaxin(ATX) inhibitor with EC50s of 460 nM and 1.09 μM for hATX-β and hATX-ɣ (analysis with LPC18:1). MEY-003 behaves as a non-competitive inhibitor with K iof 432 nM. MEY-003 can be used for targeted ATX-related disease research .
|
-
- HY-19101
-
|
|
Kallikrein
|
Cardiovascular Disease
|
|
ONO-3307 is a protease inhibitor that competitively inhibits a variety of proteases including trypsin, thrombin, plasma kallikrein, plasmin, pancreatic kallikrein, and chymotrypsin. ONO-3307 alleviates endotoxin-induced experimental disseminated intravascular coagulation (DIC) in rats. ONO-3307 can be used in the study of thrombosis and protease-mediated diseases .
|
-
- HY-15901A
-
|
|
Pim
mTOR
|
Cancer
|
|
LGB321 monohydrochloride is a potent, selective, orally active and ATP competitive inhibitor of all three PIM kinases. LGB321 monohydrochloride inhibits proliferation, mTOR-C1 signaling and phosphorylation of BAD in a number of cell lines derived from diverse hematologic malignancies. LGB321 monohydrochloride can be used for the research of hematologic malignancies .
|
-
- HY-W728545
-
|
AH5158-d6 hydrochloride; Sch-15719W-d6
|
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
Labetalol-d6 hydrochloride (AH5158-d6 hydrochloride; Sch-15719W-d6) is a deuterium labeled Labetalol (HY-121383). Labetalol is an orally active α1- and β-adrenergic receptors competitive antagonist, which exhibits anti-hypertensive property .
|
-
- HY-137321
-
|
Estriol 3-β-D-Glucuronide sodium salt
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Estriol 3-glucuronide (Estriol 3-β-D-Glucuronide) sodium salt is a metabolite of Estriol. Estriol 3-glucuronide sodium salt competitively inhibits the hydrolysis of 4-methylumbelliferyl-β-D-glucuronide (4Mu-GlcU). Estriol 3-glucuronide sodium salt is a substrate for hydrolysis by Klotho-human IgG1 Fc protein (KLFc) .
|
-
- HY-B1729R
-
|
|
Oxidative Phosphorylation
Bacterial
|
Infection
|
|
Phenoxyethanol (Standard) is the analytical standard of Phenoxyethanol. This product is intended for research and analytical applications. Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al .
|
-
- HY-163433
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-57 (Compound 10c) is a competitive and orally active α-glucosidase inhibitor with an IC50 value of 0.180 μM and a Ki of 0.15 μM. α-Glucosidase-IN-57 can reduce fasting and overall blood glucose levels in mice, and can be used for anti-diabetes research .
|
-
- HY-N12761
-
|
|
Phosphatase
Glucosidase
|
Metabolic Disease
Inflammation/Immunology
|
|
Penpaxilloids A (Compound 1) is a non-competitive inhibitor of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 8.60 μM. Penpaxilloids A can be isolated from the fungus Penicillium sp. ZYX-Z-143. Penpaxilloids A is also an α-glucosidase (α-glucosidase) inhibitor with anti-inflammatory activity .
|
-
- HY-101355
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
CGP 20712 is a highly selective β1-adrenoceptor antagonist (Ki=0.3 nmol/L). CGP 20712’s primary mechanism of action is through competitively binding to β1-receptors, thereby blocking the positive chronotropic effects of adrenaline and noradrenaline .
|
-
- HY-10285R
-
|
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Saxagliptin (Standard) is the analytical standard of Saxagliptin. This product is intended for research and analytical applications. Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research .
|
-
- HY-14664AR
-
|
|
HMG-CoA Reductase (HMGCR)
Autophagy
Ferroptosis
|
Cardiovascular Disease
Cancer
|
|
Fluvastatin (sodium) (Standard) is the analytical standard of Fluvastatin (sodium). This product is intended for research and analytical applications. Fluvastatin sodium (XU 62320) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin sodium protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway .
|
-
- HY-17423R
-
|
|
HIV
Reverse Transcriptase
Telomerase
Apoptosis
|
Infection
Cancer
|
|
Abacavir (Standard) is the analytical standard of Abacavir. This product is intended for research and analytical applications. Abacavir is an orally active and competitive nucleoside reverse transcriptase inhibitor. Abacavir can inhibits the replication of HIV. Abacavir shows anticancer activity in prostate cancer cell lines. Abacavir can trespass the blood-brain-barrier and suppresses telomerase activity .
|
-
- HY-P10392
-
|
|
β-catenin
Wnt
|
Cancer
|
|
aStAx-35R, a stapled peptide, antagonizes nuclear form of β-catenin and inhibits Wnt signaling. aStAx-35R inhibits competitively the binding of β-catenin to TCF4. aStAx-35R selectively induces growth inhibition of Wnt-dependent cancer cells .
|
-
- HY-106684
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Ridazolol is a β-adrenergic receptor (βAR) antagonist. Ridazolol exhibits a high degree of selectivity for β-1 adrenergic receptor (β1AR) and possesses moderate intrinsic sympathomimetic activity (ISA). Ridazolol can competitively antagonize the relaxation effects induced by isoproterenol. Ridazolol is utilized in the research of cardiovascular diseases .
|
-
- HY-107001
-
|
(S)-DPC 961; DMP 961
|
HIV
Reverse Transcriptase
|
Infection
|
|
DPC 961 (DMP 961) is a non-nucleoside reverse transcriptase inhibitor (NNRTI). DPC 961 is a potent and specific inhibitor of HIV-1 reverse transcriptase, which inhibits the activity of HIV-1 reverse transcriptase in a non-competitive manner, thereby preventing viral replication. DPC 961 can be used for research on AIDS .
|
-
- HY-134245
-
|
Tubercidin 5'-phosphate; 7-Deaza-AMP
|
Others
|
Others
|
|
7-Deazaadenosine 5'-phosphate (Tubercidin 5'-phosphate; 7-Deaza-AMP) is a potential substrate or competitive inhibitor of enzymes that interact with 5′-adenylic acid monophosphate. As a nucleotide derivative, 7-Deazaadenosine 5'-phosphate can regulate cellular functions by affecting intracellular signaling pathways, especially in signaling involving AMP .
|
-
- HY-B0549AR
-
|
|
Phosphodiesterase (PDE)
Calcium Channel
mAChR
|
Neurological Disease
|
|
Flavoxate (hydrochloride) (Standard) is the analytical standard of Flavoxate (hydrochloride). This product is intended for research and analytical applications. Flavoxate hydrochloride is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate hydrochloride is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate hydrochloride shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate hydrochloride can be used for the research of overactive bladder (OAB) and lower urinary tract infections .
|
-
- HY-B0231R
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Enalaprilat (dihydrate) (Standard) is the analytical standard of Enalaprilat (dihydrate). This product is intended for research and analytical applications. Enalaprilat dihydrate (MK-422), the active metabolite of the oral proagent Enalapril, is a potent, competitive and long-acting angiotensin-converting enzyme (ACE) inhibitor, with an IC50 of 1.94 nM. Enalaprilat dihydrate can be used for the research of hypertension .
|
-
- HY-W684904
-
|
|
TGF-β Receptor
|
Cancer
|
|
LY550410 is a small-molecule ATP-competitive inhibitor against type I TGF-β receptor kinase, which contains heteroaryl rings for potent binding to the kinase-domain active site. LY550410 modulates TGF-β signalling, thereby regulates gene expression and ultimately cell growth. LY550410 is promising for research of cancers .
|
-
- HY-162884
-
|
|
Others
|
Infection
|
|
EcGUS-IN-1 (Compound E-9) is a non-competitive β-glucuronidase inhibitor, with an IC50 of 2.68 μM and a Ki value of 1.64 μM. EcGUS-IN-1 can improve gastrointestinal adverse events (GIAE) caused by Escherichia coli infection by inhibiting E. coli β-glucuronidase activity .
|
-
- HY-106684A
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Ridazolol hydrochloride is a β-adrenergic receptor (βAR) antagonist. Ridazolol hydrochloride exhibits a high degree of selectivity for β-1 adrenergic receptor (β1AR) and possesses moderate intrinsic sympathomimetic activity (ISA). Ridazolol hydrochloride can competitively antagonize the relaxation effects induced by isoproterenol. Ridazolol hydrochloride is utilized in the research of cardiovascular diseases .
|
-
- HY-13299
-
MK-8033
2 Publications Verification
|
c-Met/HGFR
|
Cancer
|
|
MK-8033 is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
|
-
- HY-13011
-
|
CH5424802; RO5424802; RG7853
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
|
-
- HY-13203
-
|
TAE226
|
FAK
Pyk2
IGF-1R
Insulin Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
NVP-TAE 226 (TAE226) is a potent and ATP-competitive dual FAK and IGF-1R inhibitor with IC50s of 5.5 nM and 140 nM, respectively. NVP-TAE 226 (TAE226) also effectively inhibits Pyk2 and insulin receptor (InsR) with IC50s of 3.5 nM and 44 nM, respectively .
|
-
- HY-13007
-
|
PF-03758309
|
PAK
Apoptosis
|
Cancer
|
|
PF-3758309 (PF-03758309) is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .
|
-
- HY-13024
-
|
DCC-2036
|
Bcr-Abl
FLT3
Src
Apoptosis
|
Cancer
|
|
Rebastinib (DCC-2036) is an orally active, non-ATP-competitive Bcr-Abl inhibitor for Abl1 WT and Abl1 T315I with IC50s of 0.8 nM and 4 nM, respectively. Rebastinib also inhibits SRC, KDR, FLT3, and Tie-2, and has low activity to seen towards c-Kit.
|
-
- HY-15656
-
|
LDK378
|
Anaplastic lymphoma kinase (ALK)
Insulin Receptor
IGF-1R
|
Endocrinology
Cancer
|
|
Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency .
|
-
- HY-15656A
-
|
LDK378 dihydrochloride
|
Anaplastic lymphoma kinase (ALK)
Insulin Receptor
IGF-1R
|
Endocrinology
Cancer
|
|
Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride (LDK378 dihydrochloride) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride (LDK378 dihydrochloride) shows great antitumor potency .
|
-
- HY-13299A
-
|
|
c-Met/HGFR
|
Cancer
|
|
MK-8033 hydrochloride is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 hydrochloride can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
|
-
- HY-B0236
-
|
EACA; Epsilon-Amino-n-caproic Acid; 6-Aminohexanoic acid
|
Others
|
Metabolic Disease
Cancer
|
|
6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders .
|
-
- HY-12333
-
|
G-749
|
FLT3
Apoptosis
|
Cancer
|
|
Denfivontinib (G-749) is a potent, oral active and ATP competitive FLT3 inhibitor, with IC50s of 0.4 nM and 0.6 nM for FLT3 wild type and FLT3-D835Y, respectively. Denfivontinib can be used for the research of agent resistance for acute myeloid leukemia (AML) .
|
-
- HY-12344
-
UNC2025
4 Publications Verification
|
FLT3
|
Cancer
|
|
UNC2025 is a potent, ATP-competitive and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 exhibits an excellent PK properties, and can be used for the investigation of acute leukemia .
|
-
- HY-15959
-
|
Volitinib; HMPL-504; AZD-6094
|
c-Met/HGFR
|
Cancer
|
|
Savolitinib (AZD-6094) is a potent, highly selective, and orally bioavailable c-Met inhibitor with IC50 s of 5 nM and 3 nM for c-Met and p-Met, respectively. Savolitinib (AZD-6094) selectively binds to and inhibits the activation of c-Met in an ATP-competitive manner, and disrupts c-Met signal transduction pathways. Antineoplastic activity .
|
-
- HY-12344A
-
|
|
FLT3
|
Cancer
|
|
UNC2025 hydrochloride is a potent, ATP-competitive, and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 hydrochloride is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 hydrochloride exhibits an excellent PK properties, and can be used for the investigation of acute leukemia .
|
-
- HY-117743S
-
|
|
Isotope-Labeled Compounds
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Eprosartan-d3 is the deuterium labeled Eprosartan. Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively [1].
|
-
- HY-10873S
-
|
|
Isotope-Labeled Compounds
Drug Metabolite
|
Cancer
|
|
N-Desethyl Sunitinib-d5 is the deuterium labeled N-Desethyl Sunitinib. N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively[1].
|
-
- HY-10255AS1
-
|
|
Isotope-Labeled Compounds
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib-d4 is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
|
-
- HY-15237
-
|
SL0101
|
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
SL 0101-1 (SL0101), a kaempferol glycoside, isolated from the tropical plant F. refracta, is a cell-permeable, selective, reversible, ATP-competitive p90 Ribosomal S6 Kinase (RSK) inhibitor, with an IC50 of 89 nM . SL 0101-1 (SL0101) is a selective RSK1/2 inhibitor, with a Ki of 1 μM .
|
-
- HY-112683
-
|
|
ASCT
|
Cancer
|
|
V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells .
|
-
- HY-120619
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
Endocrinology
|
|
BMS-193885 is a potent, selective, competitive, and brain penetrant neuropeptide Y1 receptor antagonist with a Ki of 3.3 nM, and has an IC50 of 5.9 nM for hY1, which displays > 100, > 160, > 160 and > 160-fold selectivity over α1, hY2, hY4 and hY5 receptors, respectively .
|
-
- HY-114641A
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
BIIL-260 hydrochloride is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. BIIL-260 hydrochloride interacts with the LTB4 receptor in a saturable, reversible, and competitive manner, has high affinity to the LTB4 receptor on isolated human neutrophil cell membranes with Ki values of 1.7 nM .
|
-
- HY-15271A
-
|
|
mTOR
PI3K
|
Cancer
|
|
WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM . WYE-687 dihydrochloride concurrently inhibits activation of mTORC1 and mTORC2 . WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively .
|
-
- HY-112683A
-
|
|
ASCT
|
Cancer
|
|
V-9302 hydrochloride is a competitive antagonist of transmembrane glutamine flux. V-9302 hydrochloride selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells .
|
-
- HY-70053A
-
|
|
mAChR
|
Neurological Disease
Metabolic Disease
|
|
Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine L-mandelate is used for the overactive bladder (OAB) .
|
-
- HY-136174
-
|
|
PARP
|
Cancer
|
|
RBN-2397 is a potent, accross species and orally active NAD + competitive inhibitor of PARP7 (IC50<3 nM). RBN-2397 selectively binds to PARP7 (Kd=0.001 μM) and restores IFN signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors .
|
-
- HY-15491
-
|
|
COX
Apoptosis
|
Cancer
|
|
AG-024322 is a potent ATP-competitive pan-CDK inhibitor against cell cycle kinases CDK1, CDK2, and CDK4 with Ki values in the 1-3 nM range . AG-024322 displays broad-spectrum anti-tumor activity and clear target modulation in vivo. AG-024322 induces cell apoptosis .
|
-
- HY-131081
-
|
|
DNA/RNA Synthesis
ADC Cytotoxin
|
Cancer
|
|
γ-Amanitin an ADC cytotoxin and isolated from the mushroom. γ-Amanitin inhibits RNA polymerase II and disrupts synthesis of mRNA. γ-Amanitin shows similar effects to α-Amanitin and β-Amanitin. γ-Amanitin competitively binds to monoclonal antibody (mAb), with an IC50 of 163.1 ng/mL .
|
-
- HY-15847
-
HS38
1 Publications Verification
|
DAPK
|
Cardiovascular Disease
|
|
HS38 is a potent, selective, and ATP-competitive inhibitor of death-associated protein kinase 1 (DAPK1) and zipper-interacting protein kinase (ZIPK, also called DAPK3), with Kds of 300 nM and 280 nM, respectively. HS38 is also a PIM3 inhibitor with an IC50 of 200 nM. HS38 can be used for the research of smooth muscle related disorders .
|
-
- HY-133596
-
|
|
Potassium Channel
GABA Receptor
|
Neurological Disease
|
|
12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca 2+-activated K + (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive GABAA antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca 2+ and stimulates transmitter release .
|
-
- HY-P1178A
-
|
|
Trk Receptor
|
Neurological Disease
|
|
Cyclotraxin B TFA, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B TFA non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B TFA can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects .
|
-
- HY-13007B
-
|
PF-03758309 dihydrochloride
|
PAK
Apoptosis
|
Cancer
|
|
PF-3758309 (PF-03758309) dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .
|
-
- HY-13302C
-
|
|
VEGFR
FGFR
|
Cancer
|
|
CP-547632 TFA is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 TFA is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 TFA has antitumor efficacy .
|
-
- HY-103353A
-
|
|
Cathepsin
Parasite
|
Infection
Cancer
|
|
SID 26681509 quarterhydrate is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 quarterhydrate inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 quarterhydrate shows no inhibitory activity against cathepsin G .
|
-
- HY-10517A
-
|
(Z)-SU6668; (Z)-TSU-68
|
VEGFR
PDGFR
FGFR
|
Cancer
|
|
(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC50s of 2.1, 0.008, and 1.2 µM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors .
|
-
- HY-14892
-
|
LC15-0444
|
Dipeptidyl Peptidase
|
Metabolic Disease
Cancer
|
|
Gemigliptin (LC15-0444 ) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin exhibits potent anti-glycation properties. Gemigliptin can be used for the research of advanced glycation end products (AGE)-related diabetic complications .
|
-
- HY-120051
-
|
S44819; Egis-13529
|
GABA Receptor
|
Neurological Disease
|
|
Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy .
|
-
- HY-13007A
-
|
PF-03758309 hydrochloride
|
PAK
Apoptosis
|
Cancer
|
|
PF-3758309 (PF-03758309) hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .
|
-
- HY-19432
-
|
|
iGluR
|
Neurological Disease
|
|
UBP-282 is a potent, selective and competitive AMPA and kainate receptor antagonist. UBP-282 inhibits the fast component of the dorsal root-evoked ventral root potential (fDR-VRP) with an IC50 value of 10.3 μM. UBP-282 antagonizes kainate-induced depolarisations of dorsal roots with a pA2 value of 4.96 .
|
-
- HY-131800
-
|
|
Others
|
Metabolic Disease
|
|
3'-Deoxy-3'-amino-ATP, an ATP analogue, is a potent and competitive inhibitor of ATP, with a Ki of 2.3 μM. 3'-Deoxy-3'-amino-ATP can be used to synthesis of 3′-Amino-3′-deoxy transfer RNA by incorporation into the 3' terminus of tRNA-C-C .
|
-
- HY-117596
-
UNC569
1 Publications Verification
|
TAM Receptor
|
Cancer
|
|
UNC569 is a potent, reversible, ATP-competitive and orally active Mer kinase inhibitor with an IC50 of 2.9 nM and a Ki of 4.3 nM. UNC569 also inhibits Axl and Tyro3 with IC50s of 37 nM and 48 nM, respectively. UNC569 can be used for acute lymphoblastic leukemia (ALL) and atypical teratoid/rhabdoid tumors research
|
-
- HY-P3229
-
SN52
2 Publications Verification
|
NF-κB
|
Cancer
|
|
SN52 is a potent, competitive, and cell-permeable inhibitor of NF-κB2. SN52 is a variant of the SN50 peptide and inhibits the nuclear translocation of p52-RelB heterodimers. SN52 has a strong radiosensitization effect on prostate cancer cells. SN52 can be used for cancer research .
|
-
- HY-101119
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
GLL398, an orally active selective estrogen receptor degrader (SERD), competitively binds to the estrogen receptor with an IC50 value of 1.14 nM. GLL398 exhibits a strong dose-dependent binding profile for the ER with a Y537S point mutation (IC50= 29.5 nM). GLL398 blocks tumor growth in xenograft breast cancer models .
|
-
- HY-101037S1
-
|
N-Methylglycine-d3; Sarcosin-d3
|
Isotope-Labeled Compounds
Endogenous Metabolite
GlyT
|
Cancer
|
|
Sarcosine-d3 is the deuterium labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia[1][2].
|
-
- HY-I0096S
-
-
- HY-144778
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
Apoptosis
Bcl-2 Family
|
Cancer
|
|
IDO1/TDO-IN-1 (30) is a potent dual IDO1 (uncompetitive, Ki of 0.23 μM) and TDO (competitive, Ki of 0.73 μM) inhibitor. IDO1/TDO-IN-1 (30) significantly promotes cell apoptosis through the potential mitochondria-mediated Bcl-2/Bax pathway .
|
-
- HY-10163S3
-
|
BIBR 953-13C,d3; BIBR 953ZW-13C,d3
|
Isotope-Labeled Compounds
Thrombin
|
Cardiovascular Disease
|
|
Dabigatran- 13C,d3 is the 13C- and deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
|
-
- HY-A0166S
-
|
MK0791-15N,d3
|
Bacterial
Antibiotic
|
Infection
|
|
Cilastatin- 15N,d3 is a 15N-labeled and deuterium labeled Cilastatin. Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct[1][2][3].
|
-
- HY-B0236A
-
|
EACA hydrochloride; Epsilon-Amino-n-caproic Acid hydrochloride; 6-Aminohexanoic acid hydrochloride
|
Others
|
Metabolic Disease
Cancer
|
|
6-Aminocaproic acid hydrochloride, a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders .
|
-
- HY-13204B
-
|
KL 373 lactate
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) lactate is an orally active non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors. Biperiden (KL 373) lactate inhibits acetylcholine and enhances dopamine signaling in the central nervous system. Biperiden (KL 373) lactate has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-P0205A
-
|
[Sar1,Ala8] Angiotensin II acetate hydrate
|
Angiotensin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Saralasin ([Sar1,Ala8] Angiotensin II) acetate hydrate is an octapeptide analog of angiotensin II. Saralasin acetate hydrate is a competitive angiotensin II receptor antagonist with a Ki value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin acetate hydrate can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension .
|
-
- HY-P0205
-
|
[Sar1,Ala8] Angiotensin II
|
Angiotensin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Saralasin ([Sar1,Ala8] Angiotensin II) is an octapeptide analog of angiotensin II. Saralasin is a competitive angiotensin II receptor antagonist with a Ki value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension .
|
-
- HY-148327
-
|
|
Adenosine Kinase
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
AK-IN-1 (compound 4072-2732) is an adenosine kinase (AK) inhibitor that is competitive for adenosine (Ado) but not for ATP. AK-IN-1 inhibits 86%, 87% and 89% of AK activity at concentrations of 2, 4 and 10 µM, respectively. AK-IN-1 has good potential for research in many disease areas, including ischaemia, inflammation and seizures .
|
-
- HY-148318
-
|
|
Casein Kinase
|
Cancer
|
|
CK2α-IN-1 (compound 2) is a selective CK2α inhibitor (IC50=7.0 µM; Ki=1.6 µM) that exhibits a non-ATP-competitive mode of action. CK2α-IN-1 exhibits good potential for anticancer studies .
|
-
- HY-13418G
-
|
Compound C dihydrochloride; BML-275 dihydrochloride
|
AMPK
|
Neurological Disease
Cancer
|
|
Dorsomorphin dihydrochloride (GMP) is the GMP level of Dorsomorphin dihydrochloride (HY-13418). GMP guidelines are used to produce Dorsomorphin dihydrochloride (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. Dorsomorphin dihydrochloride (GMP) is a potent, selective and ATP-competitive AMPK inhibitor. Dorsomorphin dihydrochloride (GMP) can be used for the research of induced differentiation of pluripotent stem cells (PSCs) .
|
-
- HY-153089
-
|
|
GSK-3
Mitophagy
|
Neurological Disease
|
|
GSK3-IN-3 is a mitophagy inducer, inducing Parkin-dependent mitophagy. GSK3-IN-3 is also a GSK-3 inhibitor with an IC50 value of 3.01 μM. GSK3-IN-3 is non-ATP nor substrate competitive and is neuroprotective against 6-OHDA .
|
-
- HY-B0192S
-
|
SL 77499-d7
|
Adrenergic Receptor
|
Endocrinology
|
|
Alfuzosin-d7 is the deuterium labeled Alfuzosin[1]. Alfuzosin (SL 77499-10) is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin can be used in study of benign prostatic hyperplasia (BPH)[2][3].
|
-
- HY-149248
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
NF-κB-IN-8 competitively antagonizes LPS binding to MD-2. NF-κB-IN-8 reduces the expression of inflammatory factors by binding to MD-2. NF-κB-IN-8 also inhibits ALP activity. NF-κB-IN-8 can be used for the research of inflammation such as acute lung injury (ALI) .
|
-
- HY-155098
-
|
|
SHP2
|
Cancer
|
|
CNBCA is a potent, selective, competitive SHP2 enzyme inhibitor, with the IC50 of 0.87 μM. CNBCA binds to full-length SHP2 and inhibits enzyme activity. CNBCA inhibits pAkt and pERK1/2, and the cell growth of BT474 and MDA-MB468 cells. CNBCA can be used for breast cancer study .
|
-
- HY-W484263
-
|
|
NO Synthase
|
Neurological Disease
|
|
hnNOS-IN-3 (compound 39) is a selective nNOS inhibitor, with a Ki of 0.32 μM. The nNOS binding of hnNOS-IN-3 is competitive with L-arginine. The selectivity of hnNOS-IN-3 for nNOS versus iNOS (Ki=37 μM) and eNOS (Ki=9.4 μM) is 115-fold and 29-fold, respectively .
|
-
- HY-P5038
-
|
c(GRGDSP)
|
Integrin
|
Cancer
|
|
Cyclo(Gly-Arg-Gly-Asp-Ser-Pro) (c(GRGDSP)) is an RGD-containing inhibitory peptide. Cyclo(Gly-Arg-Gly-Asp-Ser-Pro) is a synthetic α5β1 integrin ligand that competitively inhibits the binding of invasin (Inv) to α5β1 integrin expressed on Caco-2 cells .
|
-
- HY-W758126
-
|
|
Isotope-Labeled Compounds
|
Others
|
|
(R)-Brivanib alaninate-d4 is the deuterium-labeled Brivanib (alaninate) (HY-10336). Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ .
|
-
- HY-N0368R
-
|
|
iGluR
Apoptosis
Endogenous Metabolite
|
Cardiovascular Disease
Cancer
|
|
Linalool (Standard) is the analytical standard of Linalool. This product is intended for research and analytical applications. Linalool is natural monoterpene in essential olis of coriander, acts as a competitive antagonist of Nmethyl d-aspartate (NMDA) receptor, with anti-tumor, anti-cardiotoxicity activity .Linalool is a PPARα ligand that reduces plasma TG levels and rewires the hepatic transcriptome and plasma metabolome .
|
-
- HY-14721
-
|
EMD-1214063
|
c-Met/HGFR
Autophagy
|
Cancer
|
|
Tepotinib (EMD-1214063) is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib inhibits c-Met phosphorylation and induces autophagy. Tepotinib has antitumor effects .
|
-
- HY-13204R
-
|
KL 373 hydrochloride (Standard)
|
mAChR
|
Neurological Disease
|
|
Biperiden (hydrochloride) (Standard) is the analytical standard of Biperiden (hydrochloride). This product is intended for research and analytical applications. Biperiden (KL 373) hydrochloride is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden hydrochloride has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-158037
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-55 (Compound 8g) is an orally active and competitive alpha-glucosidase inhibitor, with IC50 and Ki values of 12.1 and 9.66 µM, respectively. α-Glucosidase-IN-55 can be used for the research into type 2 diabetes mellitus (T2DM) to improve blood sugar control and metabolic health .
|
-
- HY-158245
-
|
|
Acetolactate Synthase (ALS)
|
Others
|
|
Herbicide safener-2 (Compound III-7) is a herbicide safener with the same pharmacokinetic profile as the safener mefenpyr-diethyl (HY-136376). Herbicide safener-2 competitively binds to the acetolactate synthase (ALS) active site with mesosulfuron-methyl (HY-126987). Herbicide safener-2 protects crops against herbicide injury .
|
-
- HY-14721A
-
|
EMD-1214063 hydrochloride
|
c-Met/HGFR
Autophagy
|
Cancer
|
|
Tepotinib (EMD-1214063) hydrochloride is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib hydrochloride inhibits c-Met phosphorylation and induces autophagy. Tepotinib hydrochloride has antitumor effects .
|
-
- HY-107339R
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Neurological Disease
Metabolic Disease
|
|
Deserpidine (Standard) is the analytical standard of Deserpidine. This product is intended for research and analytical applications. Deserpidine (Harmonyl) is an alkaloid isolated from the root of Rauwolfia canescens related to Reserpine. Deserpidine is used as an antihypertensive agent and a tranquilizer. Deserpidine is a competitive angiotensin converting enzyme (ACE) inhibitor. Deserpidine also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex .
|
-
- HY-13204AR
-
|
|
mAChR
|
Neurological Disease
|
|
Biperiden (Standard) is the analytical standard of Biperiden. This product is intended for research and analytical applications. Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-10873S2
-
|
SU-12662-d5 hydrochloride
|
Isotope-Labeled Compounds
Drug Metabolite
|
Cancer
|
|
N-Desethyl Sunitinib-d5 (hydrochloride) is a deuterated labeled N-Desethyl Sunitinib . N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively .
|
-
- HY-122564
-
|
|
Dynamin
|
Others
|
|
Pyrimidyn 7 is an inhibitor of dynamin I/II with IC50 values of 1.1 μM and 1.8 μM, respectively. Pyrimidyn 7 competitively inhibits the interactions between GTP and phospholipids with dynamin I. Additionally, Pyrimidyn 7 reversibly inhibits clathrin-mediated endocytosis (CME) of transferrin and epidermal growth factor (EGF) in various non-neuronal cell linecell [1.
|
-
- HY-114641
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
BIIL-260 is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. BIIL-260 interacts with the LTB4 receptor in a saturable, reversible, and competitive manner, has high affinity to the LTB4 receptor on isolated human neutrophil cell membranes with the Ki value of 1.7 nM .
|
-
- HY-14518R
-
|
|
Antifolate
|
Inflammation/Immunology
Cancer
|
|
Aminopterin (Standard) is the analytical standard of Aminopterin. This product is intended for research and analytical applications. Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia .
|
-
- HY-B0192AR
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
Alfuzosin (hydrochloride) (Standard) is the analytical standard of Alfuzosin (hydrochloride). This product is intended for research and analytical applications. Alfuzosin (SL 77499-10) hydrochloride is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin hydrochloride relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin hydrochloride can be used in study of benign prostatic hyperplasia (BPH) .
|
-
- HY-159625
-
|
Ro 91-4714
|
PIKfyve
|
Cancer
|
|
WX8 (Ro 91-4714) is an ATP-competitive PIKFYVE inhibitor, with Kd values of 0.9 nM and 340 nM for PIKFYVE and PIP4K2C, respectively. WX8 (Ro 91-4714) inhibits lysosomal fission without effecting homotypic lysosomal fusion. WX8 (Ro 91-4714) is used in the research of autophagy-dependent cancer .
|
-
- HY-10572A
-
|
(R)-DMP 266; (R)-EFV; (R)-L-743726
|
Reverse Transcriptase
|
Infection
|
|
(R)-Efavirenz ((R)-DMP 266) is a non-nucleoside reverse transcriptase inhibitor that acts by non-competitive inhibition of the viral enzyme. (R)-Efavirenz can be metabolized by CYP2B6 to 8-hydroxyefavirenz in a highly stereoselective manner. (R)-Efavirenz is promising to be a useful probe for the CYP2B6 active site and catalytic mechanisms .
|
-
- HY-U00079A
-
|
FK-176
|
mAChR
|
Neurological Disease
|
|
Vamicamide (FK-176) is an orally active competitive mAChR antagonist that inhibits contractions induced by cholinergic nerve stimulation by preventing mAChR agonists from binding to mAChR. Vamicamide exhibits a good anti-bladder spasm effect, with a pA2 value of 6.82 in bladder tissue. Vamicamide can be used in research within the field of neurological diseases .
|
-
- HY-117583A
-
|
|
HDAC
Histone Methyltransferase
|
Neurological Disease
|
|
BG47 is a prototypical histone deacetylases HDAC1 and HDAC2 selective, optoepigenetic probe. BG47 can bind to and competitively inhibits the deacetylase activity of HDAC targets upon a light-induced trans-to-cis isomerization, and increases Histone Methyltransferase H3K9 acetylation. BG47 can be used for neurological disease research .
|
-
- HY-B0371FR
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
|
|
Terazosin (hydrochloride) (Standard) is the analytical standard of Terazosin (hydrochloride). This product is intended for research and analytical applications. Terazosin hydrochloride is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin hydrochloride works by relaxing blood vessels and the opening of the bladder. Terazosin hydrochloride has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment .
|
-
- HY-116138
-
|
|
Others
|
Others
|
|
RG-14467 is an epidermal growth factor receptor tyrosine kinase inhibitor with activity that inhibits enzyme activity. RG-14467 has similar inhibition kinetics to Lavendustin-A, with a dissociation constant of 3.4μM for the initial rapidly formed complex and an overall dissociation constant estimated to be less than or equal to 30nM, and is a partially competitive inhibitor for ATP.
|
-
- HY-W050122
-
|
|
Others
|
Neurological Disease
|
|
S-(+)-GABOB is an endogenous ligand with antiepileptic activity. S-(+)-GABOB is a metabolite of GABA and may function as a neurotransmitter. S-(+)-GABOB behaves as a full agonist when bound to the ρ(1) wild-type receptor. S-(+)-GABOB acts as a competitive antagonist in the ρ(1) T244S mutant receptor .
|
-
- HY-10181
-
|
BMS-354825
|
Bcr-Abl
Src
Autophagy
Apoptosis
|
Cancer
|
|
Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
|
-
- HY-10254
-
|
PD0325901; PD325901
|
MEK
Autophagy
Apoptosis
|
Cancer
|
|
Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC50 of 0.33 nM. Mirdametinib exhibits a Ki app of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts .
|
-
- HY-15478
-
WZ811
3 Publications Verification
|
CXCR
|
Endocrinology
Cancer
|
|
WZ811 is an orally active, highly potent competitive antagonist of CXCR4. WZ811 efficiently inhibits CXCR4/SDF-1 (or CXCL12)-mediated modulation of cAMP levels (EC50=1.2 nM) and SDF-1 induced Matrigel invasion in cells (EC50=5.2 nM) .
|
-
- HY-10510
-
|
|
Ribosomal S6 Kinase (RSK)
Autophagy
|
Cancer
|
|
BI-D1870 is an ATP-competitive, cell permeable and brain penetrated inhibitor of RSK isoforms, with IC50s of 31 nM/24 nM/18 nM/15 nM for RSK1/RSK2/RSK3/RSK4, respectively .
|
-
- HY-13912
-
|
|
Wnt
Porcupine
Casein Kinase
|
Cancer
|
|
IWP-2 is an inhibitor of Wnt processing and secretion with an IC50 of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC50 of 40 nM for the gatekeeper mutant M82FCK1δ .
|
-
- HY-10181A
-
|
BMS-354825 hydrochloride
|
Bcr-Abl
Src
Autophagy
Apoptosis
|
Cancer
|
|
Dasatinib (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib hydrochloride also induces apoptosis and autophagy.
|
-
- HY-14552
-
|
SB 223412
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Talnetant (SB 223412) is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant can be used in schizophrenia-related studies .
|
-
- HY-14552A
-
|
SB 223412 hydrochloride; SB 223412-A
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Talnetant (SB 223412) hydrochloride is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant hydrochloride is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant hydrochloride can be used in schizophrenia-related studies .
|
-
- HY-B0379A
-
|
|
nAChR
|
Neurological Disease
|
|
Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 μM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has anticonvulsant effects .
|
-
- HY-B0394
-
|
Tropine tropate sulfate monohydrate; DL-Hyoscyamine sulfate monohydrate
|
mAChR
|
Cardiovascular Disease
Neurological Disease
|
|
Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .
|
-
- HY-B1126
-
|
|
iGluR
|
Neurological Disease
|
|
Orphenadrine hydrochloride is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine hydrochloride relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine hydrochloride is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases .
|
-
- HY-B1205A
-
|
Tropine tropate sulfate; DL-Hyoscyamine sulfate; Sulfatropinol
|
mAChR
|
Cardiovascular Disease
Neurological Disease
|
|
Atropine (Tropine tropate) sulfate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate can be used for research of anti-myopia and bradycardia .
|
-
- HY-103392S
-
|
|
Isotope-Labeled Compounds
Cytochrome P450
|
Neurological Disease
|
|
Stiripentol-d9 is the deuterium labeled Stiripentol. Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediatated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59±0.07 and 0.516±0.065 μM and IC50 of 1.58 and 3.29 μM, respectively[1][2].
|
-
- HY-135390
-
|
Ro 64-1056
|
Drug Metabolite
|
Cardiovascular Disease
|
|
Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver . Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively. Bosentan can be used in treatment of pulmonary arterial hypertension .
|
-
- HY-16231
-
|
|
Apoptosis
|
Cancer
|
|
GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors .
|
-
- HY-116000
-
|
Gumarontinib; SCC244
|
c-Met/HGFR
|
Cancer
|
|
Glumetinib (SCC244) is a highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC50 of 0.42 nM. Glumetinib has greater than 2400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, TyrO3. Antitumor activity .
|
-
- HY-12783
-
|
|
GABA Receptor
|
Neurological Disease
|
|
SCH 50911 hydrochloride, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor with IC50 of 1.1 μM. SCH 50911 hydrochloride antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated 3H overflow with an IC50 of 3 μM.
|
-
- HY-122614
-
S29434
2 Publications Verification
NMDPEF
|
Autophagy
|
Neurological Disease
|
|
S29434 (NMDPEF) is a potent, competitive, selective and cell-permeable inhibitor of quinone reductase 2 (QR2), with IC50s ranging from 5 to 16 nM for human QR2 at different organizational levels, and has good selectivity for QR2 over QR1. S29434 induces autophagy and inhibits QR2-mediated ROS production .
|
-
- HY-107794
-
|
Disodium clodronate tetrahydrate
|
Others
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Clodronate disodium tetrahydrate (Disodium clodronate tetrahydrate) is first-generation bisphosphonate, with anti-osteoporotic, anti-inflammatory and analgesic effects. Clodronate disodium tetrahydrate is a selective, potent, reversible and Cl - competitive vesicular nucleotide transporter (VNUT) inhibitor, with an IC50 of 15.6 nM. Clodronate disodium tetrahydrate inhibits vesicular ATP release from neurons and reduces chronic neuropathic and inflammatory pain .
|
-
- HY-18263A
-
|
SB-656933
|
CXCR
Interleukin Related
|
Inflammation/Immunology
|
|
Elubrixin (SB-656933) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation .
|
-
- HY-P0205B
-
|
[Sar1,Ala8] Angiotensin II TFA
|
Angiotensin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Saralasin ([Sar1,Ala8] Angiotensin II) TFA is an octapeptide analog of angiotensin II. Saralasin TFA is a competitive angiotensin II receptor antagonist with a Ki value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin TFA can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension .
|
-
- HY-D0939
-
|
Chicago Sky Blue 6B
|
Amyloid-β
NF-κB
|
Inflammation/Immunology
|
|
Direct Blue 1 (Chicago Sky Blue 6B) is a complex dye for background autofluorescence in immunofluorescence histochemistry. Direct Blue 1 is a potent and competitive VGLUT inhibitor. Direct Blue 1 can inhibit the Aβ-binding small molecule PrP ligand. Direct Blue 1 has anti-inflammatory activity .
|
-
- HY-P2426
-
|
|
Thyroid Hormone Receptor
|
Metabolic Disease
|
|
(D-Trp12,Tyr34)-pTH (7-34) amide (bovine) is a potent and competitive antagonist of parathyroid hormone (PTH), with a Ki of 69 nM in bovine renal cortical membrane. (D-Trp12,Tyr34)-pTH (7-34) amide (bovine) can be used for growth and development regulation .
|
-
- HY-18263C
-
|
SB-656933 tosylate
|
CXCR
Interleukin Related
|
Inflammation/Immunology
|
|
Elubrixin tosylate (SB-656933 tosylate) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin tosylate inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin tosylate has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation .
|
-
- HY-118567
-
|
BMOV
|
SHP2
Phosphatase
|
Metabolic Disease
|
|
Bis(maltolato)oxovanadium(IV) (BMOV) is a potent, reversible, competitive and orally active pan-PTP (protein tyrosine phosphatases) inhibitor. Bis(maltolato)oxovanadium(IV) inhibits HCPTPA, PTP1B, HPTPβ and SHP2 with IC50s of 126 nM, 109 nM, 26 nM and 201 nM, respectively. Bis(maltolato)oxovanadium(IV) is a potent insulin sensitizer .
|
-
- HY-10181B
-
|
BMS-354825 monohydrate
|
Bcr-Abl
Src
Autophagy
Apoptosis
|
Cancer
|
|
Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib monohydrate also induces apoptosis and autophagy.
|
-
- HY-108490
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
VPC 23019, an aryl amide-containing Sphingosine 1-phosphate (S1P) analog, is a competitive antagonist at the S1P1 and S1P3 receptors (pKi= 7.86 and 5.93, respectively) and an agonist at the S1P4 and S1P5 receptors (pEC50= 6.58 and 7.07, respectively) .
|
-
- HY-19539
-
|
|
Ras
|
Cancer
|
|
NSC-658497 is an effective inhibitor of Ras-GEF, SOS1. NSC-658497 binds to SOS1, competitively suppresses SOS1-Ras interaction, and dose-dependently inhibits SOS1 GEF activity. NSC-658497 showed dose-dependent efficacy in inhibiting Ras, downstream signaling activities, and associated cell proliferation .
|
-
- HY-12542
-
|
F 368
|
Calcium Channel
Autophagy
|
Neurological Disease
Inflammation/Immunology
|
|
Dantrolene is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene is a ryanodine receptor (RyR) antagonist and Ca2+ signaling stabilizer. Dantrolene is a direct-acting skeletal muscle relaxant. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome .
|
-
- HY-101037S
-
|
N-Methylglycine-15N; Sarcosin-15N
|
Endogenous Metabolite
GlyT
|
Cancer
|
|
Sarcosine- 15N is the 15N-labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia[1][2].
|
-
- HY-N10096
-
|
|
Parasite
|
Infection
|
|
Epoxyazadiradione is a limonoid purified from neem (Azadirachta indica) fruits. Epoxyazadiradione inhibits the tautomerase activity of MIF of both human (huMIF) and malaria parasites (Plasmodium falciparum (PfMIF) and Plasmodium yoelii (PyMIF)) non-competitively in a reversible fashion (Ki, 2.11-5.23 μM). Epoxyazadiradione has the potential against proinflammatory reactions induced by MIF of both malaria parasites and human .
|
-
- HY-B0985A
-
|
|
TRP Channel
|
Neurological Disease
|
|
Phenazopyridine is a competitive SARM1 inhibitor, with IC50 145 μM. Phenazopyridine is a TRPM8 antagonist. Phenazopyridine has a local anesthetic/analgesic effect. Phenazopyridine is used to relieve painful symptoms of conditions such as cystitis and urethritis. Phenazopyridine can promote neuronal differentiation and can also be used in the study of traumatic brain injury, peripheral neuropathy and neurodegenerative diseases .
|
-
- HY-33549
-
|
|
Others
|
Neurological Disease
Cancer
|
|
α-Methyl-p-tyrosine is a competitive inhibitor of tyrosine hydroxylase, which converts tyrosine into DOPA. α-Methyl-p-tyrosine is also an orally active inhibitor of catecholamine synthesis, inhibiting the hydroxylation of tyrosine into DOPA. α-Methyl-p-tyrosine can be used in research related to epilepsy, glaucoma, cancer, and other related diseases .
|
-
- HY-17504B
-
|
ZD 4522 Sodium; X-Plended Sodium; Crestor Sodium
|
HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
Bacterial
|
Cardiovascular Disease
Metabolic Disease
|
|
Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-150028
-
|
|
Cannabinoid Receptor
|
Inflammation/Immunology
|
|
CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand, with Ki values of 3.5 and 1.2 nM, respectively. CB1/2 agonist 2 can behave as a full CB1 agonist and CB2 competitive inverse agonist. CB1/2 agonist 2 shows antinociceptive activity .
|
-
- HY-B1205B
-
|
Tropine tropate hydrobromide; DL-Hyoscyamine hydrobromide
|
mAChR
|
Cardiovascular Disease
Neurological Disease
|
|
Atropine (Tropine tropate) hydrobromide is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine hydrobromide inhibits ACh-induced relaxations in human pulmonary veins. Atropine hydrobromide can be used for research of anti-myopia and bradycardia .
|
-
- HY-13206A
-
|
|
mGluR
|
Neurological Disease
|
|
MTEP is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP shows antidepressant and anxiolytic-like effects. MTEP can be used for Parkinson's disease research . MTEP is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-50672
-
|
|
Kinesin
Apoptosis
Lipoxygenase
|
Cancer
|
|
MK-0731 is a selective, non-competitive and allosteric kinesin spindle protein (KSP) inhibitor with an IC50 of 2.2 nM and a pKa of 7.6. MK-0731 is >20,000 fold selectivity against other kinesins. MK-0731 induces mitotic arrest and induces apoptosis in tumors. MK-0731 provides significant antitumor efficacy .
|
-
- HY-148595
-
|
|
Cytochrome P450
|
Cancer
|
|
Antitumor agent-88 exhibits potent antimitotic activity and arrests cell in the G2/M phase. Antitumor agent-88 disrupts the microtubule and the cytoskeleton in CYP1A1-expressing breast cancer cells. Antitumor agent-88 is also a competitive inhibitor of CYP1A1 (Ki: 1.4 μM) .
|
-
- HY-N0368S
-
|
|
Apoptosis
iGluR
Endogenous Metabolite
|
Cancer
|
|
Linalool-d3 is the deuterium labeled Linalool[1]. Linalool is natural monoterpene in essential olis of coriander, acts as a competitive antagonist of Nmethyl d-aspartate (NMDA) receptor, with anti-tumor, anti-cardiotoxicity activity[2].Linalool is a PPARα ligand that reduces plasma TG levels and rewires the hepatic transcriptome and plasma metabolome[3].
|
-
- HY-13100
-
|
|
Proton Pump
|
Metabolic Disease
|
|
PF 03716556 is a potent, selective, competitive and reversible acid pump (H +,K +-ATPase) antagonist with pIC50s of 6.026, 6.038 and 6.009 for porcine, canine, and human recombinant gastric H +,K +-ATPase, respectively. PF 03716556 is inactive against other receptors, ion channels, and enzymes. PF 03716556 has the potential for gastroesophageal reflux disease research .
|
-
- HY-P5010
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
(D-Arg8)-Inotocin is a potent, selective and competitive antagonist of vasopressin receptor (V1aR), with a Ki of 1.3 nM. (D-Arg8)-Inotocin shows more than 3000-fold selectivity for the human V1aR over the other three subtypes, OTR, V1bR and V2R .
|
-
- HY-149887
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
H3B-968 is a potent inhibitor of Werner syndrome protein (WRN) (IC50=~10 nM)，which acts function as helicase，ATPase，and exonuclease. WRN exhibits synthetic lethal activity in cancer research. However，H3B-968 inhibits WRN helicase activity，competitively with ATP .
|
-
- HY-155102
-
|
|
PROTACs
Glutaminase
|
Cancer
|
|
PROTAC TG2 degrader-2 (compound 7) is a selective, competitive degrader targeting Transglutaminase 2 (TG2), with Kd > 100 μM. PROTAC TG2 degrader-2 inhibits the cell migration and decreases the level of TG2 in ovarian cancer cells. PROTAC TG2 degrader-2 can be used for ovarian cancer study .
|
-
- HY-155240
-
|
|
Tyrosinase
|
Cancer
|
|
Tyrosinase-IN-13 (compound 3c), a derivative of Flurbiprofen (HY-10582), is a potent, non-competitive tyrosinase inhibitor (IC50=68 μM; Ki=36.3 μM). Tyrosinase-IN-13 is cytotoxic against hepatocellular carcinoma (HepG2), colorectal cancer (HT-29), and melanoma (B16F10) .
|
-
- HY-P3248
-
|
Myelin basic protein (85-99) antagonist
|
Biochemical Assay Reagents
|
Inflammation/Immunology
|
|
J5 peptide is an MBP inhibitor that competitively inhibits the binding of MBP85-99 to HLA-DR2. J5 peptide alleviates PLP139-151/MBP85-99-induced experimental autoimmune encephalomyelitis (EAE) in mice. J5 peptide can be used in research on inflammatory and immune diseases .
|
-
- HY-P1173
-
|
Myristoylated L 803; GSK-3β Inhibitor XIII
|
GSK-3
Amyloid-β
|
Neurological Disease
|
|
L803-mts (Myristoylated L 803) is a selective and substrate-competitive GSK-3 peptide inhibitor (IC50: 40 μM). L803-mts also reduces Aβ deposits and ameliorates cognitive deficits in 5XFAD mice. L803-mts shows antidepressive effect in the forced swimming test .
|
-
- HY-18263
-
|
SB-656933 hydrochloride
|
CXCR
Interleukin Related
|
Inflammation/Immunology
|
|
Elubrixin (SB-656933) hydrochloride is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin hydrochloride inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin hydrochloride has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation .
|
-
- HY-N7150
-
|
5,7-Dihydroxy-3',4',5'-trimethoxyflavone
|
Xanthine Oxidase
|
Metabolic Disease
|
|
Tricetin 3',4',5'-trimethyl ether (5,7-Dihydroxy-3',4',5'-trimethoxyflavone) is a flavone glucoside, that can be isolated the flowers of Chrysanthemum sinensea. Tricetin 3',4',5'-trimethyl ether displays xanthine oxidase competitive-type inhibitory activity, with an IC50 of 0.51 μM and a Ki of 0.37 μM .
|
-
- HY-10917S
-
|
|
Isotope-Labeled Compounds
c-Fms
|
Inflammation/Immunology
Cancer
|
|
GW2580-d6 is the deuterium labeled GW2580. GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling .
|
-
- HY-17623D
-
|
CJ-12420 Benzoate; RQ-00000004 Benzoate
|
Proton Pump
|
Metabolic Disease
|
|
Tegoprazan Benzoate is the benzoate form of Tegoprazan (HY-17623). Tegoprazan (CJ-12420), a potassium-competitive acid blocker, is a potent, oral active and highly selective inhibitor of gastric H +/K +-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H +/K +-ATPases in vitro .
|
-
- HY-15834AR
-
|
SKF-108566J (Standard)
|
Angiotensin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Eprosartan (mesylate) (Standard) is the analytical standard of Eprosartan (mesylate). This product is intended for research and analytical applications. Eprosartan mesylate (SKF-108566J) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan mesylate binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
|
-
- HY-N12688
-
|
|
Glucosidase
Amylases
|
Metabolic Disease
|
|
2,3-Dihydrocalodenin B (Compound 6) is a compound that can be isolated from Knema globularia. 2,3-Dihydrocalodenin B is a potent and non-competitive inhibitor against α-glucosidase and α-amylase, with IC50 values of 1.1 and 2.6 μM, respectively. 2,3-Dihydrocalodenin B can be used for the research of diabetes .
|
-
- HY-10255AR
-
|
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib (Standard) is the analytical standard of Sunitinib. This product is intended for research and analytical applications. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
|
-
- HY-10450R
-
|
|
SGLT
|
Metabolic Disease
Cancer
|
|
Dapagliflozin (Standard) is the analytical standard of Dapagliflozin. This product is intended for research and analytical applications. Dapagliflozin (BMS-512148), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin induces HIF1 expression and attenuates renal IR injury .
|
-
- HY-110140
-
|
|
CaMK
|
Cardiovascular Disease
Neurological Disease
|
|
(E)-KN-93 phosphate is an inhibitor for Ca 2+/calmodulin-dependent protein kinase II (CaMK II) with IC50 of 9 μM and 3 μM, for CaMKIIδ monomer and CaMKIIδ dodecamer. (E)-KN-93 phosphate binds competitively with Ca 2+/CaM, and disrupts their interaction with CaMK II, and thus inhibits the CaMK II activation .
|
-
- HY-111214
-
-
- HY-101258
-
|
|
Parasite
|
Infection
|
|
Cardol triene is a phenol found in cashew nut shell liquid that competitively and irreversibly inhibits mushroom tyrosinase (IC50=22.5 μM). It is schistosomicidal, killing 25, 75, and 100% of S. mansoni worms after 24 hours when used at concentrations of 50, 100, or 200 μM, respectively. It has been used as a starting material for the synthesis of bis-benzoxazines.
|
-
- HY-P10392B
-
|
|
β-catenin
Wnt
|
Cancer
|
|
aStAx-35R TFA, a stapled peptide, antagonizes nuclear form of β-catenin and inhibits Wnt signaling. aStAx-35R TFA inhibits competitively the binding of β-catenin to TCF4. aStAx-35R TFA selectively induces growth inhibition of Wnt-dependent cancer cells .
|
-
- HY-162738
-
|
|
Cytochrome P450
|
Cancer
|
|
JMV6944 is a PXR agonist. JMV6944 competitively inhibits hPXR ligand-binding domain (LBD) binding to PXR with an IC50 of 680nM. JMV6944 induces CYP3A4 mRNA expression in freshly isolated human primary human hepatocyte cultures. JMV6944 can be used for the synthesis of PROTAC PXR degrader JMV7048 (HY-162704) .
|
-
- HY-17000R
-
|
|
Vasopressin Receptor
Autophagy
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Tolvaptan (Standard) is the analytical standard of Tolvaptan. This product is intended for research and analytical applications. Tolvaptan is a selective, competitive and orally active vasopressin receptor 2 (V2R) antagonist with an IC50 of 1.28 μM for the inhibition of arginine vasopressin (AVP)-induced platelet aggregation. Tolvaptan induces cell apoposis and affects cell cycle. Tolvaptan can be used for the research of hyponatremia .
|
-
- HY-B0292AR
-
|
|
nAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Atracurium (besylate) (Standard) is the analytical standard of Atracurium (besylate). This product is intended for research and analytical applications. Atracurium (BW-33A) besylate is a potent, competitive and non-depolarizing neuromuscular blocking agent. Atracurium besylate also is an AChR receptor antagonist. Atracurium besylate induces bronchoconstriction and neuromuscular blockade. Atracurium besylate promotes astroglial differentiation .
|
-
- HY-W015332R
-
|
|
Drug Metabolite
|
Others
|
|
Captopril EP Impurity D (Standard) is the analytical standard of Captopril EP Impurity D. This product is intended for research and analytical applications. Captopril EP Impurity D is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) .
|
-
- HY-B0873R
-
|
|
Cytochrome P450
ROS Kinase
|
Others
|
|
Uniconazole (Standard) is the analytical standard of Uniconazole. This product is intended for research and analytical applications. Uniconazole, a plant growth retardant, is a potent inhibitor of abscisic acid (ABA) catabolism with an IC50 of 68 nM against ABA 8’-hydroxylase. Uniconazole is a potent competitive inhibitor of CYP707A3 activity with a Ki of 8 nM. Uniconazole evidently inhibits gibberellin biosynthesis, and brassinosteroid biosynthesis is also inhibited to some extent .
|
-
- HY-Y0258A
-
|
|
Bacterial
Sodium Channel
|
Neurological Disease
|
|
Benzocaine (hydrochloride) is an orally active local agent that can suppress or relieve pain, that acts on voltage-gated Na + channels at a common receptor, with an IC50 value of 0.8 mM at +30 mV. Additionally, Benzocaine (hydrochloride) non-competitively inhibits Ca-ATPase binding with Ca 2+, with an IC50 of 47.1 mM. Benzocaine (hydrochloride) can be used in research within the field of neuromuscular regulation .
|
-
- HY-10275
-
|
AR-H067637
|
Thrombin
|
Cardiovascular Disease
|
|
Atecegatran (AR-H067637) is an orally active competitive thrombin inhibitor with a Ki of 2-4 nM. AR-H067637 inhibits platelet activation and aggregation by blocking thrombin binding to fibrin and thrombomodulin. Atecegatran demonstrates significant anticoagulant effects in various plasma coagulation assays, with an IC50 ranging from 93 to 220 nM. Atecegatran can be used in research related to thromboembolic disorders .
|
-
- HY-101037R
-
|
|
Endogenous Metabolite
GlyT
|
Cancer
|
|
Sarcosine (Standard) is the analytical standard of Sarcosine. This product is intended for research and analytical applications. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia .
|
-
- HY-137768R
-
|
|
Drug Metabolite
|
Others
|
|
Captopril EP Impurity B (Standard) is the analytical standard of Captopril EP Impurity B. This product is intended for research and analytical applications. Captopril EP Impurity B is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) .
|
-
- HY-137769R
-
|
|
Drug Metabolite
|
Others
|
|
Captopril EP Impurity C (Standard) is the analytical standard of Captopril EP Impurity C. This product is intended for research and analytical applications. Captopril EP Impurity C is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) .
|
-
- HY-137772R
-
|
|
Drug Metabolite
|
Others
|
|
Captopril EP Impurity E (Standard) is the analytical standard of Captopril EP Impurity E. This product is intended for research and analytical applications. Captopril EP Impurity E is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) .
|
-
- HY-168112
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-127 is an ATP-competitive EGFR inhibitor with IC50s of 136.3 nM and 161. 2 nM for EGFR del19 and EGFR del19/T790M/C797S, respectively. EGFR-IN-127 has the potential for the study of non-small-cell lung cancer (NSCLC) .
|
-
- HY-50683
-
|
|
c-Met/HGFR
|
Metabolic Disease
Cancer
|
|
JNJ-38877605 is an orally active ATP-competitive inhibitor of c-Met with an IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases . JNJ-38877605 inhibits c-Met phosphorylation and regulates lipid accumulation. JNJ-38877605 can be used for tumor and metabolic disease reseach .
|
-
- HY-12137
-
|
BI 6727
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
Volasertib (BI 6727) is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib induces mitotic arrest and apoptosis. Volasertib, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models .
|
-
- HY-13241
-
|
LY2228820 dimesylate
|
p38 MAPK
Autophagy
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.
|
-
- HY-15469
-
|
|
P2X Receptor
|
Neurological Disease
|
|
GW791343 dihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease .
|
-
- HY-17387
-
|
Huperzine A
|
Cholinesterase (ChE)
Apoptosis
iGluR
|
Neurological Disease
|
|
(-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease .
|
-
- HY-12037A
-
|
ON-01910
|
Polo-like Kinase (PLK)
PI3K
Apoptosis
|
Cancer
|
|
Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM .
|
-
- HY-13635A
-
|
MK-906 acetate
|
5 alpha Reductase
|
Cancer
|
|
Finasteride (MK-906) acetate is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride acetate has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride acetate can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia .
|
-
- HY-B0091
-
|
CD271
|
RAR/RXR
Autophagy
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity .
|
-
- HY-B0091A
-
|
CD 271 sodium salt
|
RAR/RXR
Autophagy
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Adapalene (CD271) sodium salt, a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene sodium salt is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene sodium salt also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene sodium salt exhibits anti-tumor activity .
|
-
- HY-B0113
-
|
H 16868
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-15816
-
|
BVD-523; VRT752271
|
ERK
|
Cancer
|
|
Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .
|
-
- HY-18010
-
|
|
Btk
BCRP
|
Inflammation/Immunology
|
|
PCI 29732 is a potent, orally active, reversible BTK inhibitor with Ki app values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2 .
|
-
- HY-12354
-
|
|
MMP
|
Cancer
|
|
SB-3CT is a potent and competitive matrix metalloproteinase MMP-2 and MMP-9 inhibitor with Ki values of 13.9 and 600 nM, respectively. SB-3CT has high selectivity for gelatinases. SB-3CT shows blood-brain barrier permeability and has neuroprotective effects and anticancer activity .
|
-
- HY-13588
-
|
SCE-129 sodium
|
Bacterial
Antibiotic
|
Infection
|
|
Cefsulodin (SCE-129) sodium is a third generation β lactam antibiotic and member of the cephems subgroup of antibiotics. Cefsulodin sodium inhibits cell wall synthesis by competitively inhibiting penicillin binding protein (PBP) cross-linking and transpeptidation of peptidogly. Cefsulodin sodium is a potent tyrosine phosphatase inhibitor against mPTPB, a virulent phosphatase from Mycobacterium tuberculosis, with an IC50 value of 16 μM .
|
-
- HY-13011A
-
|
CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
|
-
- HY-131043
-
|
|
PAK
|
Cancer
|
|
NVS-PAK1-C is a potent, ATP-competitive and specific allosteric PAK1 inhibitor probe with IC50 values of 5 nM and 6 nM for dephosphorylated PAK1 and phosphorylated PAK1, respectively. NVS-PAK1-C is also against dephosphorylated PAK2 (IC50=270 nM) and phosphorylated PAK2 (IC50=720 nM) .
|
-
- HY-W008364
-
|
|
Cytochrome P450
Cannabinoid Receptor
|
Neurological Disease
|
|
Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2 . Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively .
|
-
- HY-117273
-
|
|
Raf
Autophagy
|
Cancer
|
|
AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits wild type BRAF, V600E mutant BRAF and wild type CRAF, with IC50s of 79 nM, 38 nM and 68 nM, respectively. AZ304 also has significant effect on other kinases, such as p38 (IC50, 6 nM), CSF1R (IC50, 35 nM). Anti-tumor activity .
|
-
- HY-12783A
-
|
|
GABA Receptor
|
Neurological Disease
|
|
SCH 50911, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor with IC50 of 1.1 μM. SCH 50911 antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated 3H overflow with an IC50 of 3 μM .
|
-
- HY-128729
-
|
|
Others
|
Cancer
|
|
DNA2 inhibitor C5 is a potent, competitive and specific inhibitor of DNA2 nuclease activity with an IC50 of 20 μM. DNA2 inhibitor C5 inhibits nuclease, DNA dependent ATPase, helicase, and DNA binding activities of DNA2. DNA2 inhibitor C5 is a promising lead compound to develop sensitizers for cancer chemotherapeutics that cause replication stress .
|
-
- HY-W008344
-
|
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
2-Chloroadenosine, a stable adenosine analogue, protects against long term development of ischaemic cell loss in the rat hippocampus. 2-Chloroadenosine is an apparent competitive inhibitor of uridine influx (apparent Ki=33 μM) and high-affinity nitrobenzylthioinosine binding (apparent Ki=0.18 mM). 2-Chloroadenosine is a transported permeant for the nucleoside transporter in human erythrocytes .
|
-
- HY-N0063
-
|
|
SARS-CoV
HBV
|
Infection
Metabolic Disease
Cancer
|
|
Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a reversible and non-competitive 3CL pro inhibitor and inhibits SARS-CoV-2 replication in vitro. Punicalagin is an anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects. Punicalagin has the potential for the research of COVID-19 .
|
-
- HY-101300
-
|
LD 3098 hydrochloride
|
Adenosine Receptor
|
Neurological Disease
|
|
Cirazoline hydrochloride (LD 3098 hydrochloride) is a potent competitive full?α1A-adrenergic receptor (α1A-AR) agonist (Ki=120 nM) and only a partial agonist at α1B-AR (Ki= 960 nM) and α1D-AR (Ki=660 nM) .
|
-
- HY-130608
-
|
|
EGFR
|
Cancer
|
|
Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively .
|
-
- HY-15470
-
|
|
P2X Receptor
|
Neurological Disease
|
|
GW791343 trihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 trihydrochloride can enhance ATP rhythm. GW791343 trihydrochloride can be used in study of neurological disease .
|
-
- HY-W009776
-
|
Suberohydroxamic acid; SBHA
|
HDAC
Apoptosis
|
Cancer
|
|
Suberoyl bis-hydroxamic acid (Suberohydroxamic acid; SBHA) is a competitive and cell-permeable HDAC1 and HDAC3 inhibitor with ID50 values of 0.25 μM and 0.30 μM, respectively .Suberoyl bis-hydroxamic acid renders MM cells susceptible to apoptosis and facilitates the mitochondrial apoptotic pathways .Suberoyl bis-hydroxamic acid can be used for the study of medullary thyroid carcinoma (MTC) .
|
-
- HY-114209
-
|
|
Histone Methyltransferase
|
Cancer
|
|
MRK-740 is a potent, selective and substrate-competitive PRDM9 histone methyltransferase inhibitor with an IC50 of 80 nM. MRK-740 is more selective for PRDM9 than other histone methyltransferases and other non-epigenetic targets. MRK-740 reduces PRDM9-dependent trimethylation of H3K4 (IC50 = 0.8 µM) .
|
-
- HY-17504AS
-
-
- HY-B0113A
-
|
H 16868 sodium
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria . Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-14892A
-
|
LC15-0444 tartrate
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Gemigliptin tartrate (LC15-0444 tartrate) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin tartrate exhibits potent anti-glycation properties. Gemigliptin tartrate can be used for the research of advanced glycation end products (AGE)-related diabetic complications .
|
-
- HY-137231B
-
|
|
nAChR
|
Neurological Disease
|
|
(S)-UFR2709 (hydrochloride) is a competitive nAChR antagonist and displays higher affinity for α4β2 nAChRs than for α7 nAChRs. (S)-UFR2709 (hydrochloride) decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. (S)-UFR2709 (hydrochloride) acts as an anxiolytic agent and can be used for the study of nicotine addiction .
|
-
- HY-137231A
-
|
|
nAChR
|
Neurological Disease
|
|
(S)-UFR2709 is a competitive nAChR antagonist and displays higher affinity for α4β2 nAChRs than for α7 nAChRs. (S)-UFR2709 decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. (S)-UFR2709 acts as an anxiolytic agent and can be used for the study of nicotine addiction .
|
-
- HY-138696
-
|
XL092
|
TAM Receptor
c-Met/HGFR
VEGFR
|
Cancer
|
|
Zanzalintinib (XL092) is an orally active, ATP-competitive inhibitor of multiple receptor tyrosine kinases (RTKs) including MET, VEGFR2, AXL and MER, with IC50s in cell-based assays of 15 nM, 1.6 nM, 3.4 nM, 7.2 nM respectively. Zanzalintinib exhibits anti-tumor activity. Zanzalintinib has the potential for kinase-dependent diseases and conditions research .
|
-
- HY-106840
-
|
|
Cholecystokinin Receptor
|
Neurological Disease
Metabolic Disease
|
|
L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance .
|
-
- HY-12137A
-
|
BI 6727 trihydrochloride
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
Volasertib (BI 6727) trihydrochloride is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib trihydrochloride inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis. Volasertib trihydrochloride, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models .
|
-
- HY-101368A
-
|
|
Bradykinin Receptor
mAChR
|
Neurological Disease
|
|
WIN 64338 hydrochloride is a potent, selective, nonpeptide competitive antagonist of bradykinin B2 receptor. WIN 64338 hydrochloride inhibits [ 3H]-Bradykinin binding to the bradykinin B2 receptor on human IMR-90 cells with a Ki of 64 nM. WIN 64338 hydrochloride also can inhibits [ 3H]Quinuclidinyl benzilate binding to the rat brain muscarinic receptor (Ki=350 nM) .
|
-
- HY-141412
-
|
3-Phospho-D-glyceric acid disodium
|
Enolase
Phosphoglycerate Dehydrogenase (PHGDH)
MDM-2/p53
Apoptosis
|
Infection
|
|
D-(-)-3-Phosphoglyceric acid (3-Phospho-D-glyceric acid) disodium is an important intermediate in the enzyme-catalyzed glycolysis process. D-(-)-3-Phosphoglyceric acid disodium competitively inhibits yeast enolase (enolase). D-(-)-3-Phosphoglyceric acid disodium can regulate the activity of phosphoglycerate dehydrogenase (PHGDH) to modulate p53 protein and apoptosis .
|
-
- HY-103550
-
|
|
mGluR
|
Neurological Disease
|
|
A-841720 is a potent, non-competitive and selective mGlu1 receptor antagonist with an IC50 of 10 nM for human mGlu1 receptor. A-841720 displays 34-fold selectivity over mGlu5 (IC50 of 342 nM), and no significant activity at a range of other neurotransmitter receptors, ion channels, and transporters. A-841720 has the potential for chronic pain research .
|
-
- HY-B0307A
-
|
5-Iodo-2′-deoxyuridine hydrate; 5-IUdR hydrate; IdUrd hydrate
|
Phosphatase
|
Infection
|
|
Idoxuridine (5-Iodo-2′-deoxyuridine, 5-IUdR, IdUrd) hydrate is an iodinated thymidine analogue that competitively inhibits phosphorylases. Idoxuridine can inhibit viral activity, particularly viral eye infections, including herpes simplex keratitis, by inhibiting DNA polymerase and affecting viral replication. Idoxuridine against feline herpesvirus has the IC50 value of 4.3 μM .
|
-
- HY-100838
-
|
L-CCG III
|
EAAT
|
Neurological Disease
|
|
cis-α-(Carboxycyclopropyl)glycine (L-CCG III) is a potent, competitive glutamate uptake inhibitor. cis-α-(Carboxycyclopropyl)glycine is a substrate of glutamate transporters (GluT) (EC50: 13 μM, 2 μM for EAAT 1 and EAAT 2, respectively). cis-α-(Carboxycyclopropyl)glycine inhibits a Na +-dependent high-affinity L-glutamate uptake in glial plasmalemmal vesicles (GPV) and synaptosomes .
|
-
- HY-108675
-
|
|
MMP
P2X Receptor
|
Infection
Cancer
|
|
PPNDS tetrasodium is a selective and competitive meprin β inhibitor (IC50: 80 nM, Ki: 8 nM), and also inhibits ADAM10 (IC50: 1.2 μM). PPNDS tetrasodium is also a P2X1 receptor antagonist. PPNDS is an agonist for the ATP receptor of Paramecium. PPNDS tetrasodium potently inhibits polymerases from viruses. PPNDS tetrasodium can be used in the research of infection and cancers .
|
-
- HY-10583G
-
|
|
ROCK
|
Neurological Disease
Cancer
|
|
Y-27632 dihydrochloride (GMP) is the GMP level of Y-27632 dihydrochloride (HY-10583). GMP guidelines are used to produce Y-27632 dihydrochloride (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor with antiepileptic effect .
|
-
- HY-152094
-
|
|
Others
|
Endocrinology
|
|
SRD5A1-IN-1 (Compound 4) is a competitive and covalent steroid 5α-reductase type 1 (SRD5A1) inhibitor with an IC50 of 1.44 µM. SRD5A1-IN-1 modulates SRD5A1 function, leading to a lower level of dihydrotestosterone (DHT) production and SRD5A1 protein suppression .
|
-
- HY-149308
-
|
|
Macrophage migration inhibitory factor (MIF)
|
Infection
|
|
MKA031 (compound 6y) is a non-competitive MIF inhibitor with an IC50 value of 1.7 μM. MKA031 (compound 6y) interferes with MIF/AIF interaction, MIF nuclear translocation, and N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced dependent cell death. MKA031 can be used in the study of chronic hepatitis C virus infection .
|
-
- HY-13588B
-
|
SCE-129 sodium hydrate
|
Antibiotic
Bacterial
|
Infection
|
|
Cefsulodin (SCE-129) sodium is a third generation β lactam antibiotic and member of the cephems subgroup of antibiotics. Cefsulodin sodium inhibits cell wall synthesis by competitively inhibiting penicillin binding protein (PBP) cross-linking and transpeptidation of peptidogly. Cefsulodin sodium is a potent tyrosine phosphatase inhibitor against mPTPB, a virulent phosphatase from Mycobacterium tuberculosis, with an IC50 value of 16 μM .
|
-
- HY-155105
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-30 (compound 8c) is a potent, orally active, competitive inhibitor against α-glucosidase, with Ki of 40.0 µM and IC50 value of 49.0 µM. α-Glucosidase-IN-30 is non-cytotoxic against the cancer and normal cell lines MCF-7 and HDF, and can be used for Type 2 diabetes study .
|
-
- HY-14281S
-
|
Win 24540-d3
|
Isotope-Labeled Compounds
|
Others
|
|
Trilostane-d3 is the deuterium-labeled Trilostane (HY-14281). Trilostane-d3 (Win 24540) is a competitive and orally active 3-β-hydroxysteroiddehydrogenase (3β-HSD) inhibitor. Trilostane-d3 is a synthetic nonhormonal steroid. Trilostane-d3 can be used for the research of breast cancer and prostate cancer .
|
-
- HY-118190
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
AL 8810 methyl ester is a prostaglandin F(2α) analog and a prostaglandin F(2α) receptor agonist. Can competitively antagonize the effects of the FP receptor agonist Fluprostenol (HY-108560). AL 8810 methyl ester has no significant potency against TP, DP, EP(2), EP(4) receptor subtypes in cell lines .
|
-
- HY-10119S
-
|
SCH 530348-d5
|
Protease Activated Receptor (PAR)
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
Vorapaxar-d5 is deuterated labeled Vorapaxar (HY-10119). Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-117743S1
-
|
SKF-108566J free base-d6
|
Angiotensin Receptor
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
Eprosartan-d6 is deuterated labeled Eprosartan (HY-117743). Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
|
-
- HY-W010201S
-
|
(±)-Citronellol-d6; (±)-β-Citronellol-d6
|
Reactive Oxygen Species
Isotope-Labeled Compounds
|
Cancer
|
|
Citronellol-d6 is deuterated labeled Linalool (HY-N0368). Linalool is a natural monoterpene which is a competitive NMDA receptor antagonist. Linalool is orally active and crosses the blood-brain barrier. Linalool has anticancer, antibacterial, anti-inflammatory, neuroprotective, anxiolytic, antidepressant, anti-stress, cardioprotective, hepatoprotective, nephroprotective and pulmonary protective activities .
|
-
- HY-10119R
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar (Standard) is the analytical standard of Vorapaxar. This product is intended for research and analytical applications. Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-108913R
-
|
|
Beta-lactamase
Antibiotic
|
Infection
|
|
Nitrocefin (Standard) is the analytical standard of Nitrocefin. This product is intended for research and analytical applications. Nitrocefin is a chromogenic β-lactamase substrate that undergoes a distinctive color change from yellow to red as the amide bond in the β-lactam ring is hydrolyzed by β-lactamase. Nitrocefin is used in competitive inhibition studies in developmental work on β-lactamase-resistant antibiotics .
|
-
- HY-117743R
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Eprosartan (Standard) is the analytical standard of Eprosartan. This product is intended for research and analytical applications. Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
|
-
- HY-13038AR
-
|
|
Syk
FLT3
|
Inflammation/Immunology
Cancer
|
|
Fostamatinib (Standard) is the analytical standard of Fostamatinib. This product is intended for research and analytical applications. Fostamatinib (R788) is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-17443BR
-
|
|
Elastase
SARS-CoV
|
Cancer
|
|
Sivelestat (sodium tetrahydrate) (Standard) is the analytical standard of Sivelestat (sodium tetrahydrate). This product is intended for research and analytical applications. Sivelestat (EI546) sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) sodium tetrahydrate has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19 .
|
-
- HY-17623R
-
|
|
Proton Pump
|
Metabolic Disease
|
|
Tegoprazan (Standard) is the analytical standard of Tegoprazan. This product is intended for research and analytical applications. Tegoprazan (CJ-12420), a potassium-competitive acid blocker, is a potent, oral active and highly selective inhibitor of gastric H +/K +-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H +/K +-ATPases in vitro .
|
-
- HY-B0876R
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
Fomepizole (Standard) is the analytical standard of Fomepizole. This product is intended for research and analytical applications. Fomepizole (4-Methylpyrazole) is a potent cytochrome P450 (CYP2E1) inhibitor. Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole has the potential for an antidote for ethylene glycol or methanol poisoning .
|
-
- HY-120857
-
|
PD 158294
|
Others
|
Others
|
|
BPIQ-II is a linear imidazoloquinazoline that potently inhibits the tyrosine kinase activity of the epidermal growth factor receptor (EGFR; IC50=8 pM). It is selective for EGFR over an assortment of other tyrosine and serine/threonine kinases. Cellular studies indicate that BPIQ-II can enter cells and very selectively shut down EGF-stimulated signal transmission by binding competitively at the ATP site of EGFR.
|
-
- HY-134308
-
|
|
Fluorescent Dye
|
Others
|
|
8-NBD-cAMP sodium is a fluorescently labeled cyclic adenosine phosphate (cAMP) analogue. 8-NBD-cAMP sodium retains a similar biological activity to cAMP, regulating their activity by binding to specific proteins such as EPACs or PKA. 8-NBD-cAMP sodium can be used in fluorescent competitive binding experiments to evaluate the binding affinity of newly synthesized EPAC1 agonists to EPAC1 proteins .
|
-
- HY-161681
-
|
|
Guanylate Cyclase
|
Metabolic Disease
|
|
Formycin triphosphate is a fluorescent analogue of ATP which on binding to enzyme active sites exhibits enhanced fluorescence. Formycin triphosphate is an ATP-competitive chicken liver pyruvate carboxylase inhibitor. Formycin triphosphate potentiates atrial natriuretic factor (ANF)-stimulated guanylate cyclase activity with an EC50 at about 90 μM and inhibits ATP-stimulated guanylate cyclase activity with an IC50 at about 100 μM .
|
-
- HY-B0377G
-
|
MK-208 (GMP)
|
Histamine Receptor
|
Inflammation/Immunology
Cancer
|
|
Famotidine GMP (MK-208 GMP) is Famotidine (HY-B0377) produced in GMP guideline. Famotidine GMP is a competitive histamine H2-receptor antagonist, inhibits gastric secretion, activates the gastric mucosal defensive mechanisms. Famotidine GMP ameliorates peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD/GORD) in rats model .
|
-
- HY-162675
-
|
|
GSK-3
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
COB-187 is a potent, ATP-competitive and selective inhibitor of GSK-3β. COB-187 inhibits GSK-3 through a reversible and Cysteine (Cys)-199-dependent mechanism. COB-187 inhibits LPS induced cytokine production and SARS-CoV-2 spike protein-induced CXCL10 production .
|
-
- HY-B0002AR
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Ondansetron (hydrochloride dihydrate) (Standard) is the analytical standard of Ondansetron (hydrochloride dihydrate). This product is intended for research and analytical applications. Ondansetron (GR 38032) hydrochloride dehydrate is an orally active, highly selective and competitive 5-HT3 receptor antagonist (crosses the blood-brain barrier). Ondansetron hydrochloride dehydrate can be used in studies of preventing nausea and vomiting associated with cancer chemotherapy, radiation therapy and surgery .
|
-
- HY-B0488R
-
|
|
Parasite
|
Infection
|
|
Clorsulon (Standard) is the analytical standard of Clorsulon. This product is intended for research and analytical applications. Clorsulon (L631529; MK401) is an orally active flukicidal agent against liver flukes (Fasciola hepatica and Fasciola gigantica) infections in calves and sheep.?Clorsulon is also a competitive inhibitor of both 3-phosphoglycorate and ATP andinhibits glucose utilization and acetate and propionate formation by mature Fasciola hepatica in vitro .
|
-
- HY-B1866R
-
|
|
Androgen Receptor
|
Endocrinology
|
|
Linuron (Standard) is the analytical standard of Linuron. This product is intended for research and analytical applications. Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive androgen receptor (AR) antagonist with a Ki of 100 μM. Linuron shows reproductive toxicity in animals that acts as an endocrine disruptor .
|
-
- HY-N1919R
-
|
|
Adrenergic Receptor
Cholinesterase (ChE)
|
Neurological Disease
Endocrinology
|
|
Ajmalicine (Standard) is the analytical standard of Ajmalicine. This product is intended for research and analytical applications. Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity .
|
-
- HY-N7136R
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
α-Terpinyl acetate (Standard) is the analytical standard of α-Terpinyl acetate. This product is intended for research and analytical applications. α-Terpinyl acetate is a monoterpene ester isolated from Laurus nobilis L. essential oil. α-Terpinyl acetate is a competitive P450 2B6 substrate which binding to the active site of P450 2B6 with a Kd value of 5.4 μM .
|
-
- HY-13716
-
|
(S,R)-Noscapine
|
Opioid Receptor
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier .
|
-
- HY-123459
-
|
ABT-232; NS-49; PNO-49B
|
Others
|
Endocrinology
|
|
Garomefrine hydrochlorid (ABT-232) is an α1A-adrenergic agonist with the potential to inhibit urinary incontinence. Garomefrine hydrochlorid showed the greatest contractility in pig nasal mucosal vessels. The biological activity of Garomefrine hydrochlorid has been shown to give it a competitive advantage compared to other drugs. The potency of Garomefrine hydrochlorid makes it a valuable research object in related research .
|
-
- HY-106805
-
|
|
5-HT Receptor
|
Others
|
|
ICI 169369 is an orally active, specific serotonin and 5-HT2/5-HT1C receptor competitive antagonist. ICI 169369 exhibits Ki values of 1.79 x 10 −8 and 1.58 x 10 −6 M for 5-HT2 and 5-HT1, respectively .
|
-
- HY-50878
-
|
PF-02341066
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
|
-
- HY-12067
-
|
|
Syk
FLT3
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
R406 is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 reduces immune complex-mediated inflammation . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-10409
-
|
TG-101348; SAR 302503
|
JAK
Apoptosis
|
Cancer
|
|
Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research .
|
-
- HY-A0009
-
|
Galantamine hydrobromide
|
Cholinesterase (ChE)
nAChR
|
Neurological Disease
|
|
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
|
-
- HY-10249
-
|
|
Akt
AMPK
Autophagy
|
Cancer
|
|
GSK-690693 is an ATP-competitive pan-Akt inhibitor with IC50s of 2 nM, 13 nM, 9 nM for Akt1, Akt2 and Akt3, respectively. GSK-690693 is also an AMPK inhibitor, affects Unc-51-like autophagy activating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation .
|
-
- HY-12034
-
|
|
mTOR
Autophagy
Apoptosis
|
Cancer
|
|
WYE-354 is an ATP-competitive mTOR inhibitor with an IC50 of 5 nM. WYE-354 also inhibits PI3Kα and PI3Kγ with IC50s of 1.89 μM and 7.37 μM, respectively. WYE-354 inhibits both mTORC1 and mTORC2. WYE-354 induces autophagy activation in vitro .
|
-
- HY-13635
-
|
MK-906
|
5 alpha Reductase
|
Cancer
|
|
Finasteride (MK-906) is an orally active and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia .
|
-
- HY-17504
-
|
Rosuvastatin hemicalcium; ZD 4522 Calcium
|
HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
Bacterial
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Calcium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-18174
-
|
LY2606368
|
Checkpoint Kinase (Chk)
Apoptosis
|
Cancer
|
|
Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity .
|
-
- HY-B0368
-
|
SQ 14225
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
Cancer
|
|
Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM .
|
-
- HY-B0369A
-
|
|
iGluR
|
Neurological Disease
|
|
Orphenadrine citrate is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine citrate relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine citrate is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases .
|
-
- HY-18174A
-
|
LY2606368 dihydrochloride
|
Checkpoint Kinase (Chk)
Apoptosis
|
Cancer
|
|
Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dihydrochloride inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity .
|
-
- HY-16903
-
|
|
PKC
|
Inflammation/Immunology
|
|
PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.
|
-
- HY-B0985
-
|
|
TRP Channel
|
Neurological Disease
|
|
Phenazopyridine hydrochlorideis a competitive SARM1 inhibitor, with IC50 145 μM. Phenazopyridine hydrochlorideis a TRPM8 antagonist. Phenazopyridine hydrochloride has a local anesthetic/analgesic effect. Phenazopyridine hydrochlorideis used to relieve painful symptoms of conditions such as cystitis and urethritis. Phenazopyridine hydrochloridecan promote neuronal differentiation and can also be used in the study of traumatic brain injury, peripheral neuropathy and neurodegenerative diseases .
|
-
- HY-12542A
-
|
Dantrolene sodium hydrate
|
Calcium Channel
Autophagy
|
Others
|
|
Dantrolene sodium hemiheptahydrate is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene sodium hemiheptahydrate is a ryanodine receptor (RyR) antagonist and Ca2+ signaling stabilizer. Dantrolene sodium hemiheptahydrate is a direct-acting skeletal muscle relaxant. Dantrolene sodium hemiheptahydrate can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome .
|
-
- HY-100201
-
A-196
5 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
|
A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 25 nM and 144 nM, respectively. A-196 inhibits SUV4-20 biochemically in a substrate-competitive manner. A-196 represents a first-in-class chemical probe of SUV4-20 to investigate the role of histone methyltransferases in genomic integrity .
|
-
- HY-103265
-
|
FPL 67156 trisodium
|
NTPDase
|
Cardiovascular Disease
Inflammation/Immunology
|
|
ARL67156 (FPL 67156) trisodium is a selective small molecular inhibitor, targeting to ecto-ATPase, CD39, and CD73. ARL67156 trisodium is also a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12?μM, respectively. ARL67156 trisodium can be used in the research of calcific aortic valve disease, asthma .
|
-
- HY-P1740
-
|
|
Integrin
Apoptosis
Caspase
|
Inflammation/Immunology
|
|
RGD peptide (GRGDNP) is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) plays an important role in cell adhesion, migration, growth, and differentiation .
|
-
- HY-107536
-
ML 145
1 Publications Verification
|
GPR35
CXCR
|
Inflammation/Immunology
Endocrinology
|
|
ML 145 is a selective and competitive human GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM. ML 145 has over 1000-fold more selective for GPR35 compared to GPR55 (IC50/EC50=21.7 μM) . ML 145 has no significant activity for GPR35 at either rodent ortholog .
|
-
- HY-107477
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
GSK8573 is an inactive control compound for GSK2801 (acetyl-lysine competitive inhibitor of BAZ2A and BAZ2B bromodomains). GSK8573 has binding activity to BRD9 with a Kd value of 1.04 μM and is inactive against BAZ2A/B and other bromodomain familiy. GSK8573 can be used as a structurally related negative control compound in biological experiments .
|
-
- HY-15844
-
|
Tyrphostin AG-825
|
EGFR
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
AG-825 (Tyrphostin AG-825) is a selective and ATP-competitive ErbB2 inhibitor which suppresses tyrosine phosphorylation, with an IC50 of 0.35 μM. AG-825 displays anti-cancer activity . AG825 significantly accelerates apoptosis of human neutrophils . AG-825 is a potential agent for overcoming Mn-induced neurotoxicity or AD development .
|
-
- HY-130250
-
|
|
CDK
Apoptosis
|
Cancer
|
|
SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 (CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM). SR-4835 acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death .
|
-
- HY-107427
-
|
|
MAPKAPK2 (MK2)
p38 MAPK
|
Inflammation/Immunology
|
|
PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect .
|
-
- HY-108476
-
INDY
2 Publications Verification
|
DYRK
|
Cancer
|
|
INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC50s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a Ki value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells .
|
-
- HY-101764
-
|
SR 27897
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin .
|
-
- HY-107407
-
|
|
Checkpoint Kinase (Chk)
CDK
PKC
Apoptosis
|
Cancer
|
|
SB-218078 is a potent, selective, ATP-competitive and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest .
|
-
- HY-106934
-
|
BCX 34
|
Nucleoside Antimetabolite/Analog
HIV
|
Infection
Inflammation/Immunology
Cancer
|
|
Peldesine (BCX 34) is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research .
|
-
- HY-106634
-
|
Methylglyoxal-bis(guanylhydrazone); MGBG; Methyl-GAG
|
HIV
Apoptosis
|
Infection
Cancer
|
|
Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment .
|
-
- HY-108676
-
|
|
P2X Receptor
|
Neurological Disease
|
|
NF023 hexasodium is a selective and competitive P2X1 receptor antagonist, with IC50 values of 0.21 μM, 28.9 μM, > 50 μM and > 100 μM for human P2X1, P2X3, P2X2, and P2X4-mediated responses respectively .
|
-
- HY-10409A
-
|
TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate
|
JAK
Apoptosis
|
Cancer
|
|
Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research .
|
-
- HY-136575
-
|
|
Virus Protease
|
Infection
|
|
4-Hydroxy-2-methylbenzenesulfonic acid ammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability .
|
-
- HY-14664B
-
|
(3R,5S)-XU 62-320 free acid
|
HMG-CoA Reductase (HMGCR)
Autophagy
|
Cardiovascular Disease
Cancer
|
|
(3R,5S)-Fluvastatin is the 3R,5S-isomer Fluvastatin. Fluvastatin (XU 62-320 free acid) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway .
|
-
- HY-136574
-
|
|
Virus Protease
|
Infection
|
|
2-Hydroxy-4-methylbenzenesulphonic acid ammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability .
|
-
- HY-133120
-
|
|
PROTACs
Akt
|
Cancer
|
|
INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively .
|
-
- HY-18174B
-
|
LY2606368 Mesylate Hydrate; LY2940930
|
Checkpoint Kinase (Chk)
Apoptosis
|
Cancer
|
|
Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib Mesylate Hydrate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor activity .
|
-
- HY-106934A
-
|
BCX 34 dihydrochloride
|
Nucleoside Antimetabolite/Analog
HIV
|
Infection
Inflammation/Immunology
Cancer
|
|
Peldesine (BCX 34) dihydrochloride is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine dihydrochloride is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine dihydrochloride has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research .
|
-
- HY-133123
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
Cancer
|
|
EP4 receptor antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist for cancer immunotherapy. EP4 receptor antagonist 1 inhibits human and mouse EP4 receptor with IC50s of 6.1 nM and 16.2 nM, respectively. IC50s >10 μM for human EP1, EP2,and EP3 receptors .
|
-
- HY-13241A
-
|
LY2228820
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Ralimetinib (LY2228820) is a potent and selective, ATP-competitive inhibitor of p38 MAPK α/β, with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc .
|
-
- HY-P3143A
-
|
|
PD-1/PD-L1
|
Cancer
|
|
BMSpep-57 hydrochloride is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68?nM. BMSpep-57 hydrochloride binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 hydrochloride facilitates T cell function by in creasing IL-2 production in PBMCs .
|
-
- HY-103274
-
|
|
Bcr-Abl
Src
c-Kit
Apoptosis
|
Neurological Disease
Cancer
|
|
PD180970 is a highly potent and ATP-competitive p210 Bcr-Abl kinase inhibitor, with an IC50 of 5 nM for inhibiting the autophosphorylation of p210 Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC50s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research .
|
-
- HY-141519
-
|
|
Parasite
|
Infection
|
|
PI-55 is a specific cytokinin receptor inhibitor. PI-55 is structurally related to 6-benzylaminopurine (BAP) and was shown to inhibit competitively BAP binding on Arabidopsis-specific receptors CRE1/AHK4 and AHK3. PI-55 inhibits cytokinins induced haustorium formation and increased parasite aggressiveness .
|
-
- HY-115745
-
|
|
Calmodulin
|
Cardiovascular Disease
|
|
Calmodulin antagonist-1 (A-5) is a calmodulin (CaM) antagonist. Calmodulin antagonist-1 inhibits calmodulin-activated Ca 2+-phosphodiesterase (PDE) (IC50=66 μM). Calmodulin antagonist-1 also inhibits trypsin-treated Ca 2+-PDE (IC50=560 μM) in a competitive fashion with respect to cyclic GMP .
|
-
- HY-139004
-
|
|
Casein Kinase
|
Neurological Disease
|
|
SGC-CK2-1 is a highly potent, ATP-competitive, and cell-active CK2 chemical probe with exclusive selectivity for both human CK2 isoforms, with IC50s of 36 and 16 nM for CK2α and CK2α′respectively in the nanoBRET assay. SGC-CK2-1 can be used for the research of neurodegenerative diseases .
|
-
- HY-117822
-
|
|
GSK-3
|
Neurological Disease
|
|
BRD0209 is a potent, selective and dual inhibitor of GSK3α/β inhibitor (GSK3α IC50 = 19 nM; GSK3β IC50 = 5 nM). BRD0209 is also a reversible ATP-competitive inhibitor with fast-off kinetics (Ki = 4.2 nM, respectively). BRD0209 is a tricyclic pyrazolotetrahydroquinolinone compound. BRD0209 has the potential for the research of mood disorder diseases .
|
-
- HY-18174C
-
|
LY2606368 mesylate
|
Checkpoint Kinase (Chk)
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Prexasertib mesylate (LY2606368 mesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib mesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib mesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib mesylate shows potent anti-tumor activity .
|
-
- HY-116852S
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Thiocolchicine-d3 is deuterium labeled Thiocolchicine. Thiocolchicine, a derivative modified in the C Ring of Colchicine (HY-16569) with enhanced biological properties. Thiocolchicine is a potent inhibitor of tubulin polymerization (IC50=2.5 µM) and competitively binds to tubulin with a Ki of 0.7 µM. Thiocolchicine induces cell apoptosis[1][2]. Thiocolchicine can be used as an ADC cytotoxin in ADC technology.
|
-
- HY-B0290S1
-
-
- HY-N0192S
-
|
β-Arbutin-d4
|
Isotope-Labeled Compounds
Tyrosinase
Endogenous Metabolite
|
Cancer
|
|
Arbutin-d4 is deuterium labeled Arbutin. Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase in melanocytes, with Kiapp values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents[1]. Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties[2][3].
|
-
- HY-12542S
-
|
F 368-13C3
|
Isotope-Labeled Compounds
Glutathione Reductase
|
Neurological Disease
Inflammation/Immunology
|
|
Dantrolene- 13C3 is the 13C3 labeled Dantrolene. Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyte glutathione reductase. Ki and IC50 values are 111.6 μM and 52.3 μM, respectively. Dantrolene is a ryanodine receptor antagonist and Ca2+ signaling stabilizer. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.
|
-
- HY-B0368A
-
|
SQ 14225 hydrochloride
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Captopril (SQ 14225) hydrochloride, antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril hydrochloride is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM .
|
-
- HY-123099
-
|
|
JAK
|
Cancer
|
|
MS-1020 is a potent and ATP-competitive JAK3 inhibitor. MS-1020 inhibits JAK3/STAT signaling and induces apoptosis. MS-1020 promotes cell death. MS-1020 decreases the expression of tyrosine phosphorylated STAT3 levels. MS-1020 has the potential for the research of cancers harboring aberrant JAK3 signaling .
|
-
- HY-P0096
-
|
|
Tyrosinase
Sirtuin
|
Inflammation/Immunology
Endocrinology
|
|
Decapeptide-12, a small oligopeptide, is a tyrosinase inhibitor that interacts with C-terminal residue of tyrosinase (Kd: 61.1 μM). Decapeptide-12 is a competitive inhibitor of mushroom tyrosinase (IC50: 40 μM). Decapeptide-12 also increases transcription of SIRT. Decapeptide-12 reduces melanin content in melanocytes. Decapeptide-12 is used for the research of melanogenesis, senescence, inflammation .
|
-
- HY-130553
-
|
β-NAAG; β-N-Acetylaspartylglutamic acid
|
Aminopeptidase
mGluR
|
Neurological Disease
|
|
β-Spaglumic acid (β-NAAG) is a competitive NAAG peptidase inhibitor (Ki=1 µM) that protects spinal cord neurons from excitotoxicity and hypoxic damage. β-Spaglumic acid is also a selective mGluR3 antagonist (mGluR3 receptor functions to regulate activity-dependent synaptic potentiation in the hippocampus). β-Spaglumic acid can be used in neuroprotection-related studies .
|
-
- HY-133120A
-
|
|
PROTACs
Akt
|
Cancer
|
|
INY-03-041 trihydrochloride is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 trihydrochloride inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively .
|
-
- HY-P3850
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
(D-Pro2,D-Trp6,8,Nle10)-Neurokinin B is a competitive antagonist of Neurokinin B (Neurokinin Receptor) with a pA2 of 5.5. (D-Pro2,D-Trp6,8,Nle10)-Neurokinin B shows no influence on Substance P or Neurokinin A .
|
-
- HY-15883
-
|
|
Checkpoint Kinase (Chk)
Apoptosis
|
Cancer
|
|
GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 µM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity .
|
-
- HY-113038AS
-
|
2-Hydroxyglutarate-13C5 disodium; 2-Hydroxyglutaric acid-13C5 sodium; 2-Hydroxypentanedioic acid-13C5 disodium
|
Histone Demethylase
Endogenous Metabolite
|
Cancer
|
|
α-Hydroxyglutaric acid- 13C5 (sodium) is the 13C labeled α-Hydroxyglutaric acid sodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) sodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid sodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[2].
|
-
- HY-A0030S
-
|
|
mAChR
|
Metabolic Disease
|
|
Fesoterodine-d7 (fumarate) is the deuterium labeled Fesoterodine fumarate[1]. Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB)[2][3].
|
-
- HY-50878B
-
|
PF-02341066 acetate
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
c-Met/HGFR
|
Cancer
|
|
Crizotinib (PF-02341066) acetate is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib acetate inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib acetate is also a ROS1 inhibitor. Crizotinib acetate has effective tumor growth inhibition .
|
-
- HY-W011834S
-
|
|
Isotope-Labeled Compounds
HCV
|
Infection
|
|
2'-O-Methylcytidine-d3 is deuterium labeled 2'-O-Methylcytidine (HY-W011834). 2'-O-Methylcytidine is a 2'-substituted nucleoside as a inhibitor of HCV replication. 2'-O-Methylcytidine inhibits RNA-dependent RNA polymerase (NS5B)-catalyzed RNA synthesis in vitro, in a manner that is competitive with substrate nucleoside triphosphate.
|
-
- HY-116096
-
|
15(R)-Prostaglandin E1; 15-Epiprostaglandin E1
|
15-PGDH
|
Others
|
|
15-epi-PGE1 (15R-Prostaglandin E1; 15-Epiprostaglandin E1) is a stereoisomer of PGE1 (HY-B0131) but with less biological activity . 15-epi-PGE1 is a non-competitive inhibitor for human placental 15-Hydroxyprostaglandin dehydrogenase (15-PGDH) with an IC50 of 170 μM .
|
-
- HY-160687
-
|
|
Others
|
Others
|
|
GW549390X is a dual inhibitor of Fluc and VEGFR2 with IC50 of 0.26 μM and 1.2 μM, respectively. GW549390X can bind to the ATP pocket of FLuc through the aniline side chain and is an ATP-competitive inhibitor of Fluc. GW549390X acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases, with potential implications for Fluc reporter assays .
|
-
- HY-10255R
-
|
|
PDGFR
VEGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib (Malate) (Standard) is the analytical standard of Sunitinib (Malate). This product is intended for research and analytical applications. Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
|
-
- HY-125146
-
|
|
Others
|
Others
|
|
BMD4503-2 is a quinoxaline derivative with inhibitory activity against LRP5/6-sclerostin interactions. BMD4503-2 restores the activity of the Wnt/β-catenin signaling pathway by competitively binding to the LRP5/6-sclerostin complex. BMD4503-2 can be used in the study of Wnt signaling pathways in bone development, maintenance and osteoporosis .
|
-
- HY-122489A
-
|
|
Others
|
Cardiovascular Disease
Neurological Disease
|
|
(S)-Laudanosine is an alkaloid that can be found in poppies and is the S-enantiomer of Laudanosine. Laudanosine acts on the central nervous system and cardiovascular system, inhibiting low-affinity GABA receptors with an IC50 value of 10 μM, and can cause seizures, hypotension, and bradycardia. Additionally, Laudanosine exerts analgesic effects by competitively binding to the opioid Mu-1 receptor (Ki = 2.7 μM) .
|
-
- HY-N0192R
-
|
|
Tyrosinase
Endogenous Metabolite
|
Cancer
|
|
Arbutin (Standard) is the analytical standard of Arbutin. This product is intended for research and analytical applications. Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase, with Kiapp values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents . Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties .
|
-
- HY-B0607R
-
|
NTBC (Standard); Nitisone (Standard); SC56735 (Standard)
|
HPPD
|
Metabolic Disease
|
|
Nitisinone (Standard) is the analytical standard of Nitisinone. This product is intended for research and analytical applications. Nitisinone is an orally active, competitive and reversible 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) inhibitor with an IC50 of 173 nM. Nitisinone promotes tyrosine accumulation in a dose-dependent manner. nitisinone can be used in studies of hereditary tyrosinemia type 1 (HT-1) (a rare genetic disorder) and albinism .
|
-
- HY-17423AR
-
|
|
Reverse Transcriptase
HIV
Telomerase
Apoptosis
|
Infection
|
|
Abacavir (sulfate) (Standard) is the analytical standard of Abacavir (sulfate). This product is intended for research and analytical applications. Abacavir sulfate (Abacavir Hemisulfate) is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir sulfate can inhibits the replication of HIV. Abacavir sulfate shows anticancer activity in prostate cancer cell lines. Abacavir sulfate can trespass the blood-brain-barrier and suppresses telomerase activity .
|
-
- HY-B0371AR
-
|
|
Adrenergic Receptor
|
Metabolic Disease
Endocrinology
|
|
Terazosin (hydrochloride dihydrate) (Standard) is the analytical standard of Terazosin (hydrochloride dihydrate). This product is intended for research and analytical applications. Terazosin hydrochloride dihydrate is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin hydrochloride dihydrate works by relaxing blood vessels and the opening of the bladder. Terazosin hydrochloride dihydrate has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment .
|
-
- HY-W009156R
-
|
|
ATP Citrate Lyase
HIF/HIF Prolyl-Hydroxylase
Bacterial
Endogenous Metabolite
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Citric acid (tripotassium hydrate) (Standard) is the analytical standard of Citric acid (tripotassium hydrate). This product is intended for research and analytical applications. Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) is the major active ingredient of Garcinia cambogia. Hydroxycitric acid tripotassium hydrate competitively inhibits ATP citrate lyase with weight loss benefits. Hydroxycitric acid tripotassium hydrate effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects .
|
-
- HY-111291
-
|
|
5-HT Receptor
|
Neurological Disease
Endocrinology
|
|
ICI 169369 (free base) is an orally active, selective and non-competitive antagonist against 5HT receptor. ICI 169369 (free base) blunts the vasopressin (AVP), but not the ACTH, prolactin or growth hormone reponses to insulin-induced hypoglycaemia. ICI 169369 (free base) blocks centrally mediated 5-HT responses and lowers portal pressure in portal hypertensive rats .
|
-
- HY-120039
-
|
|
Elastase
|
Inflammation/Immunology
|
|
(R)-MDL-101146 is the R-isomer of MDL-101146. MDL-101146 is an orally active, competitive and reversible inhibitor against human neutrophil elastase (HNE) with a Ki value of 25 nM. MDL-101146 inhibits HNE-induced hemorrhage in hamsters. MDL-101146 is promising for research of emphysema, rheumatoid arthritis, chronic bronchitis, cystic fibrosis, adult respiratory distress syndrome and glomerulonephritis .
|
-
- HY-120039A
-
|
|
Elastase
|
Inflammation/Immunology
|
|
(S)-MDL-101146 is the S-isomer of MDL-101146. MDL-101146 is an orally active, competitive and reversible inhibitor against human neutrophil elastase (HNE) with a Ki value of 25 nM. MDL-101146 inhibits HNE-induced hemorrhage in hamsters. MDL-101146 is promising for research of emphysema, rheumatoid arthritis, chronic bronchitis, cystic fibrosis, adult respiratory distress syndrome and glomerulonephritis .
|
-
- HY-101586A
-
|
Lu 25-109 maleate
|
mAChR
|
Neurological Disease
|
|
Alvameline (Lu 25-109) maleate is a partial agonist of M1 and an antagonist of M2/M3. Alvameline maleate competitively antagonizes contractions induced by ammonium chloride (HY-Y1269) and electrical field stimulation in human detrusor muscle, indicating its potential application in regulating bladder function. Additionally, alvameline maleate can improve cognitive function following traumatic brain injury in rats .
|
-
- HY-P10668
-
|
|
Dengue virus
Flavivirus
|
Infection
|
|
Ac-EVKKQR-pNA is a competitive chromogenic para-nitroanilide substrate corresponding to the P6-P1 segment amino-terminal to the NS2B-NS3 cleavage site but with a more reactive, hydrolytically cleavable, para-nitroanilide at the P1’ position. Ac-EVKKQR-pNA is promising for research of dengue 2 virus and flavivirus virus infection .
|
-
- HY-167855
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
MRS4833 (compound 15) is an orally active, potent, competitive P2Y14R antagonist with IC50=5.92 nM for hP2Y14R and IC50=4.8 nM for mP2Y14R. MRS4833 reduces airway eosinophilia in a protease-mediated asthma model and reverses chronic neuropathic pain in a mouse CCI model .
|
-
- HY-11107
-
|
|
c-Met/HGFR
Autophagy
Apoptosis
|
Cancer
|
|
PHA-665752 is a selective, ATP-competitive, and active-site inhibitor of the catalytic activity of c-Met kinase (Ki=4 nM; IC50=9 nM). PHA-665752 exhibits >50-fold selectivity for c-Met compared with a panel of diverse tyrosine and serine-threonine kinases. PHA-665752 induces apoptosis and cell cycle arrest, and exhibits cytoreductive antitumor activity .
|
-
- HY-10424
-
|
PHA-848125
|
CDK
Autophagy
|
Cancer
|
|
Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.
|
-
- HY-12037
-
|
ON-01910 sodium
|
Polo-like Kinase (PLK)
PI3K
Apoptosis
|
Cancer
|
|
Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib sodium is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM .
|
-
- HY-10683
-
|
|
PI3K
mTOR
|
Cancer
|
|
PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC50=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).
|
-
- HY-17395
-
|
TDT 067 hydrochloride
|
Fungal
Bacterial
Antibiotic
|
Infection
|
|
Terbinafine hydrochloride (TDT 067 hydrochloride) is an orally active and potent antifungal agent. Terbinafine hydrochloride is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a Ki of 30 nM. Terbinafine hydrochloride also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria . Terbinafine hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-17395A
-
|
TDT 067
|
Fungal
Bacterial
Antibiotic
|
Infection
|
|
Terbinafine (TDT 067) is an orally active and potent antifungal agent. Terbinafine is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a Ki of 30 nM. Terbinafine also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria . Terbinafine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-B0307
-
|
5-Iodo-2′-deoxyuridine; 5-IUdR; IdUrd
|
Phosphatase
Orthopoxvirus
|
Infection
Cancer
|
|
Idoxuridine (5-Iodo-2′-deoxyuridine, 5-IUdR, IdUrd) is an iodinated thymidine analogue that competitively inhibits phosphorylases. Idoxuridine can inhibit viral activity, particularly viral eye infections, including herpes simplex keratitis, by inhibiting DNA polymerase and affecting viral replication. Idoxuridine against feline herpesvirus has the IC50 value of 4.3 μM . Idoxuridine shows anti-orthopoxvirus activity.
|
-
- HY-10805
-
|
ACT 078573
|
Orexin Receptor (OX Receptor)
Calcium Channel
Caspase
Apoptosis
|
Neurological Disease
Endocrinology
Cancer
|
|
Almorexant (ACT 078573) is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant totally blocked the intracellular Ca 2+ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis .
|
-
- HY-10805A
-
|
ACT 078573 hydrochloride
|
Orexin Receptor (OX Receptor)
Calcium Channel
Caspase
Apoptosis
|
Neurological Disease
Endocrinology
Cancer
|
|
Almorexant (ACT 078573) hydrochloride is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant hydrochloride reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant hydrochloride totally blocked the intracellular Ca 2+ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis .
|
-
- HY-12830
-
|
|
Pim
|
Cancer
|
|
M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM .
|
-
- HY-15586
-
L67
1 Publications Verification
DNA Ligase Inhibitor
|
DNA/RNA Synthesis
Caspase
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
L67 (DNA Ligase Inhibitor) is a competitive DNA ligase inhibitor that effectively inhibits DNA ligases I/III (both IC50 are 10 μM). L67 can cause nuclear DNA damage by reducing levels of mitochondrial DNA and increasing levels of mitochondrially-generated ROS. L67 also activates the Caspase 1-dependent apoptosis pathway in cancer cells, can be used in cancer research .
|
-
- HY-19340
-
|
(E)-2,3',4,5'-tetramethoxystilbene
|
Cytochrome P450
|
Cancer
|
|
TMS ((E)-2,3',4,5'-tetramethoxystilbene) is a selective and competitive CYP1B1 inhibitor with an IC50 of 6 nM and a Ki value of 3 nM. TMS shows a lesser extent inhibitory effect on CYP1A1 (IC50=300 nM) and CYP1A2 (IC50=3.1 μM). TMS is a methylated derivative of resveratrol and has anti-cancer activity .
|
-
- HY-13072
-
|
AS-703569; R-763
|
Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
|
Cancer
|
|
Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
|
-
- HY-N2553
-
|
|
LPL Receptor
|
Metabolic Disease
|
|
4-Deoxypyridoxine 5'-phosphate is a Pyridoxal 5'-phosphate analogue and a sphingosine 1-phosphate (S1P) inhibitor. 4-Deoxypyridoxine 5'-phosphate inhibits ornithine decarboxylase activity with a Ki of 60 μM. 4-Deoxypyridoxine 5'-phosphate is a competitive inhibitor of the activation of glutamate apodecarboxylase by Pyridoxal 5'-phosphate (Ki of 0.27 μM) and strongly inhibits glutamate-dependent labeling of glutamate decarboxylase .
|
-
- HY-136573
-
|
|
Virus Protease
|
Infection
|
|
5-Hydroxytoluene-2,4-disulphonic acid diammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability .
|
-
- HY-14664DS
-
|
(3S,5R)-XU 62-320-d6 free acid
|
Autophagy
|
Cardiovascular Disease
Cancer
|
|
(3S,5R)-Fluvastatin-d6 is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
|
-
- HY-13457
-
TCN 201
1 Publications Verification
|
iGluR
|
Neurological Disease
|
|
TCN 201 is a potent, selective and non-competitive antagonist of GluN1/GluN2A NMDA receptor, with a pIC50 of 6.8. TCN 201 is selective for GluN1/GluN2A NMDA receptor over GluN1/GluN2B NMDA receptor (pIC50<4.3) .
|
-
- HY-P1318
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
|
-
- HY-P1318A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
|
-
- HY-101222
-
|
|
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
SB-203186 hydrochloride is a potent, selective and competitive 5-HT4 antagonist. SB-203186 hydrochloride antagonizes the 5-HT4 receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pKB values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively .
|
-
- HY-W097792
-
|
5'-O-DMT-dU
|
DNA/RNA Synthesis
|
Others
|
|
5'-O-(4,4'-Dimethoxytrityl)-2'-deoxyuridine (5'-O-DMT-dU) is a competitive inhibitor of E. coli dUTP nucleotidohydrolase (dUTPase), with the Ki higher than 1000 μM. 5'-O-(4,4'-Dimethoxytrityl)-2'-deoxyuridine can be used in machine-assisted DNA synthesis by synthesizing nucleosidic phosphoramidite blocks .
|
-
- HY-139467
-
|
|
SHP2
PKC
|
Metabolic Disease
|
|
PF-04577806 is a potent, selective and ATP competitive PKC inhibitor. PF-04577806 shows potent inhibitory activity towards PKCα, PKCβI, PKCβII, PKCγ, and PKCθ with IC50s of 2.4 nM, 8.1 nM, 6.9 nM, 45.9 nM, and 29.5 nM, respectively. PF-04577806 can reverse retinal vascular leakage in diabetic rats .
|
-
- HY-13011S
-
|
CH5424802-d8; RO5424802-d8; AF802-d8
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Alectinib-d8 is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
|
-
- HY-105184
-
|
|
Cytochrome P450
|
Endocrinology
|
|
YM511 is a highly specific non-steroidal aromatase inhibitor. YM511 inhibits aromatase activities in microsomes from rat ovary and human placenta competitively (IC50s of 0.4 and 0.12 nM, respectively). YM511 slightly inhibits production of other steroid hormones. YM511 has the potential for suppressing estrogen-dependent action research without affecting serum levels of other steroid hormones .
|
-
- HY-110042
-
|
|
HSP
Apoptosis
|
Cancer
|
|
CCT018159, a 3,4-diaryl pyrazoleresorcinol, is a ATP-competitive HSP90 ATPase activity inhibitor with IC50s of 3.2 and 6.6 µM for human Hsp90β and yeast Hsp90, respectively. CCT018159 caused cell cytostasis associated with a G1 arrest and induces apoptosis. CCT018159 inhibits key endothelial and tumor cell functions implicated in invasion and angiogenesis .
|
-
- HY-13011S1
-
|
CH5424802-d6; RO5424802-d6; AF802-d6
|
Isotope-Labeled Compounds
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
|
-
- HY-N7389A
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
GDP-D-mannose disodium contains GDP-α-D-mannose (HY-N7389B) and GDP-β-D-mannose. GDP-α-D-mannose is the donor substrate for mannosyltransferases and the precursor of GDP-β-L-fucose. GDP-α-D-mannose gives a competitive inhibition with respect to GTP (Ki 14.7 μM) and an uncompetitive inhibition with respect to mannose-1-P (Ki 115 μM) .
|
-
- HY-146142
-
|
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
|
AChE/BuChE-IN-2 (Compound 5f) is an orally active AChE and BuChE inhibitor with IC50 values of 0.72 μM and 0.16 μM, respectively. AChE/BuChE-IN-2 shows a non-competitive inhibition with AChE and shows potent self-induced β-amyloid (Aβ) aggregation inhibition with an IC50 of 62.52 μM. AChE/BuChE-IN-2 can cross the BBB .
|
-
- HY-146165
-
|
|
Beta-lactamase
Bacterial
|
Infection
|
|
Metallo-β-lactamase-IN-8 (compound 17) is a potent, reversible and competitive broad-spectrum inhibitor of metallo-β-lactamases (MβLs), with IC50s of 1.3 μM, 5.7 μM, 9.8 μM, and 9.9 μM for L1, ImiS, IMP-1 and VIM-2, respectively. Metallo-β-lactamase-IN-8 exhibits antibacterial activity .
|
-
- HY-111313
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
JNJ-26070109 is a high-affinity, competitive, orally bioactive, and selective cholecystokinin 2 (CCK2) receptor antagonist with good pharmacokinetic properties, with pKis of 8.49, 7.99, and 7.70 for human, rat, and dog CCK2 receptors, respectively. The dual function of CCK2 receptors in regulating gastric acid secretion and growth of the gastrointestinal mucosa make this an attractive and novel target for the research of gastroesophageal reflux disease .
|
-
- HY-113038AS1
-
|
2-Hydroxyglutarate-d4 disodium; 2-Hydroxyglutaric acid-d4 disodium; 2-Hydroxypentanedioic acid-d4 disodium
|
Histone Demethylase
Endogenous Metabolite
|
Cancer
|
|
α-Hydroxyglutaric acid-d4 (disodium) is the deuterium labeled α-Hydroxyglutaric acid disodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[2].
|
-
- HY-149426
-
|
|
Sirtuin
|
Inflammation/Immunology
|
|
SIRT5 inhibitor 7 (compound 58) is a substrate-competitive and selective SIRT5 inhibitor with anti-inflammatory activity. SIRT5 inhibitor 7 has renal protective effects and regulates protein succinylation and the release of pro-inflammatory cytokines. SIRT5 inhibitor 7 has in vivo activity in AKI mouse models of lipopolysaccharide (LPS) and cecal ligation/perforation (CLP)-induced sepsis-related acute kidney injury .
|
-
- HY-157116
-
|
|
ICMT
|
Cancer
|
|
ICMT-IN-48 (compound 1) is an ICMT inhibitor that is competitive (Km=13 μM) for the prenylated methyl acceptor, the first substrate of ICMT. ICMT-IN-48 inhibits ICMT activity with IC50s affected by the concentration of the second substrate S-adenosylmethinine (SAM), and the IC50s are 3.5 μM (1×Km SAM) and 2.3 μM (10×Km SAM), respectively .
|
-
- HY-B1205R
-
|
Tropine tropate (Standard); DL-Hyoscyamine (Standard)
|
mAChR
Endogenous Metabolite
|
Cardiovascular Disease
Neurological Disease
|
|
Atropine (Standard) is the analytical standard of Atropine. This product is intended for research and analytical applications. Atropine (Tropine tropate) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine inhibits ACh-induced relaxations in human pulmonary veins. Atropine can be used for research of anti-myopia and bradycardia .
|
-
- HY-157382
-
|
|
Cholinesterase (ChE)
Amyloid-β
MMP
|
Neurological Disease
|
|
AChE-IN-51 (compound 8C) is an orally active, non-competitive inhibitor of AChE and BChE (IC50: 84 nM, 97 nM). It also inhibits MMP-2 and amyloid Aβ1-42 aggregates (IC50: 724 nM, 302 nM). AChE-IN-51 has low cytotoxicity and in silico predicted blood-brain barrier permeability. Can be used for research on diseases such as Alzheimer's disease (AD) .
|
-
- HY-N11706
-
|
(+)-β-Cedrene
|
Fungal
|
Infection
Inflammation/Immunology
|
|
β-Cedrene ((+)-β-Cedrene) is a sesquiterpene compound that can be isolated from Centaurea kotschyi var. kotschyi and Centaurea kotschyi var. decumbens, exhibiting antibacterial, anti-inflammatory, antispasmodic, tonic, diuretic, sedative, insecticidal, and antifungal activities. β-Cedrene is also a potent competitive inhibitor of the CYP2B6-mediatedbupropion hydroxylase, with a Ki value of 1.6 μM .
|
-
- HY-163457
-
|
|
Aminoacyl-tRNA Synthetase
Parasite
|
Infection
|
|
Antileishmanial agent-27 (compound 7j) is a benzothiazolo-coumarin derivative. Antileishmanial agent-27 is a competitive inhibitor of arginyl-tRNA synthetases (ArgRSs). Antileishmanial agent-27 shows selectivity toward ArgRS of Leishmania donovani (LdArgRS) than its human counterpart (HsArgRS), with IC50 values of 1.2 and 19 μM, respectively. Antileishmanial agent-27 possesses high pharmacokinetic properties .
|
-
- HY-162480
-
|
|
Glucosidase
Phosphatase
|
Endocrinology
|
PTP1B-IN-27 (Compound 7i) is an inhibitor of protein tyrosine phosphatase 1-B (PTP‐1B)(IC50=8.2 µM). PTP1B-IN-27 also inhibits α-Glucosidase (IC50=120 µM) and shows competitive inhibition (Ki=118 µM) .
|
-
- HY-106301R
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
Devazepide (Standard) is the analytical standard of Devazepide. This product is intended for research and analytical applications. Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .
|
-
- HY-14721R
-
|
|
c-Met/HGFR
Autophagy
|
Cancer
|
|
Tepotinib (Standard) is the analytical standard of Tepotinib. This product is intended for research and analytical applications. Tepotinib (EMD-1214063) is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib inhibits c-Met phosphorylation. Tepotinib has antitumor effects .
|
-
- HY-B0290R
-
|
|
Leukotriene Receptor
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Pranlukast (Standard) is the analytical standard of Pranlukast. This product is intended for research and analytical applications. Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [ 3H]LTE4, [ 3H]LTD4, and [ 3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
|
-
- HY-P10465
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
TRPV1-Tat is an antagonistic peptide that fuses the TRPV1 (transient receptor potential vanilla subtype 1) of the cell-penetrating peptide Tat. TRPV1-Tat blocks this phosphorylation process by competitively binding to the AKAP79 binding site of TRPV1, thereby inhibiting the sensitization of TRPV1. TRPV1-Tat can be used in the study of inflammatory pain .
|
-
- HY-120600
-
|
|
Necroptosis
Apoptosis
RIP kinase
|
Inflammation/Immunology
|
|
Sibiriline is a specific competitive inhibitor of RIPK1 that targets the RIPK1 ATP-binding site and locks it in an inactive conformation. Sibiriline inhibits TNF-induced RIPK1-dependent necroptosis and RIPK1-dependent apoptosis, but does not protect cells from caspase-dependent apoptosis. Sibiriline protects mice from concanavalin A-induced hepatitis and has the potential to inhibit immune-dependent hepatitis. .
|
-
- HY-N4110R
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
Friedelin (Standard) is the analytical standard of Friedelin. This product is intended for research and analytical applications. Friedelin is isolated from isolated from the leaves of Maytenus ilicifolia(Mart). Friedelin is a noncompetitive inhibitor of CYP3A4 with IC50 and Kivalues of 10.79 ?μM and 6.16? μM, respectively. Friedelin is also a competitive inhibitor of CYP2E1 with IC50 and Ki values of 22.54? μM and 18.02 μM, respectively .
|
-
- HY-100840A
-
|
4-Carboxy-3-hydroxyphenylglycine
|
mGluR
|
Neurological Disease
|
|
(RS)-4C3HPG (4-Carboxy-3-hydroxyphenylglycine) is an effective competitive antagonist at the metabotropic glutamate receptor 1 (mGluR1) in the central nervous system, and it is also an agonist at mGluR2/3. (RS)-4C3HPG exhibits neuroprotective effects in an acute global ischemia rat model .
|
-
- HY-118175
-
|
|
Others
|
Others
|
|
RG 14921, a compound structurally related to erbstatin, was investigated for its mechanism of inhibition of epidermal growth factor (EGF) receptor tyrosine kinase and CAMP-dependent kinase activity by kinetic analysis. Both compounds are slow-binding inhibitors of EGF receptor kinase. Erbstatin inhibits EGF receptor kinase as a partially competitive inhibitor relative to ATP and peptide substrates, suggesting that it binds at different positions in the enzyme's ATP- and peptide substrate-binding sites, thereby reducing the enzyme's binding affinity for both substrates. In contrast, the derivative RG 14921 inhibits EGF receptor kinase activity as a noncompetitive inhibitor relative to ATP and peptide substrates. Structurally related compounds exhibit different modes of inhibition, suggesting that the catalytic center of the receptor kinase domain may have a dynamic and possibly extended structure. Erbstatin and RG 14921 exerted similar effects on CAMP-dependent protein kinase activity. In this system, both compounds exhibited strong inhibition and acted in a competitive inhibition manner with ATP and a noncompetitive inhibition manner with peptide substrates.
|
-
- HY-10524
-
|
|
IGF-1R
Insulin Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
GSK1904529A is a potent, selective, orally active, and ATP-competitive inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR), with IC50s of 27 and 25 nM, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity .
|
-
- HY-10580
-
|
6-Bromoindirubin-3'-oxime; BIO; MLS 2052
|
GSK-3
CDK
Apoptosis
|
Cancer
|
|
GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.
|
-
- HY-P1230
-
|
|
Dipeptidyl Peptidase
GLP Receptor
|
Metabolic Disease
|
|
HAEGT is the first N-terminal 1-5 residues of glucagon like peptide-1 (GLP-1) peptide, and the sequence is His-Ala-Glu-Gly-Thr. HAEGT acts as a competitive substrate for probing prime substrate binding sites of human dipeptidyl peptidase-IV (DPP-IV) 1, in which the N-terminal His-Ala is catalyzed cleavage by DPP-IV. HAEGT can be used in the research of diabetes, obesity .
|
-
- HY-120214
-
|
|
Syk
RET
|
Inflammation/Immunology
|
|
TAS05567 is a potent, highly selective, ATP-competitive and orally active Syk inhibitor with an IC50 of 0.37 nM. In a panel of 192 kinases, TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, JAK2, KDR and RET with IC50s of 10 nM, 4.8 nM, 600 nM and 29 nM, respectively). TAS05567 can be used for humoral immune-mediated inflammatory conditions such as autoimmune and allergic diseases .
|
-
- HY-50867
-
|
CEP-701; KT-5555
|
JAK
FLT3
Trk Receptor
Apoptosis
STAT
|
Cancer
|
|
Lestaurtinib (CEP-701) is an orally active and selective RPTKs (receptor protein tyrosine kinase) inhibitor, competitively inhibits ATP binding to the TrkA/B/C domain. Lestaurtinib inhibits RPTKs phosphorylation, with IC50s of 2, 25 and 0.9 nM for FLT3, TrkA and JAK2, respectively. Lestaurtinib induces apoptosis and cycle arrest, also can inhibit growth of tumor .
|
-
- HY-16749A
-
|
PLX-3397 hydrochloride
|
c-Fms
c-Kit
Apoptosis
|
Cancer
|
|
Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib hydrochloride exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib hydrochloride induces cell apoptosis and has anti-cancer activity .
|
-
- HY-P1740A
-
|
|
Integrin
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
RGD peptide (GRGDNP) TFA is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) TFA competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) TFA promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) TFA plays an important role in cell adhesion, migration, growth, and differentiation .
|
-
- HY-N0241
-
|
|
Cholinesterase (ChE)
|
Metabolic Disease
|
|
Rhodionin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.761 μM and a Ki of 0.769 μM . Rhodionin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL . Rhodionin exhibits potent DPPH free radical scavenging activities, with an IC50 of 19.49 μM .
|
-
- HY-123872
-
|
|
p97
|
Cancer
|
|
MSC1094308 is a non-competitive and reversible VPS4B/p97 (VCP) (I/II type AAA ATPase) allosteric inhibitor, with IC50 values of 0.71 μM and 7.2 μM for VPS4B and p97, respectively . MSC1094308 inhibits the D2 ATPase activity by binding to a agentable hotspot of p97. MSC1094308 can be used in study of cancer .
|
-
- HY-W011266
-
|
|
PDGFR
|
Cancer
|
|
JNJ-10198409 is a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor (IC50=2 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent. JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM) .
|
-
- HY-129997
-
|
|
CD38
NADPH Oxidase
Tyrosinase
|
Cardiovascular Disease
|
|
Luteolinidin chloride is a deoxyanthocyanidin isolated from the plant Sorghum bicolor with antioxidant activity. Luteolinidin chloride is a potent CD38 inhibitor (Ki=11.4 μM) and protects the heart from ischemia/reperfusion injury by preserving endothelial nitric oxide synthase (eNOS) function and preventing endothelial dysfunction. Luteolinidin chloride is also a competitive inhibitor of tyrosinase (IC50=3.7 μM) and blocks the production of melanin .
|
-
- HY-14664CS
-
|
(3S,5R)-XU 62-320-d6
|
HMG-CoA Reductase (HMGCR)
|
Cardiovascular Disease
Cancer
|
|
(3S,5R)-Fluvastatin-d6 (sodium) is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
|
-
- HY-13335
-
|
|
PKC
Apoptosis
|
Cancer
|
|
PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε) .
|
-
- HY-125957
-
|
|
PKA
Casein Kinase
CaMK
PKC
|
Others
|
|
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 μM), casein kinase II (Ki=5.1 μM) and myosin light chain kinase (MLCK) (Ki=7.4 μM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 μM and 80 μM, respectively .
|
-
- HY-16576A
-
SMI-4a
1 Publications Verification
TCS-PIM-1-4a
|
Pim
|
Cancer
|
|
SMI-4a (TCS-PIM-1-4a) is a poten, selective, cell-permeable and ATP-competitive Pim-1 inhibitor with an IC50 of 24 μM and a Ki of 0.6 μM. SMI-4a also inhibits Pim-2 (IC50 of 100 μM), and does not significantly inhibit the other serine/threonine- or tyrosine-kinases. SMI-4a has anticancer activity .
|
-
- HY-18174E
-
|
LY2606368 dimesylate
|
Checkpoint Kinase (Chk)
Apoptosis
|
Cancer
|
|
Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity .
|
-
- HY-103265B
-
|
FPL 67156 trisodium hydrate
|
NTPDase
|
Cardiovascular Disease
Inflammation/Immunology
|
|
ARL67156 (FPL 67156) trisodium hydrate is a selective small is a selective samll molecular inhibitor, targeting to ecto-ATPase, CD39, and CD73. ARL67156 trisodium hydrate is also a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12?μM, respectively. ARL67156 trisodium hydrate can be used in the research of disease like calcific aortic valve disease, asthma .
|
-
- HY-116815
-
|
|
Beta-lactamase
Bacterial
|
Infection
Neurological Disease
|
|
Lalistat 1 is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) and against purified human LAL (phLAL) with an IC50 of 68 nM. Lalistat 1 is a inhibitor of immunoglobulin A1 protease (IgA1P) proteases for H. influenzae, has less effects on other serine hydrolases (trypsin or β-lactamase, etc.). Lalistat 1 can be used for the research of niemann-pick type C (NPC) disease .
|
-
- HY-P3143
-
|
|
PD-1/PD-L1
|
Cancer
|
|
BMSpep-57 is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50?of 7.68?nM. BMSpep-57 binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST?and SPR assays, respectively.?BMSpep-57?facilitates T cell function by in creasing IL-2 production in PBMCs .
|
-
- HY-103441
-
|
|
EGFR
|
Cancer
|
|
JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2 .
|
-
- HY-139577
-
|
IMB-1018972; IMB-101
|
Mitochondrial Metabolism
|
Cardiovascular Disease
Metabolic Disease
|
|
Ninerafaxstat (IMB-1018972) is a novel orally active cardiac mitochondrial drug that restores myocardial energy homeostasis. Ninerafaxstat competitively inhibits 3-ketoacyl-CoA thiolase (3-KAT) to partially suppress fatty acid oxidation, and shifts cardiac energy metabolism from free fatty acid oxidation to glucose oxidation, regulating myocardial substrate utilization and thereby improving cardiac efficiency. Ninerafaxstat can be used for research on cardiovascular diseases .
|
-
- HY-110152
-
|
|
mGluR
|
Neurological Disease
|
|
LSN2463359 is positive allosteric modulator of metabotropic glutamate 5 (mGlu5). LSN2463359 attenuates aspects of the behavioral response to administration of the competitive NMDA receptor antagonist. LSN2463359 selectively attenuates reversal learning deficits observed in the neurodevelopmental MAM E17 model . LSN2463359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-103265D
-
|
FPL 67156 triethylamine
|
NTPDase
|
Cardiovascular Disease
Inflammation/Immunology
|
|
ARL67156 (FPL 67156) triethylamine is a selective small is a selective samll molecular inhibitor, targeting to ecto-ATPase, CD39, and CD73. ARL67156 triethylamine is also a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12?μM, respectively. ARL67156 triethylamine can be used in the research of disease like calcific aortic valve disease, asthma .
|
-
- HY-143288
-
|
|
NTPDase
|
Infection
Inflammation/Immunology
Cancer
|
|
NTPDase-IN-2 (compound 5g) is a selective NTPDase inhibitor with IC50s of 0.04 and 2.27 µM for h-NTPDase-2/-8, respectively. NTPDase-IN-2 non-competitively inhibits h-NTPDase-1/-2 with a Km of 74 µM for h-NTPDase-2. NTPDase-IN-2 can be used in studies of cancer, immunologic disorders as well as bacterial infections .
|
-
- HY-W401531S
-
|
|
Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
(R)-3-O-Methyldopa-d3 is a deuterium labeled (R)-3-O-Methyldopa, and (R)-3-O-Methyldopa is an R-enantiomer of 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of L-DOPA and dopamine[1][2].
|
-
- HY-W401531S1
-
|
|
Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
(R)-3-O-Methyldopa-d3 (hydrochloride) is a deuterium labeled (R)-3-O-Methyldopa, and (R)-3-O-Methyldopa is an R-enantiomer of 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of L-DOPA and dopamine[1][2].
|
-
- HY-123983
-
|
|
Pim
DAPK
|
Cardiovascular Disease
|
|
HS56 is an ATP-competitive dual Pim/DAPK3 inhibitor with Ki values of 0.26, 0.208, 2.94, and ＞100 μM for DAPK3, Pim-3, Pim-1, and Pim-2, respectively. HS56 inhibits LC20 phosphorylation and smooth muscle contraction. HS56 decreases blood pressure in spontaneously hypertensive mice. HS56 can be used in research of hypertension .
|
-
- HY-153219A
-
|
|
Potassium Channel
|
Endocrinology
|
|
P-CAB agent 2 is a potent and orally active potassium-competitive acid blocker and a gastric acid secretion inhibitor. P-CAB agent 2 inhibits H +/K +-ATPase activity with an IC50 value of <100 nM. P-CAB agent 2 inhibits the hERG potassium channel with an IC50 value of 18.69 M. P-CAB agent 2 shows no acute toxicity and inhibits histamine (HY-B1204)-induced gastric acid secretion .
|
-
- HY-153219
-
|
|
Potassium Channel
|
Endocrinology
|
|
P-CAB agent 2 hydrochloride is a potent and orally active potassium-competitive acid blocker and a gastric acid secretion inhibitor. P-CAB agent 2 hydrochloride inhibits H +/K +-ATPase activity with an IC50 value of <100 nM. P-CAB agent 2 hydrochloride inhibits the hERG potassium channel with an IC50 value of 18.69 M. P-CAB agent 2 hydrochloride shows no acute toxicity and inhibits histamine (HY-B1204)-induced gastric acid secretion .
|
-
- HY-B0267B
-
|
Aroxybutynin hydrochloride
|
mAChR
|
Neurological Disease
|
|
(R)-Oxybutynin hydrochloride, a (R)-isomer of Oxybutynin hydrochloride, is an orally active muscarinic receptor antagonist. (R)-Oxybutynin hydrochloride has antimuscarinic, antispasmodic and anticholinergic activity, competitively antagonizes Carbachol-induced contractions. (R)-Oxybutynin hydrochloride can be used for researching incontinence due to neurogenic bladder dysfunction . (R)-Oxybutynin (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-117583
-
|
|
HDAC
Histone Methyltransferase
|
Neurological Disease
|
|
cis-BG47 is an cis-isomer of BG47, BG47 is a prototypical histone deacetylases HDAC1 and HDAC2 selective, optoepigenetic probe. BG47 can bind to and competitively inhibits the deacetylase activity of HDAC targets upon a light-induced trans-to-cis isomerization, and increases Histone Methyltransferase H3K9 acetylation. cis-BG47 can be used for neurological disease research .
|
-
- HY-155108
-
|
|
Arginase
|
Cancer
|
|
OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and 2. OATD-02 is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 abolishes tumor immunosuppression induced by both arginases. OATD-02 can be used for melanoma study .
|
-
- HY-124267
-
|
SOMG-833
|
c-Met/HGFR
|
Cancer
|
|
Zgwatinib (SOMG-833) is a potent, selective, and ATP-competitive c-MET inhibitor, with an IC50 of 0.93 nM against c-MET, over 10,000-fold more potent compared with 19 tyrosine kinases (including c-MET family members and highly homologous kinases). Zgwatinib potently inhibits c-MET-driven cell proliferation. Zgwatinib as a potential candidate agent for c-MET-driven human cancers research .
|
-
- HY-13011R
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Alectinib (Standard) is the analytical standard of Alectinib. This product is intended for research and analytical applications. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
|
-
- HY-15656R
-
|
|
Anaplastic lymphoma kinase (ALK)
Insulin Receptor
IGF-1R
|
Endocrinology
Cancer
|
|
Ceritinib (Standard) is the analytical standard of Ceritinib. This product is intended for research and analytical applications. Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency .
|
-
- HY-117809
-
|
|
PDK-1
|
Cancer
|
|
PDK1-IN-2 is a small molecule inhibitor of 3-phosphoinositol-dependent protein kinase-1 (PDK1). PDK1-IN-2 inhibits the binding of PDK1 to its substrate by competitively binding to the PIF pocket of PDK1, thereby inhibiting the kinase activity and downstream signaling of PDK1. PDK1-IN-2 can be used for cell survival and proliferation in cancer .
|
-
- HY-117005
-
|
|
Bacterial
|
Infection
|
|
C450-0730 is an antagonist targeting the AHL membrane-bound sensor kinase and is an antagonist of the nine-transmembrane protein LuxN of Vibrio harveyi . C450-0730 competitively binds to the LuxN AI-1 binding site and specifically antagonizes the LuxN/AI-1 quorum sensing signal in Vibrio harveyi. The inhibitory activity of C450-0730 against LuxN I209F was not significant .
|
-
- HY-76474A
-
|
|
Apoptosis
Syk
|
Inflammation/Immunology
Cancer
|
|
BAY 61-3606 hydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 hydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 hydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates. BAY 61-3606 hydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
|
-
- HY-115827
-
|
|
Others
|
Others
|
|
AH22921 is an EP4 prostaglandin receptor antagonist with the activity of antagonizing the activation of adenylate cyclase by prostaglandins in CHO cells. AH22921 can shift the PGE2 concentration-response curve to the right in CHO cells. It is a non-competitive antagonist that is selective for EP4 receptors and has an antagonistic effect on EP4 receptors in CHO cells, but does not affect the PGE2 concentration-response curve in NPE cells containing EP2 receptors.
|
-
- HY-N12109
-
|
|
Others
|
Others
|
|
Albizziin is an amino acid analog with activity as a competitive inhibitor of asparagine synthetase. Albizziin has been used to isolate Chinese hamster ovary cell mutants with altered levels of the target enzyme. Several mutational classes of albizziin can be distinguished based on cross-resistance to β-aspartic hydroxamic acid. Studies on asparagine synthetase have shown that resistance to albizziin may be associated with altered regulation of asparagine synthetase, structural mutations of the enzyme, and gene amplification .
|
-
- HY-10780
-
|
|
Others
|
Cardiovascular Disease
|
|
JTV-803 mesylate is a human factor Xa inhibitor with oral anticoagulant activity. JTV-803 exhibits competitive inhibition of human factor Xa, with a Ki value of 0.019μM and IC50Value is 0.081μM. JTV-803 is 100 times more selective at inhibiting human factor Xa than its comparator. JTV-803 is an effective oral anticoagulant for the prevention of thrombosis .
|
-
- HY-118061
-
|
|
Others
|
Infection
|
|
VCC234718 is a molecule with mycobacterial growth inhibitory activity, specifically targeting Mycobacterium tuberculosis (Mtb). The primary molecular target of VCC234718 is inosine monophosphate dehydrogenase (GuaB2), and it inhibits the growth of Mtb by affecting the function of this enzyme. VCC234718 inhibits GuaB2 with a K value of 100 nM and exhibits non-competitive inhibition with IMP and NAD+. VCC234718 exerts its inhibitory effect by directly interacting with IMP and binding at the NAD+ site .
|
-
- HY-167920
-
|
S-Sulfoglutathione
|
Others
|
Cancer
|
|
Glutathione sulfonate (S-Sulfoglutathione) is a multifunctional bioactive compound that inhibits angiogenesis and tumor growth. Glutathione sulfonate is a competitive inhibitor of glutathione S-transferase and is involved in the detoxification process and the binding of a variety of exogenous and endogenous compounds. Glutathione sulfonate acts in the substrate binding site of Escherichia coli glutathione S-transferase, affecting the catalytic mechanism. The structural characteristics of Glutathione sulfonate contribute to its inhibitory effect by hydrogen bonding in the active center of the enzyme .
|
-
- HY-76474
-
|
|
Syk
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
|
-
- HY-14985
-
|
|
Syk
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM . BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
|
-
- HY-11108
-
|
|
Syk
FLT3
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 free base reduces immune complex-mediated inflammation . R406 free base also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-13260
-
|
|
Akt
Autophagy
Apoptosis
|
Cancer
|
|
CCT128930 is a ATP-competitive and selective inhibitor of AKT (IC50=6 nM for AKT2). CCT128930 has 28-fold selectivity over the closely related PKA kinase (IC50=168 nM) through the targeting of Met282 of AKT (Met173 of PKA-AKT chimera), as well as 20-fold selectivity over p70S6K (IC50=120 nM). Antitumor activity.
|
-
- HY-15186
-
|
GDC-0068; RG7440
|
Organoid
Akt
Apoptosis
|
Cancer
|
|
Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
|
-
- HY-13285
-
|
Debio 0719
|
LPL Receptor
|
Neurological Disease
Cancer
|
|
Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with Kis of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK . Ki16425 can also inhibit LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells .
|
-
- HY-15893
-
|
Dimethyloxallyl Glycine
|
HIF/HIF Prolyl-Hydroxylase
Autophagy
|
Cancer
|
|
DMOG (Dimethyloxallyl Glycine) is a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo . DMOG is an α-ketoglutarate analogue and inhibits α-KG-dependent hydroxylases. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal . DMOG induces cell autophagy .
|
-
- HY-B0442
-
|
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-B0442A
-
|
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-16993
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
OICR-9429 is high affinity WD repeat domain 5 (WDR5) inhibitor, competitively blocks WDR5 interaction with MLL protein via binding the central peptide-binding pocket of WDR5. OICR-9429 can suppress histone H3K4 trimethylation and can be used for the research of various cancers including non-MLL-rearranged leukaemia, colon, pancreatic, prostate cancer and bladder cancer (BCa) .
|
-
- HY-18346
-
|
OPC-31260
|
Vasopressin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment .
|
-
- HY-103712A
-
|
CT7001 hydrochloride; ICEC0942 hydrochloride
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects .
|
-
- HY-W015309
-
|
|
iGluR
Tyrosinase
c-Met/HGFR
Glutaminase
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .
|
-
- HY-110322A
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
PPTN is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. PPTN exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. Anti-inflammatory and immune activity .
|
-
- HY-B0091S
-
|
|
RAR/RXR
Autophagy
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Adapalene-d3 is the deuterium labeled Adapalene. Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity[1][2][3].
|
-
- HY-50878S
-
|
PF-02341066-d5
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
|
-
- HY-114263
-
NXT629
3 Publications Verification
|
PPAR
|
Cancer
|
|
NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively . NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models .
|
-
- HY-P0097A
-
|
Melanostatine-5 acetate salt
|
Melanocortin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Nonapeptide-1 (Melanostatine-5) acetate salt, a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 acetate salt is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 acetate salt inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer .
|
-
- HY-101283
-
HCH6-1
3 Publications Verification
|
Formyl Peptide Receptor (FPR)
|
Inflammation/Immunology
|
|
HCH6-1 is a potent and competitive dipeptide antagonist of Formyl peptide receptor 1 (FPR1). HCH6-1 inhibits chemotaxis, superoxide anion generation, and elastase release in human neutrophils specifically activated by fMLF (an FPR1 agonist). HCH6-1 has protective effects against acute lung injury (ALI) in vivo and can be used for the research of FPR1-involved inflammatory lung diseases .
|
-
- HY-100671
-
|
|
Histone Acetyltransferase
STAT
|
Inflammation/Immunology
Cancer
|
|
L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an?IC50?of 1.98 μM . L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation . L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment .
|
-
- HY-101193
-
|
Zn(II)-protoporphyrin IX; ZnPP; Zinc Protoporphyrin-9
|
Reactive Oxygen Species
Endogenous Metabolite
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is an orally active and competitive heme oxygenase-1 (HO-1) inhibitor and markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2 . Zinc Protoporphyrin is used as a screening marker of iron deficiency in individual pregnant women and children, but also to assess population iron status in combination with haemoglobin concentration . Zinc Protoporphyrin has anti-cancer activity .
|
-
- HY-N1483
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes . Guanfu base A also inhibits HERG channel current .
|
-
- HY-13531
-
|
|
PI3K
|
Cancer
|
|
AS-604850 is a potent, selective and ATP-competitive PI3Kγ inhibitor with an IC50 value of 0.25 μM and a Ki value of 0.18 μM. AS-604850 shows isoform selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18-fold selectivity over PI3Kα, respectively .
|
-
- HY-19269
-
|
|
Elastase
|
Inflammation/Immunology
|
|
FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect .
|
-
- HY-14664C
-
|
(3S,5R)-XU 62-320
|
HMG-CoA Reductase (HMGCR)
|
Cardiovascular Disease
Cancer
|
|
(3S,5R)-Fluvastatin sodium ((3S,5R)-XU 62-320) is the (3S,5R)-enantiomer of Fluvastatin. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway .
|
-
- HY-124745
-
|
|
MAP4K
Wnt
Apoptosis
|
Cancer
|
|
KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM. KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity .
|
-
- HY-123593
-
|
OPC-31260 hydrochloride
|
Vasopressin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Mozavaptan hydrochloride (OPC-31260 hydrochloride) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan hydrochloride shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan hydrochloride has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment .
|
-
- HY-11052A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ 35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases .
|
-
- HY-131062
-
|
|
Others
|
Metabolic Disease
|
|
yGsy2p-IN-1 is a potent inhibitor for yeast glycogen synthase 2 (yGsy2p). yGsy2p-IN-1 is a competitive human glycogen synthase 1 (hGYS1) inhibitor with an IC50 of 2.75 µM and a Ki of 1.31 µM for wild-type hGYS1. yGsy2p-IN-H23 a pyrazole inhibitor, is used for glycogen storage diseases (GSDs) .
|
-
- HY-117026
-
|
|
Cytochrome P450
|
Metabolic Disease
Inflammation/Immunology
|
|
LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor with an IC50 of 1.7 μM. LKY-047 is inactive against other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A .
|
-
- HY-131339
-
SP-96
1 Publications Verification
|
Aurora Kinase
|
Cancer
|
|
SP-96 is a highly potent, selective and non-ATP-competitive Aurora B (IC50=0.316 nM) inhibitor and shows >2000 fold selectivity against FLT3 and KIT. SP-96 shows selective growth inhibition in NCI60 screening, incluing MDA-MD-468 (GI50=107 nM). SP-96 can be used for the research of triple negative breast cancer (TNBC) .
|
-
- HY-124828
-
|
|
HuR
|
Cancer
|
|
CMLD-2, an inhibitor of HuR-ARE interaction, competitively binds HuR protein disrupting its interaction with adenine-uridine rich elements (ARE)-containing mRNAs (Ki=350 nM). CMLD-2 induces apoptosis exhibits antitumor activity in different cancer cells as colon, pancreatic, thyroid and lung cancer cell lines. Hu antigen R (HuR) is an RNA binding protein, can regulate target mRNAs stability and translation .
|
-
- HY-119366
-
|
|
ROR
|
Inflammation/Immunology
|
|
S18-000003 is a potent, selective and orally active inhibitor of retinoic acid receptor-related orphan receptor-gamma-t (RORγt), with an IC50 of <30 nM towards human RORγt in competitive binding assays. S18-000003 shows selectivity for RORγt over other ROR family members (IC50>10 μM). S18-000003 can be used for the research of psoriasis with low risk of thymic aberrations .
|
-
- HY-110322
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
PPTN hydrochloride is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. PPTN hydrochloride exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. Anti-inflammatory and anti-immune activity .
|
-
- HY-103712B
-
|
CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride hydrate has anti-tumor effects .
|
-
- HY-100979
-
|
HDMPPA
|
mAChR
|
Others
|
|
W-84 (dibromide) is a potent allosteric modulator of M2-cholinoceptors, which retards [ 3H]N-methylscopolamine dissociation. W-84 dibromide can stabilize cholinergic antagonist-receptor complexes. W-84 (dibromide) is a non-competitive muscarinic acetylcholine receptors antagonist with allosteric effects. W-84 (dibromide) protects over additively against an organophosphate-intoxication when applied in combination with atropine .
|
-
- HY-103712
-
|
CT7001; ICEC0942
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib (CT7001) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib has anti-tumor effects .
|
-
- HY-15496
-
|
ER-806201
|
MEK
FLT3
|
Cancer
|
|
E6201 (ER-806201) is an ATP-competitive dual kinase inhibitor of MEK1 and FLT3. E6201 inhibits MEK1- induced ERK2 phosphorylation with an IC50 value of 5.2 nM, MKK4-induced JNK phosphorylation with an IC50 value of 91 nM, and MKK6-induced p38 MAPK phosphorylation with an IC50 value of 19 nM. Anti-tumor and anti-psoriasis efficacy .
|
-
- HY-100813
-
|
|
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Saclofen is an orally available competitive GABAB receptor antagonist with an IC50 of 7.8 μM, but it has a weaker antagonistic effect on GABAB1b and GABAB2 heterodimer recombinant receptors. Saclofen can inhibit the binding of baclofen (HY-B007) to rat cerebellar membranes and block the phase shifts in circadian rhythms caused by baclofen. Saclofen has also shown anti-inflammatory and analgesic effects in rats .
|
-
- HY-B0236S1
-
|
EACA-d10; Epsilon-Amino-n-caproic Acid-d10; 6-Aminohexanoic acid-d10
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
|
6-Aminocaproic acid-d10 is the deuterium labeled 6-Aminocaproic acid. 6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders[1][2].
|
-
- HY-144636
-
|
|
Atg4
Cathepsin
Phospholipase
Autophagy
|
Cancer
|
|
Atg4B-IN-2 is a potent competitive Atg4B inhibitor with Ki value of 3.1 μM, also possesses declining PLA2 inhibitory potency, IC50s of 11 μM and 3.5 μM for Atg4B and PLA2, respectively. Atg4B-IN-2 enhances the anticancer activity of anti-castration-resistant prostate cancer agents via autophagy inhibition .
|
-
- HY-W107464
-
G6PDi-1
2 Publications Verification
|
PDI
|
Metabolic Disease
Inflammation/Immunology
|
|
G6PDi-1 is a reversible and non-competitive glucose-6-phosphate dehydrogenase (G6PD) inhibitor with an IC50 of 0.07 μM for human G6PD. G6PDi-1 depletes NADPH most strongly in lymphocytes. G6PDi-1 markedly decreases inflammatory cytokine production in T cells .
|
-
- HY-13635S
-
|
MK-906-d9
|
Isotope-Labeled Compounds
5 alpha Reductase
|
Cancer
|
|
Finasteride-d9 is deuterium labeled Finasteride. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia[1][2][3].
|
-
- HY-B0236S
-
|
EACA-d6; Epsilon-Amino-n-caproic acid-d6; 6-Aminohexanoic acid-d6
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
|
6-Aminocaproic acid-d6 is deuterium labeled 6-Aminocaproic acid. 6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders[1][2].
|
-
- HY-B0368S
-
|
SQ 14225-d3
|
Isotope-Labeled Compounds
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Captopril-d3 is deuterium labeled Captopril. Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM[1][2][3].
|
-
- HY-B0442S
-
|
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
Endocrinology
|
|
Vardenafil-d5 is deuterium labeled Vardenafil. Vardenafil is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction[1][2].
|
-
- HY-146332
-
|
|
Others
|
Cardiovascular Disease
|
|
Collagen-IN-1 (compound 3), an ortho-carbonyl hydroquinone derivative, is a selective inhibitor on collagen. Collagen-IN-1 inhibits agonist-induced platelet aggregation in a non-competitive manner with an IC50 value of 1.77 μM. Collagen-IN-1 reduces the expression of P-selectin, activation of glycoprotein IIb/IIIa, and release of adenosine triphosphate and CD63 from platelet. Collagen-IN-1 has the potential for platelet-related thrombosis diseases research .
|
-
- HY-103712C
-
|
CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride hydrate has anti-tumor effects .
|
-
- HY-17395B
-
|
TDT 067 lactate
|
Antibiotic
Fungal
Bacterial
|
Infection
|
|
Terbinafine lactate (TDT 067 lactate) is an orally active and potent antifungal agent. Terbinafine lactate is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a Ki of 30 nM. Terbinafine lactate also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria . Terbinafine (lactate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-100707
-
|
|
DNA-PK
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
IC 86621 is a potent DNA-dependent protein kinase (DNA-PK) inhibitor, with an IC50 of 120 nM. IC 86621 also acts as a selective and reversible ATP-competitive inhibitor.IC 86621 inhibits DNA-PK mediated cellular DNA double-strand break (DSB) repair (EC50=68 µM). IC 86621 increases DSB-induced antitumor activity without cytotoxic effects. IC 86621 can protects rheumatoid arthritis (RA) T cells from apoptosis .
|
-
- HY-P0097
-
|
Melanostatine-5
|
Melanocortin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Nonapeptide-1 (Melanostatine-5), a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer .
|
-
- HY-B0442C
-
|
|
Endogenous Metabolite
Phosphodiesterase (PDE)
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes - .
|
-
- HY-143287
-
|
|
NTPDase
|
Infection
Inflammation/Immunology
Cancer
|
|
NTPDase-IN-1 (compound 5a) is a selective NTPDase inhibitor with IC50s of 0.05, 0.23 and 0.54 µM for h-NTPDase-1/-2/-8, respectively. NTPDase-IN-1 non-competitively inhibits h-NTPDase-1/-2 with a Km of 21 µM for h-NTPDase-1. NTPDase-IN-1 can be used in studies of cancer, immunologic disorders as well as bacterial infections .
|
-
- HY-B1324A
-
|
Ro 13-8996 free base
|
Fungal
Cytochrome P450
Antibiotic
|
Infection
Cancer
|
|
Oxiconazole (Ro 13-8996) is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest .
|
-
- HY-148396
-
|
|
DNA/RNA Synthesis
|
Infection
Cancer
|
|
UCK2 Inhibitor-3 is a non-competitive inhibitor of uridine-cytidine kinase 2 (UCK2, a pyrimidine salvage enzyme) with an IC50 value of 16.6 μM. UCK2 can replace dihydroorotate dehydrogenase (DHODH), in a certain extent, in infected or rapidly dividing cells to continue efficient uridine salvage. UCK2 Inhibitor-3 also inhibits DNA polymerase eta and kappa with IC50s of 56 μM and 16 μM .
|
-
- HY-B1126S
-
|
|
iGluR
|
Neurological Disease
|
|
Orphenadrine-d3 (hydrochloride) is the deuterium labeled Orphenadrine hydrochloride[1]. Orphenadrine hydrochloride is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine hydrochloride relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine hydrochloride is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases[2][3].
|
-
- HY-149300
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
SB-1436 is an Cholinesterase (ChE) inhibitor, inhibits acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and recombinant human acetylcholinesterase (rHuAChE) with IC50s of 0.176, 0.37 and 0.08 μM, respectively. SB-1436 inhibits AChE and BChE in a non-competitive manner with Kis of 0.046 and 0.115 μM, respectively. SB-1436 significantly stops the self-aggregation of Aβ, and can be used for neurological disease research .
|
-
- HY-13699
-
|
|
GnRH Receptor
PERK
|
Others
|
|
NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca 2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases .
|
-
- HY-149354
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora Kinases-IN-4 (Compound 11c) is a covalent and ATP competitive aurora kinase A inhibitor (IC50: 1.7 nM). Aurora Kinases-IN-4 inhibits cell proliferation in SJSA-1, MDA-MB-231, A54, HeLa cells with IC50s of 4.27, 1.54, 3.08, 6.99 μM. Aurora Kinases-IN-4 can be used for research of triple negative breast cancer (TNBC) .
|
-
- HY-P5455
-
|
|
LIM Kinase (LIMK)
|
Others
|
|
S3 Fragment is a biological active peptide. (This peptide contains the unique amino-terminal phosphorylation site of Xenopus ADF/cofilin, the LIM kinase (LIMK) phosphorylation site. LIMK1 is a key regulator of the actin cytoskeleton through its phosphorylation of ADF/cofilin at serine-3 for inactivation. This peptide is a fragment of the S3 peptide containing the serine-3 sequence of ADF/cofilin that has been widely used as an effective competitive inhibitor of LIMK1.)
|
-
- HY-19989
-
|
L-660711
|
Leukotriene Receptor
LPL Receptor
|
Inflammation/Immunology
|
|
MK-571 (L-660711) is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release .
|
-
- HY-155231
-
|
|
Elastase
|
Cancer
|
|
Neutrophil elastase inhibitor 4 (compound 4f) is a competitive human neutrophil elastase (HNE) inhibitor (IC50: 42.30 nM, Ki: 8.04 nM). Neutrophil elastase inhibitor 4 induces T47D cell apoptosis. Neutrophil elastase inhibitor 4 inhibits cell proliferation with IC50s of 21.25, 34.17, 29.93, 99.11 nM for T47D, RPMI 8226, A549, and HSF cells .
|
-
- HY-P5894
-
|
Galanin-like peptide (3-32)
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
human GALP (3-32) (Galanin-like peptide (3-32)) is a potent galanin receptor agonist with high affinity for both GalR1 (IC50=33 nM) and GalR2 (IC50=15 nM) in a competitive binding study. human GALP (3-32) exhibits the high potency in altering the extracellular acidification rate of SH-SY5Y cells transfected with GalR2 (EC50=360 nM) .
|
-
- HY-13635R
-
|
MK-906 (Standard)
|
5 alpha Reductase
|
Cancer
|
|
Finasteride (Standard) is the analytical standard of Finasteride. This product is intended for research and analytical applications. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia .
|
-
- HY-B0091R
-
|
CD271 (Standard)
|
RAR/RXR
Autophagy
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Adapalene (Standard) is the analytical standard of Adapalene. This product is intended for research and analytical applications. Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity .
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-
- HY-W010410S
-
|
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
|
Oct-1-en-3-ol-d3 is deuterated labeled Linalool (HY-N0368). Linalool is a natural monoterpene which is a competitive NMDA receptor antagonist. Linalool is orally active and crosses the blood-brain barrier. Linalool has anticancer, antibacterial, anti-inflammatory, neuroprotective, anxiolytic, antidepressant, anti-stress, cardioprotective, hepatoprotective, nephroprotective and pulmonary protective activities .
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-
- HY-162390
-
|
|
Amylases
Glucosidase
|
Endocrinology
|
|
α-Amylase/α-Glucosidase-IN-11 (Compound 5d) is a isoxazolidine-isatin hybrid with significant antidiabetic activity. α-Amylase/α-Glucosidase-IN-11 competitively inhibits α-amylase (IC50 = 30.39 μM) and α-glucosidase (IC50 = 65.1 μM), two key digestive enzymes. α-Amylase/α-Glucosidase-IN-11 does not cross the blood-brain barrier .
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-
- HY-10181R
-
|
|
Bcr-Abl
Src
Autophagy
Apoptosis
|
Cancer
|
|
Dasatinib (Standard) is the analytical standard of Dasatinib. This product is intended for research and analytical applications. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
|
-
- HY-13588R
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Cefsulodin (sodium) (Standard) is the analytical standard of Cefsulodin (sodium). This product is intended for research and analytical applications. Cefsulodin (SCE-129) sodium is a third generation β lactam antibiotic and member of the cephems subgroup of antibiotics. Cefsulodin sodium inhibits cell wall synthesis by competitively inhibiting penicillin binding protein (PBP) cross-linking and transpeptidation of peptidogly. Cefsulodin sodium is a potent tyrosine phosphatase inhibitor against mPTPB, a virulent phosphatase from Mycobacterium tuberculosis, with an IC50 value of 16 μM .
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-
- HY-B0113R
-
|
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole (Standard) is the analytical standard of Omeprazole. This product is intended for research and analytical applications. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
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-
- HY-B0379AR
-
|
|
nAChR
|
Neurological Disease
|
|
Adiphenine (hydrochloride) (Standard) is the analytical standard of Adiphenine (hydrochloride). This product is intended for research and analytical applications. Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 μM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has anticonvulsant effects .
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-
- HY-B1205AR
-
|
|
mAChR
|
Cardiovascular Disease
Neurological Disease
|
|
Atropine (sulfate) (Standard) is the analytical standard of Atropine (sulfate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate can be used for research of anti-myopia and bradycardia .
|
-
- HY-N0063R
-
|
|
SARS-CoV
HBV
|
Infection
Metabolic Disease
Cancer
|
|
Punicalagin (Standard) is the analytical standard of Punicalagin. This product is intended for research and analytical applications. Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a reversible and non-competitive 3CLpro inhibitor and inhibits SARS-CoV-2 replication in vitro. Punicalagin is an anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects. Punicalagin has the potential for the research of COVID-19 .
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-
- HY-W008364R
-
|
|
Cytochrome P450
Cannabinoid Receptor
|
Neurological Disease
|
|
Olivetol (Standard) is the analytical standard of Olivetol. This product is intended for research and analytical applications. Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2 . Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively .
|
-
- HY-12542R
-
|
|
Calcium Channel
Autophagy
|
Neurological Disease
Inflammation/Immunology
|
|
Dantrolene (Standard) is the analytical standard of Dantrolene. This product is intended for research and analytical applications. Dantrolene is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene is a ryanodine receptor (RyR) antagonist and Ca2+ signaling stabilizer. Dantrolene is a direct-acting skeletal muscle relaxant. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome .
|
-
- HY-B0394R
-
|
|
mAChR
|
Cardiovascular Disease
Neurological Disease
|
|
Atropine (sulfate monohydrate) (Standard) is the analytical standard of Atropine (sulfate monohydrate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .
|
-
- HY-113695
-
|
|
Angiotensin-converting Enzyme (ACE)
Adrenergic Receptor
|
Cardiovascular Disease
|
|
BW A575C is a dual inhibitor against angiotensin converting enzyme (ACE) and β-adrenoceptor. BW A575C produces a competitive blockade of Isoprenaline (HY-108353)-induced tachycardia in a guinea-pig right atrial. BW A575C also inhibits Angiotensin I (HY-P1032)-induced pressor responses in rats. BW A575C is promising for research of hypertensive diseases .
|
-
- HY-117053
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
ZM 253270 is a species-selective non-peptide NK-2 receptor (NK-2R) antagonist. ZM 253270 competitively inhibits the binding of [ 3H]NKA to native or cloned NK-2R from hamster bladder (Ki=2 nM), but has a weaker inhibitory effect (48-fold) on the binding of [ 3H]NKA to cloned human NK-2R .
|
-
- HY-135111R
-
|
|
Drug Metabolite
|
Infection
Metabolic Disease
Cancer
|
|
4-Desmethoxy Omeprazole (Standard) is the analytical standard of 4-Desmethoxy Omeprazole. This product is intended for research and analytical applications. 4-Desmethoxy Omeprazole is the active metabolite of Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .
|
-
- HY-13716R
-
|
|
Opioid Receptor
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Noscapine (Standard) is the analytical standard of Noscapine. This product is intended for research and analytical applications. Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier [4] .
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-
- HY-15186C
-
|
GDC-0068 tosylate; RG7440 tosylate
|
Organoid
Akt
Apoptosis
|
Cancer
|
|
Ipatasertib (GDC-0068) tosylate is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib tosylate synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib tosylate also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
|
-
- HY-13072B
-
|
AS-703569 benzoate; R-763 benzoate
|
Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
|
Cancer
|
|
Cenisertib (AS-703569) benzoate is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib benzoate induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib benzoate inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
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-
- HY-103055
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
PPTN mesylate is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. PPTN mesylate exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. Anti-inflammatory and immune activity .
|
-
- HY-101676
-
|
NID 525
|
Leukotriene Receptor
PPAR
Cytochrome P450
|
Metabolic Disease
|
|
RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 µM.
|
-
- HY-50878A
-
|
PF-02341066 hydrochloride
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
|
-
- HY-16569
-
|
|
Microtubule/Tubulin
NOD-like Receptor (NLR)
Autophagy
Apoptosis
|
Cancer
|
|
Colchicine, an orally active alkaloid, is a potent tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs). Colchicine prevents non-steroidal anti-inflammatory drug (NSAID)-induced small intestinal injury by inhibiting activation of the NLRP3 inflammasome. Colchicine has extensive anti-inflammatory, immunosuppressive and strong anti-fibrosis effects and has the potential for gouty arthritis research .
|
-
- HY-N0142
-
|
NSC 407292; RJC 02792
|
SGLT
Endogenous Metabolite
GLUT
|
Metabolic Disease
Cancer
|
|
Phloretin (NSC 407292; RJC 02792) is a flavonoid extracted from Malus pumila Mill., has anti-inflammatory activities. Phloridzin is a specific, competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). Phloretin inhibits Yeast-made GLUT1 as well as Human erythrocyte GLUT1 with IC50values of 49 μM and 61 μM, respectively .Phloretin has the potential for the treatment of rheumatoid arthritis (RA) and allergic airway inflammation .
|
-
- HY-17504A
-
|
ZD 4522
|
HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
Bacterial
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-N0215
-
|
Phenylalanine
|
Calcium Channel
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca + channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals .
|
-
- HY-N0235
-
|
(S)-(+)-Bakuchiol
|
Carboxylesterase
p38 MAPK
Autophagy
UGT
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Bakuchiol is a phytoestrogen that can be obtained from psoralen seeds. Bakuchiol has been proven to be a non-competitive inhibitor of multiple enzymes, including UDP-glucuronosyltransferase 2B7 (UGT2B7) and human carboxylesterase 2 (hCE2) , with IC50s values of 40.9 μM and 7.28 μM, respectively. Bakuchiol exhibits significant research and application potential in areas such as anti-inflammatory , antibacterial , antitumor therapies, as well as drug metabolism regulation.
|
-
- HY-12826
-
|
|
Beta-lactamase
Bcl-2 Family
Bacterial
|
Cancer
|
|
IMB-XH1 is an inhibitor of myeloid cell factor 1 (Mcl-1) . IMB-XH1 is a non-competitive Delhi metallo-β-lactamase (NDM-1) inhibitor. The IC50s of IMB-XH1 against metallo-β-lactamases NDM-1, IMP-4, ImiS and L1 are 0.4637 μM, 3.980 μM, 0.2287 μM and 1.158 μM, respectively .
|
-
- HY-16749
-
|
PLX-3397
|
c-Fms
c-Kit
Apoptosis
|
Cancer
|
|
Pexidartinib (PLX-3397) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib (PLX-3397) exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib (PLX-3397) induces cell apoptosis and has anti-tumor activity .
|
-
- HY-15257
-
|
AFQ056
|
mGluR
|
Neurological Disease
|
|
Mavoglurant (AFQ056) is a potent, selective, non-competitive and orally active mGluR5 antagonist, with an IC50 of 30 nM. Mavoglurant shows a >300 fold selectivity for the mGluR5 over all targets (238) tested. Mavoglurant can be used for the research of Fragile X syndrome (FXS), and L-dopa induced dyskinesias in Parkinson's disease . Mavoglurant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-N1584
-
|
RU-19110
|
DNA/RNA Synthesis
TGF-beta/Smad
Parasite
Sodium Channel
Calcium Channel
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM . Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity . Halofuginone is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
|
-
- HY-101903
-
|
|
FABP
|
Cardiovascular Disease
Metabolic Disease
|
|
BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .
|
-
- HY-B1324
-
|
Ro 13-8996
|
Fungal
Cytochrome P450
Antibiotic
|
Infection
Cancer
|
|
Oxiconazole (Ro 13-8996) nitrate is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole nitrate is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole nitrate exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest .
|
-
- HY-101544
-
|
|
FGFR
|
Cancer
|
|
ARQ 069, an analog of ARQ 523, inhibits FGFR in an enantiospecific manner. ARQ 069 targets the unphosphorylated, inactive forms of FGFR1/FGFR2 kinases (IC50s of 0.84 μM and 1.23 μM, respectively). ARQ 069 inhibits FGFR1/FGFR2 autophosphorylation (IC50s of 2.8 and 1.9 μM, respectively) through a mechanism in a non-ATP competitive dependent manner .
|
-
- HY-B0113S1
-
|
H 16868-d3-1
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole-d3-1 is the deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
|
-
- HY-N0376
-
|
|
Reactive Oxygen Species
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Liquiritin, a flavonoid isolated from Glycyrrhiza uralensis, is a potent and competitive AKR1C1 inhibitor with IC50s of 0.62 μM, 0.61 μM, and 3.72μM for AKR1C1, AKR1C2 and AKR1C3, respectively. Liquiritin efficiently inhibits progesterone metabolism mediated by AKR1C1 in vivo . Liquiritin acts as an antioxidant and has neuroprotective, anti-cancer and anti-inflammatory activity .
|
-
- HY-107691
-
|
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [ 3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects .
|
-
- HY-N2278
-
|
Leachianone E
|
Tyrosinase
Glucosidase
|
Cancer
|
|
Kushenol A (Leachianone E) is isolated from the root of Sophora flavescent. Kushenol A is a non-competitive tyrosinase inhibitor to block the conversion of L-tyrosine to L-DOPA, shows IC50 and Kivalues of 1.1 μM and 0.4 μM, respectively . Kushenol A is a flavonoid antioxidant, has inhibitory effects on alpha-glucosidase (IC50: 45 μM; Ki: 6.8 μM) and β-amylase . Kushenol A is confirmed as potential inhibitors of enzymes targeted by cosmetics for skin whitening and aging .
|
-
- HY-N2071
-
-
- HY-104066
-
|
Xiliertinib; HMPL-309
|
EGFR
|
Cancer
|
|
Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-113914
-
|
Elraglusib
|
GSK-3
Apoptosis
Autophagy
|
Cancer
|
|
9-ING-41 (Elraglusib) is a maleimide-based ATP-competitive and selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 0.71 μM. 9-ING-41 significantly leads to cell cycle arrest, autophagy and apoptosis in cancer cells. 9-ING-41 has anticancer activity and has the potential for enhancing the antitumor effects of chemotherapeutic agents .
|
-
- HY-101925
-
CM-272
3 Publications Verification
|
Histone Methyltransferase
DNA Methyltransferase
Apoptosis
|
Cancer
|
|
CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC50s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death .
|
-
- HY-15425
-
|
Sphingosine Kinase 1 Inhibitor II
|
SphK
LPL Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
PF-543 (Sphingosine Kinase 1 Inhibitor II) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 induces apoptosis, necrosis, and autophagy .
|
-
- HY-15425B
-
|
Sphingosine Kinase 1 Inhibitor II hydrochloride
|
SphK
LPL Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy .
|
-
- HY-107641
-
|
α-Cyano-4-hydroxycinnamate
|
Monocarboxylate Transporter
|
Metabolic Disease
|
|
α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). α-Cyano-4-hydroxycinnamic acid inhibits mitochondrial pyruvate transporter with a Ki of 6.3 μM. α-Cyano-4-hydroxycinnamic acid is used as a matrix to facilitate peptide ionization in matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry applications .
|
-
- HY-18944
-
|
|
CDK
HSV
CMV
DNA/RNA Synthesis
|
Infection
|
|
FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.
|
-
- HY-113038
-
|
(R)-2-Hydroxyglutarate; (R)-2-Hydroxyglutaric acid; (R)-2-Hydroxypentanedioic acid
|
Reactive Oxygen Species
ATP Synthase
mTOR
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
D-α-Hydroxyglutaric acid ((R)-2-Hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid binds and inhibits ATP synthase and inhibits mTOR signaling .
|
-
- HY-P1321
-
|
1229U91; GW1229
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide Y Y6 receptor (pKi= 8.8) .
|
-
- HY-P1321A
-
|
1229U91 TFA; GW1229 TFA
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
GR231118 TFA, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide YY receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide YY4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide Y Y2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide YY6 receptor (pKi= 8.8) .
|
-
- HY-10032
-
|
PF 00477736
|
Checkpoint Kinase (Chk)
VEGFR
Src
c-Fms
Aurora Kinase
FGFR
FLT3
RET
CDK
|
Cancer
|
|
PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo .
|
-
- HY-100195
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer agents .
|
-
- HY-101903A
-
|
|
FABP
|
Cardiovascular Disease
Metabolic Disease
|
|
BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .
|
-
- HY-17623
-
|
CJ-12420; RQ-00000004
|
Proton Pump
Potassium Channel
Na+/K+ ATPase
|
Inflammation/Immunology
|
Tegoprazan (CJ-12420), a potassium-competitive acid blocker, is a reversible, orally active and highly selective inhibitor of gastric H +/K +-ATPase. Tegoprazan inhibits gastric acid secretion and motility against porcine, canine and human H +/K +-ATPase with IC50 values ranging from 0.29-0.52 μM in vitro. Tegoprazan significantly improves colitis and enhances the intestinal epithelial barrier function in mice. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases .
|
-
- HY-141539
-
|
|
Histone Methyltransferase
|
Cancer
|
|
SETDB1-TTD-IN-1 is a potent, selective and endogenous binder competitive ligand of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD) that binds to TTD, with a Kd of 88 nM. SETDB1-TTD-IN-1 increases SETDB1 methyltransferase activity. SETDB1-TTD-IN-1 can be used for the research of biological functions and disease associations of SETDB1-TTD .
|
-
- HY-108907
-
|
|
Casein Kinase
|
Cancer
|
|
SR-1277 is a potent, selective and ATP competitive CK1δ/ε inhibitor, with IC50s of 49 nM and 260 nM, respectively. SR-1277 also inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9/cyclin K, with IC50s of 305 nM, 1340 nM, 311 nM and 109 nM, respectively. SR-1277 can be used for the research of cancer .
|
-
- HY-N0215S6
-
|
2-Amino-3-phenylpropionic acid-d5 hydrochloride
|
Isotope-Labeled Compounds
Calcium Channel
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
DL-Phenylalanine-d5 (hydrochloride) is the deuterium labeled DL-Phenylalanine hydrochloride. L-Phenylalanine hydrochloride is an essential amino acid isolated from Escherichia coli. L-Phenylalanine hydrochloride is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine hydrochloride is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine hydrochloride is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
|
-
- HY-116216
-
|
|
Bombesin Receptor
|
Cancer
|
|
PD 168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with the Ki of 15–45 nM . PD 168368 is neuromedin B receptor (NMBR; IC50=96 nM) / gastrin-releasing peptide receptor (GRPR IC50=3500 nM) antagonist . PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC50s of 0.57, 0.24, and 2.7 nM, respectively .
|
-
- HY-125102
-
|
|
IGF-1R
|
Cancer
|
|
AZ12253801 is an ATP-competitive IGF-1R tyrosine kinase inhibitor that shows ∼10-fold selectivity over the insulin receptor. AZ12253801 inhibits IGF-1R–driven proliferation in 3T3 mouse fibroblasts (transfected with human IGF-1R) with an IC50 of 17 nmol/L. The IC50 for epidermal growth factor receptor (EGFR)–driven proliferation is 440 nmol/L. Anti-tumor activity.
|
-
- HY-A0009S
-
|
Galantamine-d3 hydrobromide
|
Isotope-Labeled Compounds
Cholinesterase (ChE)
nAChR
|
Neurological Disease
|
|
Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD)[1][2][3].
|
-
- HY-124569
-
|
|
iGluR
|
Neurological Disease
|
|
NAB-14 is a potent, selective, orally active and non-competitive GluN2C/2D antagonists with an IC50 of 580 nM for GluN1/GluN2D. NAB-14 shows >800-fold selective for recombinant GluN2C and GluN2D over GluN2A and GluN2B. NAB-14 can cross the blood-brain-barrier .
|
-
- HY-B0442B
-
|
|
Endogenous Metabolite
Phosphodiesterase (PDE)
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-108662
-
|
2,2'-Pyridylisatogen tosylate
|
P2Y Receptor
|
Inflammation/Immunology
|
|
PIT (2,2'-Pyridylisatogen tosylate) is a selective and non-competitive antagonist of P2Y1 receptor with an IC50 value of 0.14 μM for human P2Y1 receptor. PIT antagonizes P2Y1 receptor signaling without affecting nucleotide binding. PIT is an irreversible antagonist of responses to ATP at metabotropic purinoceptors (of the P2Y family) in some smooth muscles. PIT can be used for the research of chronic bronchitis and asthma .
|
-
- HY-104066A
-
|
Xiliertinib tartrate; HMPL-309 tartrate
|
EGFR
|
Cancer
|
|
Theliatinib (Xiliertinib) tartrate is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib (tartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-P4160
-
|
THG113.31; ILGHXDYK
|
Prostaglandin Receptor
|
Endocrinology
|
|
PDC31 (THG113.31; ILGHXDYK) is an allosteric and non-competitive inhibitor of FP Prostaglandin Receptor. PDC31 is the D-amino acid-based oligopeptide, is used for smooth muscle contractile agent. PDC31 decreases the strength and duration of uterine contractions in vivo, which can be used for research of preterm labor and primary dysmenorrhea (PD). PDC31 also enhances Ca 2+-dependent large-conductance K +-channel in human myometrial cells .
|
-
- HY-139577A
-
|
MB-1018972 trihydrochloride; IMB-101 trihydrochloride
|
Mitochondrial Metabolism
|
Cardiovascular Disease
Metabolic Disease
|
|
Ninerafaxstat trihydrochloride (IMB-1018972 trihydrochloride) is the trihydrochloride salt form of Ninerafaxstat (HY-139577). Ninerafaxstat trihydrochloride is a novel orally active cardiac mitochondrial drug that restores myocardial energy homeostasis. Ninerafaxstat trihydrochloride competitively inhibits 3-ketoacyl-CoA thiolase (3-KAT) to partially suppress fatty acid oxidation, and shifts cardiac energy metabolism from free fatty acid oxidation to glucose oxidation, regulating myocardial substrate utilization and thereby improving cardiac efficiency. Ninerafaxstat trihydrochloride can be used for research on cardiovascular diseases .
|
-
- HY-17504R
-
|
Rosuvastatin hemicalcium (Standard); ZD 4522 Calcium (Standard)
|
HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
Bacterial
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Rosuvastatin (Calcium) (Standard) is the analytical standard of Rosuvastatin (Calcium). This product is intended for research and analytical applications. Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Calcium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-153896
-
|
|
c-Met/HGFR
|
Cancer
|
|
LMTK3-IN-1 (compound C28) is an ATP-competitive inhibitor of lemur tyrosine kinase 3 (LMTK3) (Kd=2.5 μM)，that acts by degrading LMTK3 via the ubiquitin-proteasome pathway. LMTK3-IN-1 shows anticancer activity in a variety of cancer cell lines and in vivo BC mouse models. LMTK3-IN-1 induces apoptosis in BC cell lines at 10-20 μM .
|
-
- HY-14664F
-
|
(3R,5S)-XU 62-320
|
HMG-CoA Reductase (HMGCR)
Autophagy
|
Cancer
|
|
(3R,5S)-Fluvastatin ((3R,5S)-XU 62-320) sodium is the 3R,5S-isomer Fluvastatin. Fluvastatin (XU 62-320 free acid) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway .
|
-
- HY-P5756
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CSD-CH2(1,8)-NH2 is a selective and competitive KOR antagonist (Ki: 6.8 nM). CSD-CH2(1,8)-NH2 inhibits calcium mobilization in DRG neurons. CH2(1,8)-NH2 antagonizes the antinociceptive effect of U50,488. CSD-CH2(1,8)-NH2 can be used for research of neuropsychiatric disorders .
|
-
- HY-19858
-
|
|
iGluR
|
Neurological Disease
|
|
LY-466195 is a selective and competitive GLUK5 receptor antagonist. LY-466195 antagonizes Kainate-induced currents with an IC50 value of 0.045 μM in rat dorsal root ganglion neurons. In HEK293 cells transfected with GLUK5, GLUK2/GLUK5, or GLUK5/GLUK66 receptors, LY466195 produces IC50 values of 0.08 μM, 0.34 μM, and 0.07 μM, respectively .
|
-
- HY-116143
-
|
|
MAGL
|
Metabolic Disease
|
|
SAR127303 is an orally active, selective, competitive monoacylglycerol lipase (MAGL) covalent inhibitor with IC50s of 3.8 nM and 29 nM for mouse and human MAGL, respectively. SAR127303 potently elevates hippocampal levels of 2-AG in mice. SAR127303 decreased long term potentiation (LTP) of CA1 synaptic transmission and acetylcholine release in the hippocampus. SAR127303 produces antinociceptive effects in assays of inflammatory and visceral pain. SAR127303 slows down epileptogenesis .
|
-
- HY-162036
-
|
|
Glucosidase
Amylases
Cholinesterase (ChE)
|
Neurological Disease
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-7 (Compound 3f) is a competitive α-glucosidase and α-amylase enzyme inhibitor with IC50 values of 18.52 and 20.25 µM, respectively. α-Amylase/α-Glucosidase-IN-7 can also effectively inhibit AChE and BChE, with IC50 values of 9.25 and 10.06 µM respectively. α-Amylase/α-Glucosidase-IN-7 can be used in diabetes and Alzheimer’s research .
|
-
- HY-A0009R
-
|
Galantamine hydrobromide (Standard)
|
nAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
Galanthamine (hydrobromide) (Standard) is the analytical standard of Galanthamine (hydrobromide). This product is intended for research and analytical applications. Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
|
-
- HY-17504BS2
-
|
ZD 4522-13C,d3 sodium; X-Plended-13C,d3 sodium; Crestor-13C,d3 sodium
|
Autophagy
Bacterial
HMG-CoA Reductase (HMGCR)
Potassium Channel
Isotope-Labeled Compounds
|
Cardiovascular Disease
Metabolic Disease
|
|
Rosuvastatin- 13C,d3 sodium is 13C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-17387S1
-
|
Huperzine A-d4
|
iGluR
Cholinesterase (ChE)
Apoptosis
Isotope-Labeled Compounds
|
Neurological Disease
|
|
(-)-Huperzine A-d4 hydrochloride is deuterated labeled (-)-Huperzine A (HY-17387). (-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease .
|
-
- HY-N6948S
-
|
|
Isotope-Labeled Compounds
|
Inflammation/Immunology
|
|
Linalyl acetate-d6 is deuterated labeled Omeprazole (HY-B0113). Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-B0113S4
-
|
H 16868-d3 sodium
|
Autophagy
Phospholipase
Proton Pump
Bacterial
Isotope-Labeled Compounds
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole-d3 sodium is deuterated labeled Omeprazole (HY-B0113). Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-162479
-
|
|
Phosphatase
Amyloid-β
|
Metabolic Disease
|
|
PTP1B-IN-26 (Compound 7a) is a derivative of phenylthiosemicarbazide‐phenoxy‐1,2,3‐triazole‐N‐phenylacetamide. PTP1B-IN-26 is an inhibitor of protein tyrosine phosphatase 1B (PTP-1B). PTP1B-IN-26 is a competitive inhibitor. PTP1B-IN-26 can be used to research in type 2 diabetes .
|
-
- HY-106634R
-
|
|
HIV
Apoptosis
|
Infection
Cancer
|
|
Mitoguazone (Standard) is the analytical standard of Mitoguazone. This product is intended for research and analytical applications. Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment .
|
-
- HY-12542AR
-
|
|
Calcium Channel
Autophagy
|
Others
|
|
Dantrolene (sodium hemiheptahydrate) (Standard) is the analytical standard of Dantrolene (sodium hemiheptahydrate). This product is intended for research and analytical applications. Dantrolene sodium hemiheptahydrate is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene sodium hemiheptahydrate is a ryanodine receptor (RyR) antagonist and Ca2+ signaling stabilizer. Dantrolene sodium hemiheptahydrate is a direct-acting skeletal muscle relaxant. Dantrolene sodium hemiheptahydrate can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome .
|
-
- HY-17395AR
-
|
|
Fungal
Bacterial
Antibiotic
|
Infection
|
|
Terbinafine (Standard) is the analytical standard of Terbinafine. This product is intended for research and analytical applications. Terbinafine (TDT 067) is an orally active and potent antifungal agent. Terbinafine is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a Ki of 30 nM. Terbinafine also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria . Terbinafine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-17395R
-
|
|
Fungal
Bacterial
Antibiotic
|
Infection
|
|
Terbinafine hydrochloride (Standard) is the analytical standard of Terbinafine hydrochloride. This product is intended for research and analytical applications. Terbinafine hydrochloride (TDT 067 hydrochloride) is an orally active and potent antifungal agent. Terbinafine hydrochloride is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a Ki of 30 nM. Terbinafine hydrochloride also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria . Terbinafine hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-50878R
-
|
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib (Standard) is the analytical standard of Crizotinib. This product is intended for research and analytical applications. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
|
-
- HY-B0985R
-
|
|
TRP Channel
|
Neurological Disease
|
|
Phenazopyridine (hydrochloride) (Standard) is the analytical standard of Phenazopyridine (hydrochloride). This product is intended for research and analytical applications. Phenazopyridine hydrochlorideis a competitive SARM1 inhibitor, with IC50 145 μM. Phenazopyridine hydrochlorideis a TRPM8 antagonist. Phenazopyridine hydrochloride has a local anesthetic/analgesic effect. Phenazopyridine hydrochlorideis used to relieve painful symptoms of conditions such as cystitis and urethritis. Phenazopyridine hydrochloridecan promote neuronal differentiation and can also be used in the study of traumatic brain injury, peripheral neuropathy and neurodegenerative diseases .
|
-
- HY-18174H
-
|
LY2606368 lactate
|
Checkpoint Kinase (Chk)
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
Prexasertib lactate (LY2606368 lactate) is the lactate form of Prexasertib (HY-18174). Prexasertib lactate is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib lactate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib lactate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib lactate shows potent anti-tumor activity .
|
-
- HY-130337
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Teicoplanin A2-2 is a glycopeptide antibiotic. Teicoplanin A2-2 exhibits antibacterial activity, particularly against coagulase-negative staphylococci (CNS). Teicoplanin A2-2 inhibits bacterial cell wall synthesis by competitively binding to the terminal D-Ala-D-Ala peptide bonds in the cell wall synthesis process, leading to bacterial death. Teicoplanin A2-2 can be used for research into bacterial resistance mechanisms and the development of new antibiotics .
|
-
- HY-13716S
-
|
|
Isotope-Labeled Compounds
Apoptosis
Opioid Receptor
|
Cancer
|
|
Noscapine-13C,d3 is a deuterated labeled Noscapine . Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier .
|
-
- HY-18187
-
|
|
Apoptosis
|
Cancer
|
|
Ki 23057 is a competitive, orally active inhibitor for tyrosine kinase, which inhibits the phosphorylation of K-samII/FGF-R2, VEGF-R1, VEGF-R2, PDGF-Rβ and c-Kit, with IC50s of 88, 69, 83, 100 and 480 nM. Ki 23057 inhibits the proliferation of sclerogastric cancer cells OCUM-2MD3 and OCUM-8, and induces apoptosis. Ki 23057 exhibits antitumor efficacy in mouse models .
|
-
- HY-137373
-
|
|
PKG
|
Others
|
|
Rp-8-pCPT-cGMPS is a competitive inhibitor of cGMP-dependent protein kinase (PKG) (Ki=0.5 μM). Rp-8-pCPT-cGMPS has high lipid solubility and can more easily penetrate the cell membrane and reach sufficient concentration inside the cell to inhibit cGMP-dependent protein kinase. Rp-8-pCPT-cGMPS can be used to study the activity and function of cGMP-dependent protein kinase in platelets .
|
-
- HY-108960
-
|
|
P2X Receptor
|
Inflammation/Immunology
|
|
PPADS is a P2 receptor antagonist, with IC50s of 68 nM (P2X1) and 214 nM (P2X3). PPADS acts as an ATP (nucleotide) mimetic and competes with ATP for its binding site on P2 receptors. PPADS is also a reversible competitive antagonist of the NAADP receptor. PPADS reverses nociceptive hypersensitivity and reduces the increased NO/NOS system and IL-1β in both peripheral and central steps of nervous system .
|
-
- HY-B0368R
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
Cancer
|
|
Captopril (Standard) is the analytical standard of Captopril. This product is intended for research and analytical applications. Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM .
|
-
- HY-B0369AR
-
|
|
iGluR
|
Neurological Disease
|
|
Orphenadrine (citrate) (Standard) is the analytical standard of Orphenadrine (citrate). This product is intended for research and analytical applications. Orphenadrine citrate is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine citrate relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine citrate is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases .
|
-
- HY-123163
-
|
RWJ-66826; RTI-6617-003
|
Progesterone Receptor
Glucocorticoid Receptor
Androgen Receptor
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
|
JNJ-1250132 (RWJ-66826) is an orally active and potent steroidal progesterone receptor (PR) antagonist, with an IC50 of 1.3 nM. JNJ-1250132 inhibits binding of the receptor to DNA in vitro. JNJ-1250132 is a potent competitive inhibitor of binding to the human glucocorticoid receptor (GR) (IC50=0.50 nM) and the rat androgen receptor (AR) (IC50=5.6 nM), and was a weak inhibitor of binding to human Estrogen receptor (ER) (IC50 >3000 nM) .
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-
- HY-107794R
-
|
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Others
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Clodronate (disodium tetrahydrate) (Standard) is the analytical standard of Clodronate (disodium tetrahydrate). This product is intended for research and analytical applications. Clodronate disodium tetrahydrate (Disodium clodronate tetrahydrate) is first-generation bisphosphonate, with anti-osteoporotic, anti-inflammatory and analgesic effects. Clodronate disodium tetrahydrate is a selective, potent, reversible and Cl-competitive vesicular nucleotide transporter (VNUT) inhibitor, with an IC50 of 15.6 nM. Clodronate disodium tetrahydrate inhibits vesicular ATP release from neurons and reduces chronic neuropathic and inflammatory pain .
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- HY-B0307R
-
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|
Phosphatase
Orthopoxvirus
|
Infection
Cancer
|
|
Idoxuridine (Standard) is the analytical standard of Idoxuridine. This product is intended for research and analytical applications. Idoxuridine (5-Iodo-2′-deoxyuridine, 5-IUdR, IdUrd) is an iodinated thymidine analogue that competitively inhibits phosphorylases. Idoxuridine can inhibit viral activity, particularly viral eye infections, including herpes simplex keratitis, by inhibiting DNA polymerase and affecting viral replication. Idoxuridine against feline herpesvirus has the IC50 value of 4.3 μM . Idoxuridine shows anti-orthopoxvirus activity.
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-
- HY-124626
-
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Histamine Receptor
|
Inflammation/Immunology
|
(R)-(+)-Mequitazine is a histamine H1 receptor antagonist that mainly undergoes bio-transformation via human liver microsomes, resulting in hydroxylated and S-oxidized metabolites. (R)-(+)-Mequitazine competitively binds to the H1 receptors in gastrointestinal, vascular, and respiratory effect cells, thus blocking the endogenous activity of histamine. (R)-(+)-Mequitazine has an inhibitory effect on CYP3A-catalyzed midazolam 1’-hydroxylase. (R)-(+)-Mequitazine can be used in the study of various allergic diseases .
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-
- HY-160843
-
|
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Apoptosis
|
Cancer
|
|
N-ω-chloroacetyl-L-ornithine (NCAO) is a potent reversible competitive ornithine decarboxylase (ODC) inhibitor that exerts cytotoxic and antiproliferative effects on tumor cell lines with EC50 values ranging from 1 to 50.6 µM. NCAO induces tumor cell Apoptosis and inhibits tumor cell migration in vitro. NCAO also exhibits a potent antitumor activity against both solid and ascitic tumors in a mouse model using the myeloma (Ag8) cell line. NCAO is promising for research of antitumor agents .
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-
- HY-119013
-
|
|
Others
|
Cardiovascular Disease
|
|
VPC32183 is a competitive antagonist of LPA1 and LPA3 receptors. The activity of VPC32183 can inhibit lipid phosphatase 1 (LPP1), thereby preventing the activation of ERK(1/2) by dioctanoic acid diglyceride (DGPP 8:0). By reducing the expression of LPP1, VPC32183 can further reduce DGPP 8:0-induced ERK(1/2) activation. The effects of VPC32183 suggest that it may have a positive regulatory function in cell signaling processes .
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-
- HY-N1584C
-
|
RU-19110 lactate
|
DNA/RNA Synthesis
TGF-beta/Smad
Parasite
Sodium Channel
Calcium Channel
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Halofuginone lactate, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM . Halofuginone lactate is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity . Halofuginone lactate is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone lactate has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
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-
- HY-116919
-
|
|
Others
|
Cardiovascular Disease
|
|
MLS000536924 is a potent and selective inhibitor of human epithelial 15-lipoxygenase-2 with competitive activity. MLS000536924 exhibits more than 50-fold selectivity in inhibiting h15-LOX-2 and can be effectively applied to study its role in atherosclerosis, cystic fibrosis, and ferroptosis. The binding mode of MLS000536924 shows stronger restriction of protein movement than other inhibitors, further verifying its higher biological activity .
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-
- HY-19279A
-
|
|
Others
|
Endocrinology
|
|
JTH-601 Free base is a novel alpha1-adrenoceptor antagonist that exhibits potent activity in inhibiting phenylephrine-induced contractions in lower urinary tract tissues. JTH-601 Free base competitively antagonizes alpha1-adrenoceptor-mediated contractile responses, demonstrating greater potency than prazosin or tamsulosin. JTH-601 Free base is anticipated to be effective in treating urinary outlet obstruction associated with benign prostatic hyperplasia.
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-
- HY-10108
-
LY294002
Maximum Cited Publications
769 Publications Verification
|
PI3K
Casein Kinase
DNA-PK
Apoptosis
Autophagy
|
Infection
Cancer
|
|
LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively . LY294002 also inhibits CK2 with an IC50 of 98 nM . LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4?μM. LY294002 is an apoptosis activator .
|
-
- HY-15196
-
TAK-285
2 Publications Verification
|
EGFR
|
Cancer
|
|
TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity . TAK-285 can cross the blood-brain barrier (BBB) .
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-
- HY-15425A
-
|
Sphingosine Kinase 1 Inhibitor II Citrate
|
SphK
LPL Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 Citrate is >100-fold selectivity for SPHK1 over SPHK2. PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 Citrate induces apoptosis, necrosis, and autophagy .
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-
- HY-10450A
-
|
BMS-512148 (2S)-1,2-propanediol, hydrate
|
SGLT
|
Metabolic Disease
Cancer
|
|
Dapagliflozin ((2S)-1,2-propanediol, hydrate) is the S-enantiomer of Dapagliflozin 1,2-propanediol, hydrate. Dapagliflozin ((2S)-1,2-propanediol, hydrate), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin ((2S)-1,2-propanediol, hydrate) induces HIF1 expression and attenuates renal IR injury .
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-
- HY-12755
-
|
CID-2950007
|
Ras
Apoptosis
|
Cancer
|
|
ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines .
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-
- HY-19989A
-
|
L-660711 sodium
|
Leukotriene Receptor
LPL Receptor
|
Inflammation/Immunology
|
|
MK-571 (L-660711) sodium is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 sodium is also a inhibitor of multidrug resistance-associated protein MRP4 (ABCC4) and ABCC1 (MRP1). MK-571 sodium inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release .
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-
- HY-100542
-
|
Disodium (R)-2-hydroxyglutarate
|
Reactive Oxygen Species
ATP Synthase
mTOR
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid disodium is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid disodium increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid disodium binds and inhibits ATP synthase and inhibits mTOR signaling .
|
-
- HY-100034
-
|
DA-3003-1
|
Phosphatase
Histone Methyltransferase
|
Cancer
|
|
NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively . NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM) .
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-
- HY-12214A
-
|
|
CDK
Apoptosis
|
Cancer
|
|
NVP-2 is a potent and selective ATP-competitive cyclin dependent kinase 9 (CDK9) probe, inhibits CDK9/CycT activity with an IC50 of 0.514 nM. NVP-2 displays inhibitory effcts on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases with IC50 values of 0.584 µM, 0.706 µM, and 0.605 µM, respectively. NVP-2 induces cell apoptosis.
|
-
- HY-B0113S3
-
|
H 16868-13C,d3
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole- 13C,d3 is a 13C-labeled and deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
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-
- HY-N1584A
-
|
RU-19110 hydrobromide
|
DNA/RNA Synthesis
TGF-beta/Smad
Parasite
Sodium Channel
Calcium Channel
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM . Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity . Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
|
-
- HY-117626
-
|
|
AAK1
Cyclin G-associated Kinase (GAK)
SARS-CoV
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
LP-935509 is an orally active, potent, selective, ATP-competitive and brain-penetrant inhibitor of adaptor protein-2 associated kinase 1 (AAK1) with an IC50 of 3.3 nM and a Ki of 0.9 nM, respectively. LP-935509 is also a potent inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-935509 shows antinociceptive activity. LP-935509 can be used for neuropathic pain and SARS-CoV-2 research .
|
-
- HY-101249
-
|
|
Neurokinin Receptor
|
Neurological Disease
Cancer
|
|
L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC50 of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732138 can reduce hyperalgesia and has antitumor action .
|
-
- HY-17504D
-
|
|
HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
|
Cardiovascular Disease
Metabolic Disease
|
|
(3S,5R)-Rosuvastatin is the (3S,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM . Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM . Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-17504C
-
|
|
HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
|
Cardiovascular Disease
Metabolic Disease
|
|
(3R,5R)-Rosuvastatin is the (3R,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM . Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM . Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-123931
-
ZLDI-8
1 Publications Verification
|
Notch
Phosphatase
Apoptosis
|
Cancer
|
|
ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor with an IC50 of 31.6 μM and a Ki of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC50 of 5.32 μM .
|
-
- HY-100434
-
|
|
FGFR
PDGFR
EGFR
Src
TGF-β Receptor
|
Cardiovascular Disease
Cancer
|
|
PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively . PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor .
|
-
- HY-17499
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC50of 21 nM. EGFR-IN-12 also inhibits mutant EGFR L858R and EGFR L861Q with IC50s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC50 = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity .
|
-
- HY-145597
-
|
|
GLUT
Disulfidptosis
|
Metabolic Disease
Cancer
|
|
KL-11743 is a potent, orally active, and glucose-competitive inhibitor of the class I glucose transporters, with IC50s of 115, 137, 90, and 68 nM for GLUT1, GLUT2, GLUT3, and GLUT4, respectively. KL-11743 specifically blocks glucose metabolism. KL-11743 can synergize with electron transport inhibitors to induce cell death. In addition, KL-11743 can induce the formation of disulfide bonds in actin cytoskeletal proteins, leading to the occurrence of cellular disulfidptosis .
|
-
- HY-105349
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. T-0156 specifically inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) by PDE5 in a competitive manner (IC50=0.23 nM). T-0156 inhibits PDE6 (IC50=56 nM) and has low potencies against PDE1, PDE2, PDE3, and PDE4 (IC50>10 μM). T-0156 enhances the nitric oxide (NO)/cGMP pathway .
|
-
- HY-141539A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
SETDB1-TTD-IN-1 TFA is a potent, selective and endogenous binder competitive ligand of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD) that binds to TTD, with a Kd of 88 nM. SETDB1-TTD-IN-1 TFA increases SETDB1 methyltransferase activity. SETDB1-TTD-IN-1 TFA can be used for the research of biological functions and disease associations of SETDB1-TTD .
|
-
- HY-151453
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive human DNA topoisomerase II inhibitor with an IC50 value of 3.8 and 10.1 μM for TopoIIα and TopoIIβ, respectively. Topoisomerase IIα-IN-4 shows potent potency in apoptosis induction and cell cycle arrest in HepG2 cells. Topoisomerase IIα-IN-4 exhibits strong antitumor activities against human cancer cell lines, it can be used for the research of cancer .
|
-
- HY-17623S
-
|
CJ-12420-d6; RQ-00000004-d6
|
Proton Pump
Na+/K+ ATPase
|
Metabolic Disease
|
|
Tegoprazan (CJ-12420; RQ-00000004), a potassium-competitive acid blocker, is a reversible, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H +/K +-ATPases in vitro. Tegoprazan significantly improves colitis in mice and enhances the intestinal epithelial barrier function. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases .
|
-
- HY-112478
-
|
|
Phosphatase
SHP2
|
Cancer
|
|
PTP Inhibitor IV is a protein tyrosine phosphatase (PTP) inhibitor that competitively inhibits DUSP14 phosphatase activity with an 50 of 5.21 μM . PTP Inhibitor IV inhibits SHP-2, PTP1B, PTP-ε, PTP Meg-2, PTP-σ, PTP-β, and PTP-μ with 50s of 1.8 μM, 2.5 μM, 8.4 μM, 13 μM, 20 μM, 6.4 μM, and 6.7 μM, respectively .
|
-
- HY-121197
-
|
Ophiocordin; Azepinostatin
|
MARCKS
PKA
PKC
|
Others
|
|
Balanol (Ophiocordin; Azepinostatin) is a potent and ATP competitive PKC/PKA inhibitor against human PKC isozymes α, β-I, β-II, γ, δ, ε, η (IC50s=4-9 nM) and ζ (IC50=150 nM). Balanol also blocks the phosphorylation of cyclic AMP response element-binding protein (CREB) and myristoylated alanine-rich C kinase substrate (MARCKS). Balanol can be isolated from the fungus Verticillium balanoides .
|
-
- HY-112291
-
|
|
p38 MAPK
Src
PKC
|
Inflammation/Immunology
|
|
SB 220025 is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC50 = 60 nM). SB 220025 also inhibits p56 Lck and PKC with IC50 values of 3.5 and 2.89 µM, respectively. SB 220025 inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation .
|
-
- HY-P5272
-
|
|
Bacterial
|
Inflammation/Immunology
|
|
Histatin-3 TFA, a 32 amino acid peptide, possesses powerful antimicrobial properties. Histatin-3 TFA behaves as a substrate for proprotein convertase 1 (PC1), being cleaved by this endoprotease primarily at a site carboxy terminal to the single Arg25 residue (HRGYR decrease SN). Histatin-3 TFA is a moderately potent, reversible and competitive inhibitor of the furin-mediated cleavage of the pentapeptide pGlu-Arg-Thr-Lys-Arg-MCA fluorogenic substrate, with an estimated inhibition constant Ki of 1.98 μM .
|
-
- HY-P5601
-
|
|
Bacterial
Fungal
|
Infection
|
|
Thanatin is an inducible cationic antimicrobial peptide. Thanatin is a pathogen-inducible single-disulfide-bond-containing β-hairpin AMP. Thanatin displays broad-spectrum activity against both Gram-negative and Gram-positive bacteria as well as against various species of fungi with MICs of 0.3-40 µM, 0.6-40 µM and 0.6-20 µM, respectively. Thanatin has the property of competitive replacement of divalent cations from bacterial outer membrane (OM), leading to OM disruption .
|
-
- HY-122595
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EZH2-IN-1 (compound 3) is a selective and SAM-competitive EZH2 and EZH1 inhibitor with an IC50s of 32 nM, 197 nM and 213 nM for EZH2wt, EZH2 Y641N mutant and EZH1, respectively. EZH2-IN-1 reduces bulk H3K27me3 and H3K27me2 levels. EZH2-IN-1 has the potential for diffuse large B cell lymphoma research .
|
-
- HY-N1584B
-
|
RU-19110 hydrochloride
|
Calcium Channel
DNA/RNA Synthesis
Parasite
Sodium Channel
TGF-beta/Smad
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
|
-
- HY-133233
-
|
1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Thioetheramide-PC is a structurally modified phospholipid that functions as a competitive, reversible inhibitor of secretory phospholipase A2 (sPLA2). The IC50 value for thioetheramide-PC is 2 μM at a substrate concentration of 0.5 mM.1 In addition to binding to the catalytic site of sPLA2, thioetheramide-PC also binds to the activator site of this enzyme. The binding of thioetheramide-PC to the activator site is tighter than its binding to the catalytic site. The result of this dual interaction is that at low concentrations thioetheramide-PC may activate phospholipase activity rather than inhibiting it.
|
-
- HY-120812
-
|
|
HIV Protease
|
Infection
|
|
HIV-IN-11 is part of the hydroxylaminoglutaramide (HAPA) transition state isomeric series of HIV protease inhibitors and is a potent and selective inhibitor of HIV-1 protease. HIV-IN-11 competitively inhibits HIV-1 PR (Ki: 0.049 nM) and potently inhibits replication of HIV(IIIb)-infected MT4 lymphocytes at concentrations of 25.0-50.0 nM. HIV-IN-11 displays a longer half-life than indinavir sulfate in animal models and serves as a promising second-generation HIV protease inhibitor .
|
-
- HY-N2071R
-
|
|
Cytochrome P450
Fungal
Apoptosis
Caspase
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Cedrol (Standard) is the analytical standard of Cedrol. This product is intended for research and analytical applications. Cedrol is a potent competitive inhibitor of cytochrome P-450(CYP) enzyme. Cedrol plays an anticancer role by inducing cell cycle arrest and Caspase-dependent apoptosis. Cedrol acts as a neutrophil agonist that can desensitize cells to subsequent stimulation of N-formyl peptides. Cedrol prevents neuropathic pain caused by chronic contractile injury by inhibiting oxidative stress and inflammation. In addition, Cedrol has antibacterial, hair loss prevention and anti-anxiety properties.
|
-
- HY-W015309R
-
|
|
iGluR
Tyrosinase
c-Met/HGFR
Glutaminase
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Decanoic acid (Standard) is the analytical standard of Decanoic acid. This product is intended for research and analytical applications. Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .
|
-
- HY-164474
-
|
|
MEK
|
Cancer
|
|
DS03090629 is an orally active MEK inhibitor that inhibits MEK activity in an ATP-competitive manner. DS03090629 exhibits high affinity for both MEK and phosphorylated MEK, with Kd values of 0.11 and 0.15 nM, respectively. It effectively inhibits the proliferation of BRAF-mutant overexpressing melanoma cell lines, with IC50 values of 74.3 and 97.8 nM for BRAF V600E and MEK1 F53L transfected A375 cells, respectively. DS03090629 holds potential value in the field of anti-melanoma therapy .
|
-
- HY-112291A
-
|
|
p38 MAPK
Src
PKC
|
Inflammation/Immunology
|
|
SB 220025 trihydrochloride is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC50 = 60 nM). SB 220025 trihydrochloride also inhibits p56 Lck and PKC with IC50 values of 3.5 and 2.89 μM, respectively. SB 220025 trihydrochloride inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 trihydrochloride effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation .
|
-
- HY-10071
-
|
|
Organoid
ROCK
Apoptosis
|
Cancer
|
|
Y-27632 is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 attenuates Doxorubicin-induced apoptosis of human cardiac stem cells. Y-27632 also suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells. Y-27632 primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation .
|
-
- HY-11009
-
|
|
CDK
PKC
|
Cancer
|
|
CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor .
|
-
- HY-10256
-
|
SB 203580; RWJ 64809
|
Organoid
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
|
Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator .
|
-
- HY-15346
-
|
BAY 80-6946
|
PI3K
Apoptosis
|
Cancer
|
|
Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity .
|
-
- HY-18299
-
|
NG 95
|
CDK
Parasite
|
Infection
Cancer
|
|
Purvalanol B (NG 95) is a potent, selective, reversible and ATP-competitive inhibitor CDK, with IC50s of 6 nM, 6 nM, 9 nM, 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively. Purvalanol B shows selectivity for CDK over a range of other protein kinases (IC50>1000 nM). Purvalanol B inhibits the growth a chloroquine-resistant strain of P. falciparum .
|
-
- HY-10256A
-
|
SB 203580 hydrochloride; RWJ 64809 hydrochloride
|
Organoid
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
|
Adezmapimod (SB 203580; RWJ 64809) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride does not disrupt JNK activity and is an autophagy and mitophagy activator .
|
-
- HY-B0267A
-
|
|
mAChR
Potassium Channel
|
Neurological Disease
|
|
Oxybutynin chloride is an oral active and competitive mAChR antagonist with Kis of 14.3 and 5.55 nM for specific [ 3H]NMS binding in the mouse bladder and cerebral cortex, respectively. Oxybutynin chloride inhibits vascular Kv channels in a manner independent of anticholinergic effect, with an IC50 value of 11.51 μM. Oxybutynin chloride reduces muscle spasm in the bladder and urinary tract, can be used in study of overactive bladder syndrome (OAB) . Oxybutynin (chloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-11010
-
|
|
JNK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
AS601245 is an orally active, selective, ATP competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. AS601245 exhibits 10- to 20-fold selectivity over c-src, CDK2, and c-Raf and more than 50- to 100-fold selectivity over a range of Ser/Thr- and Tyr-protein kinases. Neuroprotective properties .
|
-
- HY-17422S1
-
|
Aciclovir-d4; Acycloguanosine-d4
|
Isotope-Labeled Compounds
HSV
Bacterial
Apoptosis
Antibiotic
|
Infection
Cancer
|
|
Acyclovir-d4 is the deuterium labeled Acyclovir. Acyclovir (Aciclovir) is a guanosine analogue and an orally active antiviral agent. Acyclovir inhibits HSV-1 (IC50 of 0.85 μM), HSV-2 (IC50 of 0.86 μM) and varicella-zoster virus. Acyclovir can be phosphorylated by viral thymidine kinase (TK), and Acyclovir triphosphate interferes with viral DNA polymerization through competitive inhibition with guanosine triphosphate and obligatory chain termination[1][2][3]. Acyclovir prevents bacterial infections during induction therapy for acute leukaemia[4].
|
-
- HY-N6789
-
KT5720
3 Publications Verification
|
PKA
|
Neurological Disease
Cancer
|
|
KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2 + concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases .
|
-
- HY-15346A
-
|
BAY 80-6946 dihydrochloride
|
PI3K
Apoptosis
|
Cancer
|
|
Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib dihydrochloride has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib dihydrochloride has superior antitumor activity .
|
-
- HY-124131
-
|
|
Histone Methyltransferase
|
Inflammation/Immunology
Cancer
|
|
DS-437 is a dual PRMT5/7 inhibitor (IC50s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5. DS-437 also inhibits DNMT3A and DNMT3B, with IC50s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3 .
|
-
- HY-108601A
-
|
|
PKC
|
Neurological Disease
Inflammation/Immunology
|
|
(S)-Ro 32-0432 is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of (S)-Ro 32-0432 for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. (S)-Ro 32-0432 is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research .
|
-
- HY-W011109
-
|
|
Casein Kinase
CDK
SGK
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases .
|
-
- HY-122203
-
|
|
mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively .
|
-
- HY-15814
-
|
|
Bcr-Abl
PDGFR
c-Kit
Src
JAK
Apoptosis
|
Cancer
|
|
HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression .
|
-
- HY-125959
-
Ucf-101
1 Publications Verification
|
Apoptosis
|
Cardiovascular Disease
Neurological Disease
|
|
Ucf-101 is a selective and competitive inhibitor of pro-apoptotic protease Omi/HtrA2, with an IC50 of 9.5 μM for His-Omi. Ucf-101 exhibits very little activity against various other serine proteases (IC50>200 μM). Ucf-101 has a natural red fluorescence at 543 nm that is used to monitor its ability to enter mammalian cells. Ucf-101 has a significant cardioprotective effect against MI/R injury and also has certain neuroprotective effect .
|
-
- HY-N0215S13
-
|
(S)-2-Amino-3-phenylpropionic acid-d1
|
Isotope-Labeled Compounds
Calcium Channel
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Phenylalanine-d is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
|
-
- HY-146691
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible hMAO-B inhibitor, with an IC50 of 4 nM. hMAO-B-IN-2 shows low toxicity and good neuroprotective effects in SH-SY5Y cell. hMAO-B-IN-2 can be used for alzheimer’s disease research . hMAO-B-IN-2 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-W324243
-
|
|
11β-HSD
|
Metabolic Disease
|
|
11β-HSD1-IN-9 (compound c4a) is a potent 11β-HSD1 inhibitor with IC50 values of 0.48 and 1.3 µM for human and murine 11β-HSD1, respectively. 11β-HSD1-IN-9 competitively interacts with rat 11β-HSD1. 11β-HSD1-IN-19 can be used in studies of obesity, hyperglycemia and cognitive impairment .
|
-
- HY-160250
-
|
|
UGT
|
Metabolic Disease
|
|
UGT1A1-IN-1 (compound 2) is a non-competitive inhibitor of UGT1A1, which can inhibit the 1-O-glucuronidation process mediated by UGT1A1 with a Ki value of 5.02 μM. UGT1A1-IN-1 (compound 2) can bind on UGT1A1 at the same ligand-binding site as bilirubin (HY-N0323). UGT1A1-IN-1 can serve as a ‘turn-on’ fluorescent probe substrate for UGT1A1 .
|
-
- HY-P5601A
-
|
|
Bacterial
Fungal
|
Infection
|
|
Thanatin TFA is an inducible cationic antimicrobial peptide. Thanatin TFA s a pathogen-inducible single-disulfide-bond-containing β-hairpin AMP. Thanatin TFA displays broad-spectrum activity against both Gram-negative and Gram-positive bacteria as well as against various species of fungi with MICs of 0.3-40 µM, 0.6-40 µM and 0.6-20 µM, respectively. Thanatin TFA has the property of competitive replacement of divalent cations from bacterial outer membrane (OM), leading to OM disruption .
|
-
- HY-110196
-
|
|
Others
|
Others
|
|
(S)-PFI-2 hydrochloride is an inhibitor of lysine methyltransferase SETD7 and is approximately 500-fold more active than its enantiomer (R)-PFI-2. (R)-PFI-2 is a cofactor-dependent and substrate-competitive inhibitor. (R)-PFI-2 can occupy the substrate peptide binding groove of SETD7 (including the catalytic lysine binding channel) and interact with the cofactor The donor methyl group is in direct contact. However, (S)-PFI-2 was not observed to have the same interaction as (R)-PFI-2 .
|
-
- HY-B0442AS
-
|
|
Endogenous Metabolite
Phosphodiesterase (PDE)
Isotope-Labeled Compounds
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil-d5 hydrochloride is deuterated labeled Vardenafil hydrochloride (HY-B0442A). Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-B0267BS
-
|
|
mAChR
Isotope-Labeled Compounds
|
Neurological Disease
|
|
Oxybutynin-d5 hydrochloride is deuterated labeled (R)-Oxybutynin hydrochloride (HY-B0267B). (R)-Oxybutynin hydrochloride, a (R)-isomer of Oxybutynin hydrochloride, is an orally active muscarinic receptor antagonist. (R)-Oxybutynin hydrochloride has antimuscarinic, antispasmodic and anticholinergic activity, competitively antagonizes Carbachol-induced contractions. (R)-Oxybutynin hydrochloride can be used for researching incontinence due to neurogenic bladder dysfunction . (R)-Oxybutynin hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-B0442R
-
|
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil (Standard) is the analytical standard of Vardenafil. This product is intended for research and analytical applications. Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-10071A
-
|
|
Organoid
ROCK
Apoptosis
|
Cancer
|
|
Y-27632 hydrochloride hydrate is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 hydrochloride hydrate attenuates Doxorubicin-induced apoptosis of human cardiac stem cells. Y-27632 hydrochloride hydrate also suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells. Y-27632 hydrochloride hydrate primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation .
|
-
- HY-W747548
-
|
|
Others
|
Inflammation/Immunology
|
|
12(S)-HEPE is a monohydroxy fatty acid synthesized from EPA by the action of 12-LO. Unstimulated neutrophils metabolize 12(S)-HEPE to 12(S),20-diHEPE, whereas stimulated neutrophils produce 5(S),12(S)-HEPE via the 5-lipoxygenase pathway. The competitive action of 12(S)-HEPE with arachidonic acid as a substrate for 5-LO in the formation of leukotrienes may provide a basis for the anti-inflammatory potential of ω-3 fatty acids.
|
-
- HY-161667
-
|
|
GSK-3
HDAC
|
Neurological Disease
|
|
GSK-3β/HDAC-IN-1 (Compd 4) is a brain-penetrant and first in class dual non-ATP-competitive Glycogen Synthase Kinase 3β/Histone Deacetylases (GSK-3β/HDACs) Inhibitor with IC50s of 0.142, 0.03 and 0.045 μM against GSK-3β, HDAC2 and HDAC6, respectively. GSK-3β/HDAC-IN-1 can be used for Alzheimer’s disease research .
|
-
- HY-19674
-
|
SSR182289A free base
|
Thrombin
|
Cardiovascular Disease
|
|
SSR182289 (SSR182289A free base) is a selective and potent orally active thrombin inhibitor. SSR182289 competitively and selectivity inhibits human thrombin (Ki=0.031 μM). SSR182289 demonstrates anticoagulant activity in vitro (thrombin time EC100=96 nM) and inhibits tissue factor-induced thrombin generation (IC50=0.15 μM) in human plasma. SSR182289 inhibits thrombin-induced aggregation of human platelets (IC50=32 nM), but has no effect on aggregation induced by other platelet agonists .
|
-
- HY-14243
-
|
|
Anaplastic lymphoma kinase (ALK)
Insulin Receptor
VEGFR
Tie
|
Cancer
|
|
CEP-14083 is a ATP-competitive ALK kinase inhibitor with an IC50 value in enzymatic assays of 2 nM. CEP-14083 also inhibits other kinases, such as insulin receptor (IR), vascular endothelial growth factor receptor 2 (VEGFR2), angiopoietin-1 receptor (TIE2) and dual leucine zipper kinase (DLK). CEP-14083 suppresses CD274 mRNA expression and the NPM/ALK function in the NPM/ALK-carrying T cell lymphoma (ALK+TCL) cells. CEP-14083 is promising for research of lymphoma .
|
-
- HY-11010A
-
|
|
JNK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
AS601245 TFA is an orally active, selective, ATP competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. AS601245 TFA exhibits 10- to 20-fold selectivity over c-src, CDK2, and c-Raf and more than 50- to 100-fold selectivity over a range of Ser/Thr- and Tyr-protein kinases. Neuroprotective properties .
|
-
- HY-13409
-
|
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
|
SB 242084 is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C receptor antagonist (crosses the blood-brain barrier). SB 242084 increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 also increases mitochondrial gene expression and oxidative metabolism via 5-HT2A receptor. SB 242084 has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage .
|
-
- HY-13409A
-
|
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
|
SB 242084 dihydrochloride is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C receptor antagonist (crosses the blood-brain barrier). SB 242084 dihydrochloride increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 dihydrochloride also increases mitochondrial gene expression and oxidative metabolism via 5-HT2A receptor. SB 242084 dihydrochloride has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage .
|
-
- HY-N0215S3
-
|
(S)-2-Amino-3-phenylpropionic acid-d2
|
Calcium Channel
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Phenylalanine-d2 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
|
-
- HY-N0215S2
-
|
(S)-2-Amino-3-phenylpropionic acid-13C
|
Isotope-Labeled Compounds
Calcium Channel
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Phenylalanine- 13C is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
|
-
- HY-N0215S
-
|
(S)-2-Amino-3-phenylpropionic acid-d7
|
Isotope-Labeled Compounds
Calcium Channel
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Phenylalanine-d7 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
|
-
- HY-N0215S1
-
|
(S)-2-Amino-3-phenylpropionic acid-d8
|
Calcium Channel
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Phenylalanine-d8 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
|
-
- HY-18346S
-
|
OPC-31260-d6
|
Isotope-Labeled Compounds
Vasopressin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Mozavaptan-d6 (OPC-31260-d6) is the deuterium labeled Mozavaptan. Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment .
|
-
- HY-121638A
-
|
|
Apoptosis
DGK
|
Cancer
|
|
(5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells .
|
-
- HY-107522
-
|
|
EAAT
|
Neurological Disease
|
|
DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA inhibits the uptake of [ 14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively .
|
-
- HY-135680
-
|
I-OMe-AG 538
|
IGF-1R
|
Metabolic Disease
Cancer
|
|
I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells. I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50 of 1 µM .
|
-
- HY-110137A
-
|
DB75; NSC 305831
|
Histone Methyltransferase
Phosphodiesterase (PDE)
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent .
|
-
- HY-W011428
-
|
|
CDK
|
Others
Cancer
|
|
Olomoucine is an ATP competitive inhibitor of CDKs. Olomoucine is a purine (HY-34431) derivative and inhibits CDC2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E (both IC50=7 μM), CDK/p35 kinase (IC50=3 μM) and ERK1/p44 MAP kinase (IC50=25 μM) . Olomoucine regulates cell cycle and shows anti-melanin tumor activity .
|
-
- HY-110137
-
|
DB75 dihydrochloride; NSC 305831 dihydrochloride
|
Histone Methyltransferase
Phosphodiesterase (PDE)
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 μM, 283 μM, and >400 μM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent .
|
-
- HY-N0215S5
-
|
(S)-2-Amino-3-phenylpropionic acid-15N
|
Isotope-Labeled Compounds
Calcium Channel
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Phenylalanine- 15N is the 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
|
-
- HY-N0215S10
-
|
(S)-2-Amino-3-phenylpropionic acid-13C9
|
Isotope-Labeled Compounds
Calcium Channel
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Phenylalanine- 13C9 is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
|
-
- HY-N0215S12
-
|
|
Calcium Channel
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Phenylalanine-d5 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
|
-
- HY-N0215S7
-
|
(S)-2-Amino-3-phenylpropionic acid-3-13C
|
Calcium Channel
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Phenylalanine-3- 13C is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
|
-
- HY-N0215S8
-
|
(S)-2-Amino-3-phenylpropionic acid-13C6
|
Isotope-Labeled Compounds
Calcium Channel
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Phenylalanine- 13C6 is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
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-
- HY-P5846
-
|
MT3
|
mAChR
Adrenergic Receptor
|
Neurological Disease
|
|
Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC50s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M1, M4, α1A, α1B, α1D,α2A,α2B and α2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity .
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-
- HY-N0142R
-
|
NSC 407292 (Standard); RJC 02792 (Standard)
|
SGLT
Endogenous Metabolite
GLUT
|
Metabolic Disease
Cancer
|
|
Phloretin (Standard) is the analytical standard of Phloretin. This product is intended for research and analytical applications. Phloretin (NSC 407292; RJC 02792) is a flavonoid extracted from Malus pumila Mill., has anti-inflammatory activities. Phloridzin is a specific, competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). Phloretin inhibits Yeast-made GLUT1 as well as Human erythrocyte GLUT1 with IC50values of 49 μM and 61 μM, respectively .Phloretin has the potential for the treatment of rheumatoid arthritis (RA)?and allergic airway inflammation .
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-
- HY-120826
-
|
|
Monoamine Oxidase
Adenosine Receptor
|
Neurological Disease
|
|
A2AAR/hMAO-B-IN-1 (compoudn 17) is a non-xanthine dual-target inhibitor targeting the A2A adenosine receptor (A2AAR) (IC50: 34.9 nM) andMAO-B (Ki: 39.5 nM, human). A2AAR/hMAO-B-IN-1 inhibits A2AAR-induced cAMP accumulation and exhibits competitive, reversible inhibition of MAO-B. A2AAR/hMAO-B-IN-1 can be used in the study of neurodegenerative diseases such as Parkinson's disease (PD) .
|
-
- HY-50878AS
-
|
PF-02341066-d9 hydrochloride
|
c-Met/HGFR
Autophagy
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Isotope-Labeled Compounds
|
Cancer
|
|
Crizotinib-d9 hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
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-
- HY-101193S
-
|
Zn(II)-protoporphyrin IX-d2,15N2; ZnPP-d2,15N2; Zinc Protoporphyrin-9-d2,15N2
|
Apoptosis
Endogenous Metabolite
Reactive Oxygen Species
Isotope-Labeled Compounds
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Zinc Protoporphyrin-d2, 15N2 is 15N and deuterated labeled Zinc Protoporphyrin (HY-101193). Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is an orally active and competitive heme oxygenase-1 (HO-1) inhibitor and markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2 . Zinc Protoporphyrin is used as a screening marker of iron deficiency in individual pregnant women and children, but also to assess population iron status in combination with haemoglobin concentration . Zinc Protoporphyrin has anti-cancer activity .
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-
- HY-136702
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
L-97-1 is a A1 adenosine receptor (A1AR) antagonist. L-97-1 is a water-soluble small molecule compound with high affinity and high selectivity against human A1 adenosine receptors. L-97-1 works by blocking A1 adenosine receptors. In patients with asthma, adenosine is an important signaling molecule capable of causing bronchoconstriction by activating A1AR. L-97-1 reduces airway hyperreactivity (BHR) by competitively binding to A1AR, thereby alleviating or blocking adenosine-induced bronchoconstriction and inflammation .
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-
- HY-16569R
-
|
|
Microtubule/Tubulin
NOD-like Receptor (NLR)
Autophagy
Apoptosis
|
Cancer
|
|
Colchicine (Standard) is the analytical standard of Colchicine. This product is intended for research and analytical applications. Colchicine, an orally active alkaloid, is a potent tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs). Colchicine prevents non-steroidal anti-inflammatory drug (NSAID)-induced small intestinal injury by inhibiting activation of the NLRP3 inflammasome. Colchicine has extensive anti-inflammatory, immunosuppressive and strong anti-fibrosis effects and has the potential for gouty arthritis research .
|
-
- HY-B1324R
-
|
|
Fungal
Cytochrome P450
Antibiotic
|
Infection
Cancer
|
|
Oxiconazole nitrate (Standard) is the analytical standard of Oxiconazole nitrate. This product is intended for research and analytical applications. Oxiconazole (Ro 13-8996) nitrate is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole nitrate is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole nitrate exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest .
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-
- HY-N0215R
-
|
|
Calcium Channel
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Phenylalanine (Standard) is the analytical standard of L-Phenylalanine. This product is intended for research and analytical applications. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals .
|
-
- HY-N0235R
-
|
|
Carboxylesterase
p38 MAPK
Autophagy
UGT
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Bakuchiol (Standard) is the analytical standard of Bakuchiol. This product is intended for research and analytical applications. Bakuchiol is a phytoestrogen that can be obtained from psoralen seeds. Bakuchiol has been proven to be a non-competitive inhibitor of multiple enzymes, including UDP-glucuronosyltransferase 2B7 (UGT2B7) and human carboxylesterase 2 (hCE2) , with IC50s values of 40.9 μM and 7.28 μM, respectively. Bakuchiol exhibits significant research and application potential in areas such as anti-inflammatory , antibacterial , antitumor therapies, as well as drug metabolism regulation.
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-
- HY-118084
-
|
Tyrene CR-4
|
JAK
Bcr-Abl
FLT3
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
LS-104 (Tyrene CR-4) is a non-ATP-competitive kinase inhibitor against JAK2, Bcr-Abl and FLT3. LS-104 potently induces apoptosis in JAK2V617F-positive cells and inhibits JAK2 autophosphorylation and downstream signal transduction. LS-104 also inhibits proliferation and induces potent cytotoxic effects in FLT3 expressing leukemic cells. LS-104 is a hydroxystyryl-acrylonitrile compound, which is promising for research of myeloproliferative disorders and refractory/relapsed hematologic malignancies .
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-
- HY-B0442BR
-
|
|
Endogenous Metabolite
Phosphodiesterase (PDE)
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil (hydrochloride trihydrate) (Standard) is the analytical standard of Vardenafil (hydrochloride trihydrate). This product is intended for research and analytical applications. Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes - .
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-
- HY-N1584BR
-
|
|
Calcium Channel
DNA/RNA Synthesis
Parasite
Sodium Channel
TGF-beta/Smad
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Halofuginone (hydrochloride) (Standard) is the analytical standard of Halofuginone (hydrochloride). This product is intended for research and analytical applications. Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects [4] .
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-
- HY-164685
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
T-0156 free base is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. T-0156 free base specifically inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) by PDE5 in a competitive manner (IC50=0.23 nM). T-0156 free base inhibits PDE6 (IC50=56 nM) and has low potencies against PDE1, PDE2, PDE3, and PDE4 (IC50>10 μM). T-0156 free base enhances the nitric oxide (NO)/cGMP pathway .
|
-
- HY-129907
-
|
2-Aminoethyl methylphosphonate
|
Others
|
Neurological Disease
|
|
2-AEMP (2-Aminoethyl methylphosphonate) is an anti-GABA(A)-ρ1 receptor compound with antagonist activity. 2-AEMP exhibits competitive inhibition compared to TPMPA with an IC(50) value of 18 μM, compared to 7 μM for TPMPA. The release rate of inhibition at termination of 2-AEMP is significantly higher than that of TPMPA. The preincubation time required for the onset of inhibition of 2-AEMP is much shorter than that of TPMPA. Some analogs of 2-AEMP, especially those with benzyl or n-butyl substituents, show lower potency in terms of biological activity .
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-
- HY-12215
-
|
PF-06463922
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Apoptosis
|
Cancer
|
|
Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
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-
- HY-103490
-
|
EDHS-206
|
MAP3K
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM) .
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-
- HY-112457
-
|
|
MAPKAPK2 (MK2)
|
Inflammation/Immunology
|
|
MK2-IN-3 hydrate (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2 (MK-2) inhibitor with an IC50 of 0.85 nM.MK2-IN-3 hydrate is exceptional selectivity against MK-3 (IC50=0.21 μM), MK-5 (IC50=0.081 μM), ERK2 (IC50=3.44 μM), MNK1(IC50=5.7 μM) as well as CDK2, JNK2, IKK2, MSK1, and MSK2 .
|
-
- HY-129636
-
|
(E)-GABAB receptor antagonist 1
|
GABA Receptor
ERK
|
Neurological Disease
|
|
CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor .
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-
- HY-133028
-
|
|
Casein Kinase
CDK
SGK
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
CKI-7 free base is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 free base is a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 free base has a much weaker effect on casein kinase II and other protein kinases .
|
-
- HY-121744
-
PS10
2 Publications Verification
|
PDHK
|
Inflammation/Immunology
|
|
PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM) . PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy .PDK: pyruvate dehydrogenase kinase
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-
- HY-101335
-
|
|
mGluR
|
Neurological Disease
|
|
DCG-IV is a potent agonist of group II mGluRs with EC50s of 0.35 and 0.09 μM for mGlu2R and mGlu3R, reapectively. DCG-IV is also a competitive antagonist at group I (IC50: mGlu1R/5R=389/630 μM) and III receptors (IC50: mGlu4R/6R/7R/8R= 22.5/39.6/40.1/32 μM). DCG-IV has anticonvulsive and neuroprotective effects .
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-
- HY-107522B
-
|
|
EAAT
|
Neurological Disease
|
|
DL-TBOA ammonium is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA ammonium inhibits the uptake of [ 14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA ammonium blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively .
|
-
- HY-N0215S11
-
|
(S)-2-Amino-3-phenylpropionic acid-13C9,15N
|
Calcium Channel
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Phenylalanine- 13C9, 15N is the 13C- and 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
|
-
- HY-N0215S14
-
|
(S)-2-Amino-3-phenylpropionic acid-15N,d8
|
Isotope-Labeled Compounds
Calcium Channel
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Phenylalanine- 15N,d8 is the deuterium and 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca2+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
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-
- HY-149008
-
|
|
Amylases
|
Metabolic Disease
Cancer
|
|
α-Amylase-IN-3 (Compound 4) is a none-competitive type of α-Amylase inhibitor with an IC50 value of 18.04 μM, which also has radical scavenging activities (DPPH and ABTS) with IC50 values of 16.04 μM (DPPH) and 16.99 μM (ABTS), respectively. α-Amylase-IN-3 has good protein–ligand interactions profile against α-Amylase. α-Amylase-IN-3 may have pharmacological activities such as anti-oxidative, anti-inflammatory inhibitory, which is helpful for the development of diabetes and oxidative stress associated disease .
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-
- HY-P5158
-
|
|
Adrenergic Receptor
|
Others
|
|
Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α1A-Adrenergic Receptor and α1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype and may provide useful information for the development of novel α1-Adrenergic Receptor subtype-selective drugs .
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-
- HY-155141
-
|
|
Cytochrome P450
|
Cancer
|
|
hCYP3A4-IN-1 (compound C6) is a potent, orally active hCYP3A4 inhibitor. hCYP3A4-IN-1 shows the IC50 values of 43.93 nM and 153.00 nM against hCYP3A4 in human liver microsomes (HLMs) and CHO-3A4 stably transfected cell line, respectively. hCYP3A4-IN-1 potently inhibits CYP3A4-catalyzed N-ethyl-1,8-naphthalimide (NEN) hydroxylation in a competitive manner (Ki = 30.00 nM) .
|
-
- HY-108601
-
|
|
PKC
|
Inflammation/Immunology
|
|
(S)-Ro 32-0432 free base is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of (S)-Ro 32-0432 free base for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. (S)-Ro 32-0432 free base is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 free base prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research .
|
-
- HY-157404
-
|
|
Pim
|
Cancer
|
|
Pim-1/2 kinase inhibitor 2 (compound 5b) is a competitive PIM-1 and PIM-2 kinase inhibitor with IC50s of 1.31 μM and 0.67 μM, respectively. Pim-1/2 kinase inhibitor 2 shows in-vitro low cytotoxicity against normal human lung fibroblast Wi-38 cell line and potent in-vitro anticancer activity against myeloid leukaemia (NFS-60), liver (HepG-2), prostate (PC-3), and colon (Caco-2) cancer cell lines .
|
-
- HY-N1584AR
-
|
|
DNA/RNA Synthesis
TGF-beta/Smad
Parasite
Sodium Channel
Calcium Channel
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Halofuginone (hydrobromide) (Standard) is the analytical standard of Halofuginone (hydrobromide). This product is intended for research and analytical applications. Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM . Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity . Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
|
-
- HY-121998
-
|
|
Aurora Kinase
|
Others
|
|
Binucleine 2 is an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki=0.36 μM), a kinase involved in cell division. It is specific for Drosophila Aurora B kinase, inhibiting it in a dose-dependent manner, with minimal inhibition of human or X. laevis Aurora B kinases at concentrations up to 100 μM. Binucleine 2 induces mitotic and cytokinesis defects in Drosophila Kc167 cells. It prevents Drosophila S2 cells from assembling a contractile ring during cell division when used at a concentration of 40 μM but does not affect ring ingression, suggesting that Aurora B kinase activity is not required for that step.
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-
- HY-15074
-
|
NS-1209
|
iGluR
|
Neurological Disease
|
|
SPD-502 is a novel glutamate antagonist with potential neuroprotective properties, particularly in brain ischemia. It selectively targets the AMPA receptor, showing high affinity (IC50 = 0.043 μM) and competitive inhibition of AMPA-induced effects in rat cortical membranes and cultured mouse cortical neurons. In vivo, SPD-502 effectively blocks AMPA-evoked spike activity in the hippocampus after intravenous administration, significantly increasing the seizure threshold in mice and demonstrating robust protection against ischemia-induced damage to hippocampal neurons in gerbils. These findings suggest SPD-502 may be promising for treating neurodegenerative conditions associated with glutamate excitotoxicity .
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- HY-13409B
-
|
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
|
SB 242084 monohydrochloride is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C receptor antagonist (crosses the blood-brain barrier). SB 242084 monohydrochloride increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 also increases mitochondrial gene expression and oxidative metabolism via 5-HT2A receptor. SB 242084 monohydrochloride has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage .
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-
- HY-135509
-
|
PF-06463922 acetate
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Apoptosis
|
Cancer
|
|
Lorlatinib (PF-06463922) acetate is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib acetate has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib acetate targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
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-
- HY-163879
-
|
|
Monoamine Oxidase
Reactive Oxygen Species
Ferroptosis
|
Neurological Disease
|
|
hMAO-B-IN-9 (Compound 25c) is a non-competitive inhibitor for monoamine oxidase B (MAO-B) with an IC50 of 1.58 µM (hMAO-B). hMAO-B-IN-9 forms complex with iron ions as a chelator, and inhibits Erastin (HY-15763)-induced ferroptosis. hMAO-B-IN-9 exhibits antioxidant activity by downregulating the level of reactive oxygen species (ROS). hMAO-B-IN-9 improves cognitive function in mice, without significant toxicity (30 mg/kg). hMAO-B-IN-9 is blood-brain barrier permeable, according to the in silico prediction .
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- HY-116973
-
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HIV
|
Infection
|
|
L-738372 is a non-competitive reversible inhibitor of HIV-1 reverse transcriptase (RT) with an inhibition constant (Ki) of 140 nM against dTTP. When combined with any nucleoside analogs (such as azidothymidine triphosphate, didexoyinosine triphosphate, or didexoycytidine triphosphate), L-738372 exhibits synergistic inhibition of RT activity. L-738372 has 2-3 times more inhibitory potency against the azidothymidine-resistant RT (D67N, K70R, T215Y, K219Q) compared to the wild-type RT. L-738372 holds promise for research in the field of HIV virus treatment .
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- HY-15076
-
|
NS-1209 sodium
|
iGluR
|
Neurological Disease
|
|
SPD-502 sodium is a novel glutamate antagonist with potential neuroprotective properties, particularly in brain ischemia. It selectively targets the AMPA receptor, showing high affinity (IC50 = 0.043 μM) and competitive inhibition of AMPA-induced effects in rat cortical membranes and cultured mouse cortical neurons. In vivo, SPD-502 sodium effectively blocks AMPA-evoked spike activity in the hippocampus after intravenous administration, significantly increasing the seizure threshold in mice and demonstrating robust protection against ischemia-induced damage to hippocampal neurons in gerbils. These findings suggest SPD-502 sodium may be promising for treating neurodegenerative conditions associated with glutamate excitotoxicity .
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- HY-N0226
-
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Cholinesterase (ChE)
Beta-secretase
|
Neurological Disease
Metabolic Disease
|
|
Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and can be used for the research of Alzheimer disease . Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberinecan be used for the research of diabetic disease .
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-
- HY-P1320
-
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Opioid Receptor
|
Inflammation/Immunology
|
|
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
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-
![[Nphe1]Nociceptin(1-13)NH2](//file.medchemexpress.eu/product_pic/hy-p1320.gif)
- HY-P1320A
-
|
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Opioid Receptor
|
Inflammation/Immunology
|
|
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2?binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
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-
![[Nphe1]Nociceptin(1-13)NH2 TFA](//file.medchemexpress.eu/product_pic/hy-p1320a.gif)
- HY-N0215S9
-
|
(S)-2-Amino-3-phenylpropionic acid-13C9,15N,d8
|
Isotope-Labeled Compounds
Calcium Channel
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Phenylalanine- 13C9, 15N,d8 is the deuterium, 13C-, and 15-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
|
-
- HY-137191
-
|
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EGFR
|
Cancer
|
|
CH7233163 is a noncovalent ATP-competitive inhibitor for EGFR-Del19/T790M/C797S. CH7233163 can overcome Osimertinib (HY-15772)-Resistant EGFR-Del19/T790M/C797S mutation. CH7233163 blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. CH7233163 has antitumor activities .
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-
- HY-B0267AR
-
|
|
mAChR
Potassium Channel
|
Neurological Disease
|
|
Oxybutynin (chloride) (Standard) is the analytical standard of Oxybutynin (chloride). This product is intended for research and analytical applications. Oxybutynin chloride is an oral active and competitive mAChR antagonist with Kis of 14.3 and 5.55 nM for specific [ 3H]NMS binding in the mouse bladder and cerebral cortex, respectively. Oxybutynin chloride inhibits vascular Kv channels in a manner independent of anticholinergic effect, with an IC50 value of 11.51 μM. Oxybutynin chloride reduces muscle spasm in the bladder and urinary tract, can be used in study of overactive bladder syndrome (OAB) . Oxybutynin (chloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-15346R
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
Copanlisib (Standard) is the analytical standard of Copanlisib. This product is intended for research and analytical applications. Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity .
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-
- HY-103151A
-
|
|
5-HT Receptor
|
Others
|
|
CP94253 is a selective, orally active agonist for serotonin receptor 1B (5-HT1B), through competitive binding with iodocyanopindolol (ICP) to the 5-HT1 receptor. CP94253 binds to the 5-HT1B, 5-HT1A, 5-HT1D, 5-HT1C and 5-HT2 receptors, with Kis of 2, 89, 49, 860 and 1600 nM. CP94253 causes satiety, anorexia, weight loss and hyperlocomotion in rats model .
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-
- HY-N0226A
-
|
|
Cholinesterase (ChE)
Beta-secretase
Reactive Oxygen Species
|
Neurological Disease
Metabolic Disease
|
|
Epiberberine chloride is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine chloride has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and may protect against Alzheimer disease . Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberine has the potential effect in the research of diabetic disease .
|
-
- HY-121638
-
|
|
Apoptosis
DGK
|
Inflammation/Immunology
Cancer
|
|
CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells .
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-
- HY-111388A
-
|
|
CDK
|
Cancer
|
|
SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50s of 4.4 nM and 10.4 nM, respectively, with a Kd of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC50=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726 . Has anti-tumor activity .
|
-
- HY-N5072
-
|
4',6,7-Trihydroxyisoflavone
|
CDK
PI3K
PKC
|
Cancer
|
|
Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities.
Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity . Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1) . Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes .
|
-
- HY-136265
-
|
|
Aminoacyl-tRNA Synthetase
|
Cancer
|
|
BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (Kd=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated?MTOR?mutants and the growth of rapamycin-resistant cancer cells.?BC-LI-0186 is a promising agent for lung cancer research .
|
-
- HY-12215R
-
|
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Apoptosis
|
Cancer
|
|
Lorlatinib (Standard) is the analytical standard of Lorlatinib. This product is intended for research and analytical applications. Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
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-
- HY-141635
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
cis-11,14-Eicosadienoic acid methyl ester is a more lipid soluble form of the ω-6 C20-2 fatty acid 11(Z),14(Z)-eicosadienoic acid, a naturally occurring PUFA. 11(Z),14(Z)-Eicosadienoic acid competitively inhibits inosine 5’-monophosphate dehydrogenase (Ki=3.1 μM) and inhibits the binding of LTB4 to its receptor on neutrophils (Ki=3.0 μM). Also, serum levels of eicosadienoic acids negatively correlate with degree of sleep disturbance.3 Eicosadienoic acids are converted by desaturases, in vivo, to eicosatrienoic acids, which are potent vasodilators.
|
-
- HY-117063
-
|
|
Others
|
Endocrinology
|
|
LEK 8841 methanesulfonate is a gastrointestinal calming agent with strong selective 5-HT2 receptor antagonist activity. The antipsychotic potential of LEK 8841 has made it the focus of research into alternative medicines. LEK 8841 behaves as a pure competitive antagonist in response to 5-HT and norepinephrine, with pA2 values of 7.93 and 6.45, respectively. The selectivity of LEK 8841 is better than that of the comparative drug ketanserin, making it an important reference value in corresponding receptor research. Studies related to structural modifications have shown that LEK 8841 exhibits high affinity for 5-HT2 receptors and low alpha-adrenergic receptor activity .
|
-
- HY-12583
-
A-366
3 Publications Verification
|
Histone Methyltransferase
Epigenetic Reader Domain
|
Cancer
|
|
A-366 is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families .
|
-
- HY-P0299A
-
|
|
TGF-β Receptor
|
Cancer
|
|
LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier .
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-
- HY-120877
-
|
|
MARK
Salt-inducible Kinase (SIK)
AMPK
Apoptosis
|
Cancer
|
|
MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively . MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells . MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370 .
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-
- HY-P0299
-
|
|
TGF-β Receptor
|
Cancer
|
|
LSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) can readily crosse the blood-brain barrier .
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-
- HY-145836
-
|
|
FGFR
|
Cancer
|
|
FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4 V550L, FGFR4 V550M and FGFR4 C552S with IC50s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model .
|
-
- HY-108548
-
|
Rp-8-Bromo-PET-cGMPS
|
Others
|
Inflammation/Immunology
|
|
Rp-8-bromo-PET-Cyclic GMPS (Rp-8-bromo-PET-cGMPS) is an analog of cyclic GMP (cGMP). It is a cell permeable, competitive, and reversible inhibitor of cGMP-dependent protein kinases (cGKs) that blocks activation of cGKI and cGKII by cGMP (Kis=35 and 30 nM). It less potently inhibits protein kinase A (Ki=11 μM) and cGMP-induced activation of cyclic nucleotide-gated channels (IC50=25 μM). In the absence of cGMP stimulation, Rp-8-bromo-PET-cGMPS can act as a partial agonist of cGKI (Ki=1 μM). Rp-8-bromo-PET-cGMPS is resistant to hydrolysis by phosphodiesterase 11.
|
-
- HY-117747
-
|
JCR 424; XM 323
|
HIV Protease
|
Infection
|
|
DMP 323 is a potent, nonpeptide cyclic urea inhibitor of HIV protease, effective against both HIV type 1 and type 2. Designed using structural information and database searching, it competitively inhibits the cleavage of both peptide and HIV-1 gag polyprotein substrates. DMP 323 shows comparable potency to other highly effective HIV protease inhibitors like A-80987 and Ro-31-8959. Importantly, its efficacy against HIV protease remains unaffected by human plasma or serum, suggesting low affinity for plasma proteins. Furthermore, DMP 323 demonstrates minimal inhibition of various mammalian proteases at concentrations much higher than those needed for HIV protease inhibition, highlighting its specificity for viral targets .
|
-
- HY-10450AR
-
|
|
SGLT
|
Metabolic Disease
Cancer
|
|
Dapagliflozin ((2S)-1,2-propanediol, hydrate) (Standard) is the analytical standard of Dapagliflozin ((2S)-1,2-propanediol, hydrate). This product is intended for research and analytical applications. Dapagliflozin ((2S)-1,2-propanediol, hydrate) is the S-enantiomer of Dapagliflozin 1,2-propanediol, hydrate. Dapagliflozin ((2S)-1,2-propanediol, hydrate), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin ((2S)-1,2-propanediol, hydrate) induces HIF1 expression and attenuates renal IR injury .
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-
- HY-19633A
-
|
|
Others
|
Neurological Disease
|
|
CS-003 is a triple neurokinin receptor antagonist with activity in inhibiting neurokinin-related respiratory diseases. CS-003 exhibits high affinity for human neurokinin 1, 2 and 3 receptors, withKi values of 2.3 nM, 0.54 nM and 0.74 nM respectively. The Ki values of CS-003 on the guinea pig neurokinin receptor are 5.2 nM, 0.47 nM and 0.71 nM respectively, showing superior inhibitory effect. CS-003 significantly inhibits the formation of inositol phosphate involving substance P, neurokinin A and neurokinin B through competitive antagonism. CS-003 significantly inhibits citric acid-induced cough, and its effect is better than other selective neurokinin receptor antagonists .
|
-
- HY-B1311
-
|
SKF-525A; U-5446; RP-5171
|
Cytochrome P450
Monoamine Oxidase
Bcl-2 Family
Survivin
PARP
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC50 value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases .
|
-
- HY-N1957
-
|
γ-Mangostin
|
5-HT Receptor
COX
Transthyretin (TTR)
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer . Gamma-Mangostin inhibits [3 H] spiperone binding to cultured rat aortic myocytes (IC50=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC50=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .
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-
- HY-120877A
-
|
|
MARK
Salt-inducible Kinase (SIK)
AMPK
Apoptosis
|
Cancer
|
|
(R)-MRT199665 is an isomer of MRT199665 (HY-120877). MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370 .
|
-
- HY-161449
-
|
|
11β-HSD
|
Metabolic Disease
|
|
JTT-654 is an orally active, potent and selective11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. The IC50 of JTT-654 for 11β-HSD1 is 4.65, 0.97, and 0.74 nM in human, rat, and mouse recombinant enzymes, respectively. JTT-654 showed competitive inhibition against human recombinant enzyme. The IC50 value for human 11β-HSD2 is > 30 μM (human 11β-HSD2 is responsible for the reverse reaction against human 11β-HSD1). JTT-654 ameliorates insulin resistance and non-obese type 2 diabetes by inhibiting adipose tissue and liver 11β-HSD1 .
|
-
- HY-A0139
-
|
NSC 108165; Navan; Navane
|
Others
|
Others
|
|
Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
|
-
- HY-19261
-
|
|
Others
|
Metabolic Disease
|
|
T-0632 is a CCK A receptor antagonist that exhibits significant pharmacological properties in in vitro studies. T-0632 competitively inhibits the binding of [125I]CCK-8 to rat pancreatic CCK A receptors with a K_i value of 0.24 nM, which is significantly lower than the K_i value for guinea pig CCK B receptors. T-0632 has higher selectivity in inhibiting CCK-8-stimulated pancreatic enzyme release, with an IC_50 value of 5.0 nM, which is more advantageous than L-364,718 and loxiglumide. In rabbit gallbladder smooth muscle, the antagonistic effects of T-0632 and loxiglumide are reversible, while L-364,718 shows a persistent inhibitory effect. These results indicate that T-0632 is a highly potent, reversible and more selective CCK A receptor antagonist.
|
-
- HY-164393
-
|
|
JAK
Bcr-Abl
Apoptosis
|
Cancer
|
|
ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC50s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2 V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the BCR-ABL kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling .
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-
- HY-B1311R
-
|
|
Cytochrome P450
Monoamine Oxidase
Bcl-2 Family
Survivin
PARP
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Proadifen (hydrochloride) (Standard) is the analytical standard of Proadifen (hydrochloride). This product is intended for research and analytical applications. Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC50 value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases [4] .
|
-
- HY-123597
-
|
DDUG; NCI C04808
|
Others
|
Cancer
|
|
NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
|
-
- HY-N1957R
-
|
|
5-HT Receptor
COX
Transthyretin (TTR)
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Gamma-Mangostin (Standard) is the analytical standard of Gamma-Mangostin. This product is intended for research and analytical applications. Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer . Gamma-Mangostin inhibits [3H] spiperone binding to cultured rat aortic myocytes (IC50=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC50=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .
|
-
- HY-30004
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
1-Aminocyclopropane-1-carboxylic acid is an endogenous metabolite. In the presence of low concentrations (1 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a small molecule agonist of NMDA receptors with an EC50 of 0.7-0.9 μM. At high concentrations (10 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a competitive antagonist of NMDA receptors with an EC50 of 81.6 nM. 1-Aminocyclopropane-1-carboxylic acid exerts neuroprotective activity by moderately activating NMDA receptors to prevent neuronal cell death in ischemic animal models. Additionally, 1-Aminocyclopropane-1-carboxylic acid is an antagonist of NMDA receptors, inducing blood pressure reduction and antioxidant effects in stroke-prone hypertensive rats. 1-Aminocyclopropane-1-carboxylic acid enhances object recognition memory and cognitive flexibility dependent on the prefrontal cortex, but does not affect impulsivity nor exhibit an antipsychotic-like profile. 1-Aminocyclopropane-1-carboxylic acid shows promise for research in the field of neurotoxicity. .
|
-
- HY-118156
-
|
|
Others
|
Others
|
|
L-699333 is a 5-lipoxygenase (5-LO) inhibitor belonging to the thieno[2,3,4-cd]indole class. This compound has a 2-ethoxybutyric acid side chain and is a potent inhibitor of the biosynthesis of 5-HPETE and LTB4 produced from human 5-LO, with ICm values of 22 nM, 7 nM, and 3.8 pM for human neutrophils and whole blood, respectively. L-699333 has shown anti-inflammatory and antiasthmatic effects in a variety of animal models, including rat pleurisy models, antigen-induced wheezing models, and awake macaque and sheep asthma models. Its inhibition of 5-LO is highly selective, with higher ICm values or stronger competitive inhibition in FLAP binding assays compared to inhibition of human 15-LO, porcine 12-LO, and ram epididymal cyclooxygenase. The racemic enantiomer 14g of L-699333 is the most potent enantiomer to date, with inhibitory effects similar to those of the known MK-0591, which has been shown in clinical trials to inhibit the biochemical effects of LTB4 biosynthesis in vitro and LTE4 excretion in urine.
|
-
- HY-117811
-
|
L-680574
|
Others
|
Others
|
|
(R,R)-MK 287 is a tetrahydrofuran derivative that effectively inhibits the binding of [3H]C18-PAF to human platelets, polymorphonuclear leukocytes (PMNs), and lung membranes with K1 values of 6.1 ± 1.5, 3.2 ± 0.7, and 5.49 ± 2.3 nM, respectively. The inhibition is stereospecific and competitive. Its racemate, L-668,750, is less potent, and its enantiomer, L-680574, is only 1/20 as potent as MK 287. MK 287 inhibits the binding of [3H]C18-PAF to human PMN membranes, reducing the affinity of the radioligand without changing the number of receptor sites. The binding of other radioligands (e.g., LTB4, LTC4, C5a, FMLP) to their specific receptors is unchanged at 1-10 microM MK 287. [3H]MK 287 binds to human platelet and PMN membranes with KD values of 2.1 ± 0.6 and 2.9 ± 1.2 nM. When tested on isolated human cells, MK 287 potently and selectively inhibits PAF-induced platelet aggregation (ED50 = 56 ± 38 nM or ED50 = 1.5 ± 0.5 nM for gel-filtered platelets) and elastase release from PMNs (ED50 = 4.4 ± 2.6 nM). In vivo studies, MK 287 inhibited PAF-induced lethality in mice (ED50 = 0.8 mg/kg oral) and PAF-induced bronchospasm in guinea pigs (ED50 = 0.18 mg/kg intraduodenally and 0.19 mg/kg intravenously). The inhibition of PAF-induced bronchospasm was accompanied by a rightward shift in the concentration-response curve for PAF-induced platelet aggregation measured in vitro.
|
-
-
-
HY-L0123V
-
|
|
30,300 compounds
|
|
The incidence and significance of central nervous system diseases are increasing at an alarming rate all over the world. Although substantial research efforts have been applied to develop new CNS-active drugs, only a few CNS disorders are addressed satisfactorily, while the remaining ones pose significant clinical challenges. Blood-brain barrier (BBB) permeability is one of the most important limiting factors in the design and development of novel CNS-targeted pharmaceuticals for the treatment of neurological disorders.
Carefully selected from the HTS Compound Collection to meet the parameters optimized for high BBB-permeability, our CNS Focused Screening Library comprising over 30,300 structurally-diverse and potentially CNS-active screening compounds. This original Screening Compound Library is aimed at supporting CNS drug design projects and HTS efforts in search for novel neurotherapeutics.
|
-
-
HY-L158
-
|
|
4,617 compounds
|
|
According to reports, most known kinase inhibitors exert their effects through competitive binding in highly conserved ATP pockets. Although genetic techniques such as RNA interference can inactivate specific genes, most kinases are multi domain proteins, each of which has an independent function. Highly selective inhibitors have higher efficiency than non-selective inhibitors, and the selectivity to the target is at least 100 times higher. Therefore, ensuring the validation of targets with the most selective inhibitors is crucial for a more thorough understanding of the pharmacology of the kinase field. The Highly Selective Inhibitors Library contains 4,617 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Inhibitors Library is an effective tool for screening different phenotypes
|
| Cat. No. |
Product Name |
Type |
-
- HY-D0145
-
|
Resorufin ethyl ether
|
Chromogenic Substrates
|
|
7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase .
|
-
- HY-D1594
-
|
|
Fluorescent Dyes/Probes
|
|
BODIPY TR Cadaverine, a cadaverine derivative, is a red fluorescent dye. BODIPY TR Cadaverine can be used in a a highly sensitive and robust fluorescent displacement assay, which binds to native LPS strongly, specifically recognizing lipid A, and is competitively displaced by compounds displaying an affinity for lipid A .
|
-
- HY-15141G
-
|
Antibiotic AM-2282 (GMP); STS (GMP); AM-2282 (GMP)
|
Fluorescent Dye
|
|
Staurosporine (AM-2282) (GMP) is Staurosporine (HY-15141) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Staurosporine is a potent, ATP-competitive and non-selective inhibitor of protein kinases .
|
-
- HY-D0939
-
|
Chicago Sky Blue 6B
|
Dyes
|
|
Direct Blue 1 (Chicago Sky Blue 6B) is a complex dye for background autofluorescence in immunofluorescence histochemistry. Direct Blue 1 is a potent and competitive VGLUT inhibitor. Direct Blue 1 can inhibit the Aβ-binding small molecule PrP ligand. Direct Blue 1 has anti-inflammatory activity .
|
-
- HY-10583G
-
|
|
Fluorescent Dye
|
|
Y-27632 dihydrochloride (GMP) is the GMP level of Y-27632 dihydrochloride (HY-10583). GMP guidelines are used to produce Y-27632 dihydrochloride (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor with antiepileptic effect .
|
-
- HY-D1493
-
|
|
Fluorescent Dyes/Probes
|
|
FIM-1 is a fluorescent PKC (protein kinase C) probe that can be used for mitochondrial staining. FIM-1 inhibits PKC and acts as ATP-competitive catalytic site inhibitor .
|
-
- HY-10254G
-
|
PD0325901 (GMP); PD325901 (GMP)
|
Fluorescent Dye
|
|
Mirdametinib (PD0325901) (GMP) is Mirdametinib (HY-10254) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Mirdametinib is an orally active, selective and non-ATP-competitive MEK inhibitor .
|
-
- HY-13418G
-
|
Compound C dihydrochloride (GMP); BML-275 dihydrochloride (GMP)
|
Fluorescent Dye
|
|
Dorsomorphin dihydrochloride (GMP) is the GMP level of Dorsomorphin dihydrochloride (HY-13418). GMP guidelines are used to produce Dorsomorphin dihydrochloride (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. Dorsomorphin dihydrochloride (GMP) is a potent, selective and ATP-competitive AMPK inhibitor. Dorsomorphin dihydrochloride (GMP) can be used for the research of induced differentiation of pluripotent stem cells (PSCs) .
|
-
- HY-B0377G
-
|
MK-208 (GMP)
|
Fluorescent Dye
|
|
Famotidine GMP (MK-208 GMP) is Famotidine (HY-B0377) produced in GMP guideline. Famotidine GMP is a competitive histamine H2-receptor antagonist, inhibits gastric secretion, activates the gastric mucosal defensive mechanisms. Famotidine GMP ameliorates peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD/GORD) in rats model .
|
| Cat. No. |
Product Name |
Type |
-
- HY-126388
-
|
|
Enzyme Substrates
|
|
Trypsin Inhibitor, soybean is a potent and reversible inhibitor of trypsin .
|
-
- HY-126306
-
-
- HY-W087937
-
|
Benzenecarboximidamide hydrochloride hydrate
|
Biochemical Assay Reagents
|
|
Benzamidine (Benzenecarboximidamide) hydrochloride hydrate is a reversible competitive trypsin-like serine proteases inhibitor with Kis of 20, 21, 97, 110, 320 and 750 μM against Tryptase, Trypsin, uPA, Factor Xa, Thrombin and tPA, respectively .
|
-
- HY-15141G
-
|
Antibiotic AM-2282 (GMP); STS (GMP); AM-2282 (GMP)
|
Biochemical Assay Reagents
|
|
Staurosporine (AM-2282) (GMP) is Staurosporine (HY-15141) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Staurosporine is a potent, ATP-competitive and non-selective inhibitor of protein kinases .
|
-
- HY-15908
-
BCA
5 Publications Verification
Disodium bicinchoninate
|
Biochemical Assay Reagents
|
|
BCA (Disodium bicinchoninate) is an orally active and non-competitive Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 value of 28 µM, a Ki value of 43 µM. BCA shows anticancer activity. BCA has the potential for the research of Alzheimer's disease (AD) .
|
-
- HY-128466
-
|
|
Biochemical Assay Reagents
|
|
N-Biotinyl-L-cysteine is a biotinylated biochemical assay reagent, which is used to detect avidin and biotin through a competitive binding reaction .
|
-
- HY-118563
-
|
|
Biochemical Assay Reagents
|
|
S-Farnesyl thioacetic acid is an analog of S-farnesyl cysteine, which is a prenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase) competitive inhibitors. It also inhibits the methylation of farnesylated and geranylgeranylated substrates.
|
-
- HY-W039920
-
|
β-D-Galactosylamine, 98%
|
Carbohydrates
|
|
1-Amino-1-deoxy-β-D-galactose, 98% is a galactose analog used as a competitive inhibitor to aid in the separation, purification, identification, differentiation, and characterization of β-D-galactosidase and galactose oxidase.
|
-
- HY-134438
-
|
|
Enzyme Substrates
|
|
Hexanoyl coenzyme A trilithium is a hexanoyl-based medium-chain fatty acyl coenzyme A that is present in all organisms. Hexanoyl coenzyme A trilithium can be used as a precursor for cannabinoid biosynthesis and acts as a competitive inhibitor of medium-chain acyl coenzyme A dehydrogenase (MCAD) .
|
-
- HY-10254G
-
|
PD0325901 (GMP); PD325901 (GMP)
|
Biochemical Assay Reagents
|
|
Mirdametinib (PD0325901) (GMP) is Mirdametinib (HY-10254) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Mirdametinib is an orally active, selective and non-ATP-competitive MEK inhibitor .
|
-
- HY-B1295
-
|
Litarex tetrahydrate
|
Biochemical Assay Reagents
|
|
Lithium citrate (Litarex) tetrahydrate is the major active ingredient of Garcinia cambogia. Lithium citrate tetrahydrate competitively inhibits ATP citrate lyase with weight loss benefits. Lithium citrate tetrahydrate effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects .
|
-
- HY-13418G
-
|
Compound C dihydrochloride (GMP); BML-275 dihydrochloride (GMP)
|
Biochemical Assay Reagents
|
|
Dorsomorphin dihydrochloride (GMP) is the GMP level of Dorsomorphin dihydrochloride (HY-13418). GMP guidelines are used to produce Dorsomorphin dihydrochloride (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. Dorsomorphin dihydrochloride (GMP) is a potent, selective and ATP-competitive AMPK inhibitor. Dorsomorphin dihydrochloride (GMP) can be used for the research of induced differentiation of pluripotent stem cells (PSCs) .
|
-
- HY-10583G
-
|
|
Biochemical Assay Reagents
|
|
Y-27632 dihydrochloride (GMP) is the GMP level of Y-27632 dihydrochloride (HY-10583). GMP guidelines are used to produce Y-27632 dihydrochloride (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor with antiepileptic effect .
|
-
- HY-B0377G
-
|
MK-208 (GMP)
|
Biochemical Assay Reagents
|
|
Famotidine GMP (MK-208 GMP) is Famotidine (HY-B0377) produced in GMP guideline. Famotidine GMP is a competitive histamine H2-receptor antagonist, inhibits gastric secretion, activates the gastric mucosal defensive mechanisms. Famotidine GMP ameliorates peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD/GORD) in rats model .
|
-
- HY-W097792
-
|
5'-O-DMT-dU
|
Gene Sequencing and Synthesis
|
|
5'-O-(4,4'-Dimethoxytrityl)-2'-deoxyuridine (5'-O-DMT-dU) is a competitive inhibitor of E. coli dUTP nucleotidohydrolase (dUTPase), with the Ki higher than 1000 μM. 5'-O-(4,4'-Dimethoxytrityl)-2'-deoxyuridine can be used in machine-assisted DNA synthesis by synthesizing nucleosidic phosphoramidite blocks .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1292
-
|
|
PKG
|
Cancer
|
|
PKG inhibitor peptide is an ATP-competitive inhibitor of cGMP-dependent protein kinase (PKG), with a Ki of 86 μM .
|
-
- HY-P1294
-
|
|
CRFR
|
Neurological Disease
|
|
α-Helical CRF(9-41) is a competitive CRF2 receptor antagonist with KB of ~100 nM. α-Helical CRF(9-41) is also a partial agonist of CRF1 receptor with an EC50 of 140 nM .
|
-
- HY-P1294A
-
|
|
CRFR
|
Neurological Disease
|
|
α-Helical CRF(9-41) TFA is a competitive CRF2 receptor antagonist with KB of ~100 nM. α-Helical CRF(9-41) TFA is also a partial agonist of CRF1 receptor with an EC50 of 140 nM .
|
-
- HY-P0222
-
|
|
PKA
|
Others
|
|
PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor .
|
-
- HY-P1299A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect .
|
-
- HY-P2026
-
|
|
Peptides
|
Cardiovascular Disease
|
|
A 71915 is a highly potent and competitive natriuretic peptide receptor A (ANP, NPRA) antagonist (pKi= 9.18). A 71915 displaces [ 125I]ANP dose dependently, with a Ki of 0.65 nM. A71915( pA2= 9.48) against rat ANP-induced cGMP production in NB-OK-1 cells .
|
-
- HY-P3786
-
|
|
PKA
PKC
|
Cancer
|
|
H-Arg-Gly-Tyr-Ala-Leu-Gly-OH is a competitive and CAMP dependent protein kinase inhibitor .
|
-
- HY-P0222A
-
|
|
PKA
|
Others
|
|
PKI(5-24) TFA is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) TFA corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor .
|
-
- HY-P1299
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 is a potent, selective, and competitive antagonist of the NOP receptor, with a pKi of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 shows antidepressant-like effect .
|
-
- HY-164388
-
|
|
Caspase
Apoptosis
Autophagy
Necroptosis
|
Cardiovascular Disease
Cancer
|
|
Z-VAD is a competitive, irreversible pan-caspase inhibitor. Z-VAD inhibits all 10 caspases, except for caspase-2 which is only weakly inhibited. Z-VAD decreases radiation-induced apoptosis. Z-VAD induces both autophagy and necrosis in irradiated MDA-MB-231 and H460 mouse xenografts. Z-VAD with radiation produces a significant tumor growth delay and shows dramatic antiangiogenic effect in cancer xenograft .
|
-
- HY-W142169
-
|
Formyl-L-histidine
|
Peptides
|
Others
|
|
N-Formyl-L-histidine shows binding affinity to histidyl-tRNA synthetase with a Ki value of 4.6 μM. N-Formyl-L-histidine shows a competitive inhibition against L-histidine ammonia-lyase, inhibits urocanic acid formation from L-histidine with a Ki value of 4.26 mM .
|
-
- HY-P3245
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-P3245A
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 hydrochloride is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 hydrochloride antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 hydrochloride selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-103282
-
|
|
Bombesin Receptor
|
Others
|
|
[D-Phe12]-Bombesin is a derivative of Bombesin (HY-P0195) and an antagonist for bombesin receptor with Ki of 4.7 μM. [D-Phe12]-Bombesin inhibits the Bombesin (HY-P0195)-induced amylase release, with IC50 of 4 μM .
|
-
- HY-P10552
-
|
|
CXCR
|
Inflammation/Immunology
|
|
pCXCL8-1aa is an anti-inflammatory peptide. pCXCL8-1aa competitively inhibits the binding of CXCL8 to glycosaminoglycans such as heparin sulfate (HS) by binding with high affinity. This reduces the presentation of CXCL8 on the surface of vascular endothelial cells, thereby inhibiting neutrophil migration and inflammatory responses. pCXCL8-1aa can be used to study inflammatory diseases such as rheumatoid arthritis .
|
-
- HY-P3678
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Neuropeptide Y (18-36) (porcine) is a competitive neuropeptide Y (NPY) cardiac receptor antagonist. Neuropeptide Y (18-36) (porcine) inhibits the binding of I-NPY to cardiac ventricular membranes in a concentration-dependent manner with an IC50 value of 158 nM and an Ki value of 140 nM. Neuropeptide Y (18-36) (porcine) can be used for the research of congestive heart failure .
|
-
- HY-P2625
-
|
|
GCGR
|
Metabolic Disease
|
|
GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC50=5.8 nM) .
|
-
- HY-P2625S1
-
|
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
|
GLP-2(3-33) (Leu- 13C6, 15N) TFA is 13C and 15N labeled GLP-2(3-33) (HY-P2625). GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC50=5.8 nM).
|
-
- HY-P2625S
-
|
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
|
GLP-2(3-33) (Leu- 13C6, 15N) is 13C and 15N labeled GLP-2(3-33) (HY-P2625). GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC50=5.8 nM).
|
-
- HY-P4543
-
-
- HY-P10657
-
-
- HY-P5188A
-
-
- HY-P1292A
-
|
|
PKG
|
Cancer
|
|
PKG inhibitor peptide TFA is an ATP-competitive inhibitor of cGMP-dependent protein kinase (PKG), with a Ki of 86 μM .
|
-
- HY-B0686
-
|
|
Integrin
|
Cardiovascular Disease
|
|
Eptifibatide is a cyclic heptapeptide, acts as a competitive antagonist for the activated platelet glycoprotein IIb/IIIa receptor, with anti-platelet activity .
|
-
- HY-P1017
-
-
- HY-P1315
-
|
Glycylglycyl-L-tyrosyl-L-arginine
|
Cathepsin
|
Others
|
|
Papain inhibitor (Glycylglycyl-L-tyrosyl-L-arginine) acts as an effective competitive inhibitor to papain, with a Ki of 9 μM at pH 6.2 .
|
-
- HY-P0177
-
-
- HY-B0686A
-
|
|
Integrin
|
Cardiovascular Disease
|
|
Eptifibatide monoacetate is a cyclic heptapeptide, acts as a competitive antagonist for the activated platelet glycoprotein IIb/IIIa receptor, with anti-platelet activity .
|
-
- HY-P2271
-
|
|
Apelin Receptor (APJ)
|
Cancer
|
|
MM 54 (compound 5) is a competitive antagonist at APJ, with an IC50 of 93 nM. MM 54 behaves as a potent and selective inhibitor of apelin binding and APLNR activation .
|
-
- HY-16168B
-
|
FE 200486 acetate hydrate
|
GnRH Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
Degarelix acetate hydrate (FE 200486 acetate hydrate) is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix acetate hydrate can be used for prostate cancer research .
|
-
- HY-P1083
-
|
|
Dynamin
|
Neurological Disease
|
|
Dynamin inhibitory peptide competitively blocks binding of dynamin to amphiphysin, thus preventing endocytosis. Dynamin inhibitory peptide blocks the dopamine D3 effect on GABAA receptors .
|
-
- HY-P1628
-
|
|
GnRH Receptor
|
Metabolic Disease
|
|
Ganirelix is a competitive and selective gonadotropin releasing hormone (GnRH) antagonist. Ganirelix prevents endogenous GnRH from inducing luteinising hormone (LH) and follicle stimulating hormone relea .
|
-
- HY-P1264F1
-
|
|
nAChR
|
Neurological Disease
|
|
Biotin-α-Bungarotoxin is the Biotin labelled α-Bungarotoxin (HY-P1264). α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs) .
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- HY-P10278
-
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Peptides
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Endocrinology
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Anantin binds competitively to the receptor of atrial natriuretic factor (ANF) from bovine adrenal cortex (Kd = 0.6 μM) and acts as natriuretic peptide receptor A antagonist .
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-
- HY-P1083A
-
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Dynamin
|
Neurological Disease
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|
Dynamin inhibitory peptide TFA competitively blocks binding of dynamin to amphiphysin, thus preventing endocytosis. Dynamin inhibitory peptide TFA blocks the dopamine D3 effect on GABAA receptors .
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-
- HY-W013407
-
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Peptides
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Neurological Disease
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α-Methyltyrosine methyl ester hydrochloride is a competitive tyrosine hydroxylase inhibitor that inhibits the conversion of tyrosine to dopamine. α-Methyltyrosine methyl ester hydrochloride can be used as a tool for sympathetic nervous system research .
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- HY-P4633
-
|
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Dipeptidyl Peptidase
|
Metabolic Disease
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|
γ-Glu-Tyr, a competitive inhibitor of dipeptidyl peptidase-IV (DPP-IV) (IC50=6.77 mM), is a potentially functional component of the type 2 diabetes diet .
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-
- HY-P1264F
-
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nAChR
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Neurological Disease
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α-Bungarotoxin, FITC labeledis the FITC labelled α-Bungarotoxin (HY-P1264). α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs) .
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- HY-17572
-
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RW22164; RWJ22164
|
Oxytocin Receptor
Vasopressin Receptor
|
Endocrinology
Cancer
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Atosiban (RW22164; RWJ22164) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research .
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- HY-17572A
-
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RW22164 acetate; RWJ22164 acetate
|
Oxytocin Receptor
Vasopressin Receptor
|
Endocrinology
Cancer
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Atosiban acetate (RW22164 acetate;RWJ22164 acetate) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research .
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-
- HY-105173
-
|
EP 24332
|
GnRH Receptor
Histamine Receptor
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Endocrinology
Cancer
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|
Teverelix (EP 24332) is a GnRH antagonist. Teverelix binds competitively and reversibly to GnRH receptors, thereby suppressing the release of LH and FSH. Teverelix can be used in the research of prostatic hyperplasia, endometriosis, and prostate cancer .
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-
- HY-P3853
-
|
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Neurokinin Receptor
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Neurological Disease
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GR 87389 is a potent NK2 receptor antagonist. GR 87389 antagonized GA 64349-induced smooth muscle strips contractions in a competitive manner in the human detrusor, prostate and prostatic urethra .
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-
- HY-P4270
-
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Peptides
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Neurological Disease
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Met-Arg-Phe-Ala is a peptide. Met-Arg-Phe-Ala also is a potent competitive inhibitor for enkephalin-generating endopeptidase (EGE). Met-Arg-Phe-Ala can be used for the research of neurological disease .
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-
- HY-16168AR
-
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GnRH Receptor
Apoptosis
|
Endocrinology
Cancer
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Degarelix (Standard) is the analytical standard of Degarelix. This product is intended for research and analytical applications. Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix can be used for prostate cancer research .
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-
- HY-111173
-
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Dipeptidyl Peptidase
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Others
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Diprotin B is a dipeptidyl aminopeptidase IV (DPP IV) inhibitor. The apparent competitive inhibition of DPP-IV by the diprotins is a kinetic artifact, derived from the substrate-like nature of tripeptides containing a penultimate proline residue .
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-
- HY-P3808
-
-
- HY-P0322
-
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EMD 56574
|
Integrin
|
Cardiovascular Disease
Metabolic Disease
|
|
GRGDSPK (EMD 56574) is a peptide incluing Arg-Gly-Asp (RGD). GRGDSPK (EMD 56574) is an competitive and reversible inhibitory peptide for inhibiting integrin-fibronectin binding. GRGDSPK is used to study the role of integrins in bone formation and resorption .
|
-
- HY-P0319
-
|
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Peptides
|
Others
|
|
3X FLAG peptides are FLAG-tagged peptides containing three repeats of the Asp-Tyr-Lys-Xaa-Xaa-Asp motif. 3X FLAG peptide can be used for protein separation and purification, and competitive elution with target proteins.
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-
- HY-P2333
-
|
|
Peptides
|
Cardiovascular Disease
|
|
LCKLSL is a N-terminal hexapeptide and a competitive annexin A2 (AnxA2) inhibitor. LCKLSL potently inhibits the binding of tissue plasminogen activator (tPA) to AnxA2. LCKLSL also inhibits the generation of plasmin and has anti-angiogenic roles .
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-
- HY-P2333A
-
|
|
Peptides
|
Cardiovascular Disease
|
|
LCKLSL hydrochloride is a N-terminal hexapeptide and a competitive annexin A2 (AnxA2) inhibitor. LCKLSL hydrochloride potently inhibits the binding of tissue plasminogen activator (tPA) to AnxA2. LCKLSL hydrochloride also inhibits the generation of plasmin and has anti-angiogenic roles .
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- HY-P5427
-
|
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Peptides
|
Others
|
|
EAC3I is a biological active peptide. (The autocamtide-3 derived inhibitory peptide (EAC3I) sequence (KKALHRQEAVDAL) mimics the autoinhibitory region of the CaMKII regulatory domain (residues 278–290) and acts by competitively binding to the catalytic site.)
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- HY-P0319A
-
|
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Peptides
|
Others
|
|
3X FLAG peptide TFA is a FLAG-tagged peptide containing three repeats of the Asp-Tyr-Lys-Xaa-Xaa-Asp motif. 3X FLAG peptide TFA can be used for protein separation and purification, and competitive elution with target proteins.
|
- HY-P0322A
-
|
EMD 56574 TFA
|
Integrin
|
Cardiovascular Disease
Metabolic Disease
|
|
GRGDSPK TFA (EMD 56574 TFA) is a peptide incluing Arg-Gly-Asp (RGD). GRGDSPK TFA is an competitive and reversible inhibitory peptide for inhibiting integrin-fibronectin binding. GRGDSPK TFA is used to study the role of integrins in bone formation and resorption .
|
- HY-P1271
-
|
|
nAChR
|
Cardiovascular Disease
|
|
Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
|
- HY-13634B
-
- HY-P0027
-
|
|
Arp2/3 Complex
Fungal
|
Infection
Cancer
|
|
Jasplakinolide is a potent actin polymerization inducer and stabilizes pre-existing actin filaments. Jasplakinolide binds to F-actin competitively with phalloidin with a Kd of 15 nM. Jasplakinolide, a naturally occurring cyclic peptide from the marine sponge, has both fungicidal and anti-cancer activity .
|
- HY-P1376
-
|
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
- HY-P1293
-
|
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iGluR
|
Neurological Disease
|
|
Conantokin G, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G has neuroprotective properties .
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- HY-P1694
-
|
|
Bradykinin Receptor
|
Cardiovascular Disease
|
|
B4148 is a selective competitive bradykinin (BK) antagonist that significantly inhibits BK-induced hypotension in rats. In a rat model of endotoxin shock induced by Escherichia coli lipopolysaccharide, B4148 significantly attenuated the decrease in mean arterial blood pressure compared with the control group .
|
- HY-P1271A
-
|
|
nAChR
|
Cardiovascular Disease
|
|
Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
|
- HY-100047
-
|
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Taste Receptor
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Others
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|
Nα,Nα-Bis(carboxymethyl)-L-lysine is a competitive inhibitor of bitter taste receptor 4, with an IC50 of 59 nM. Nα,Nα-Bis(carboxymethyl)-L-lysine can be used in bitter receptors related study .
|
- HY-17572R
-
|
|
Oxytocin Receptor
Vasopressin Receptor
|
Endocrinology
Cancer
|
|
Atosiban (Standard) is the analytical standard of Atosiban. This product is intended for research and analytical applications. Atosiban (RW22164; RWJ22164) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research .
|
- HY-P4522
-
|
|
Endogenous Metabolite
|
Others
|
|
Bz-Ala-Arg is a dipeptide. Bz-Ala-Arg is also a spectrophotometric substrate (0.4 M pyridine formate, pH 4.25) of human pancreatic carboxypeptidase B and plasma carboxypeptidase N. Bz-Ala-Arg can be used to screen competitive inhibitors of these two enzymes .
|
- HY-P10346
-
|
Smooth-Muscle Myosin Light-Chain Kinase (796-815)
|
Peptides
|
Cardiovascular Disease
Inflammation/Immunology
|
|
smMLCK peptide is a specific inhibitor of smooth muscle myosin light chain kinase (smMLCK). The smMLCK peptide mimics the substrate and competitively inhibits the binding of the actual substrate to the enzyme, thereby inhibiting the kinase activity. This inhibition prevents the phosphorylation of the myosin light chain, thus inhibiting muscle contraction .
|
- HY-P1293A
-
|
|
iGluR
|
Neurological Disease
|
|
Conantokin G TFA, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G TFA inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G TFA has neuroprotective properties .
|
- HY-P2477
-
|
|
PD-1/PD-L1
|
Inflammation/Immunology
|
|
Human PD-L1 inhibitor IV, a polypeptide, is a competitive human PD-1 protein inhibitor with a Kd value of 1.38 μM. Human PD-L1 inhibitor IV inhibits the interaction of hPD-1/hPD-L1 .
|
- HY-17572AR
-
|
|
Oxytocin Receptor
Vasopressin Receptor
|
Endocrinology
Cancer
|
|
Atosiban (acetate) (Standard) is the analytical standard of Atosiban (acetate). This product is intended for research and analytical applications. Atosiban acetate (RW22164 acetate;RWJ22164 acetate) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research .
|
- HY-P1115
-
|
|
Akt
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Others
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|
AKTide-2T is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position .
|
- HY-P1297
-
|
|
CRFR
|
Neurological Disease
|
|
CRF(6-33)(human) is a CRF binding protein (CRF-BP) ligand inhibitor. CRF(6-33)(human) competitively binds the CRF-BP but not the post-synaptic CRF receptors. CRF(6-33)(human) has anti-obesity effect .
|
- HY-P2244
-
|
|
YAP
|
Cancer
|
|
YAP-TEAD-IN-1 is a potent and competitive inhibitor of?YAP–TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd=40 nM) .
|
- HY-P5305A
-
|
|
GABA Receptor
|
Metabolic Disease
|
|
GAD65(247-266) epitope TFA is the T cell epitopes of islet antigens，binding to I-A g7 (type I diabetes-associated molecule) competitively with poor affinity. GAD65 refers to Glutamic Acid Decarboxylase 65，involved in the conversion of glutamate to gamma-aminobutyric acid (GABA) .
|
- HY-108055
-
|
|
Peptides
|
Cardiovascular Disease
|
|
Urantide is a selective and competitive urotensin-II (UT) receptor antagonist peptide (pKB=8.3) that blocks human urotensin-II (hU-II)-induced contractions in rat thoracic aorta ex vivo. Urantide can be used to study the (patho)physiological role of hU-II in the mammalian cardiovascular system .
|
- HY-P10313
-
|
[Nle8'18,Tyr34]bPTH (3-34) amide
|
Peptides
|
Others
|
|
[Nle8,18,Tyr34]-pTH (3-34) amide (bovine) ([Nle8'18,Tyr34]bPTH (3-34) amide) is an analogue of parathyroid hormone (PTH), and is a competitive inhibitor of PTH-stimulated biological responses in vitro .
|
- HY-P4522A
-
|
|
Endogenous Metabolite
|
Others
|
|
Bz-Ala-Arg TFA is a dipeptide. Bz-Ala-Arg TFA is also a spectrophotometric substrate (0.4 M pyridine formate, pH 4.25) of human pancreatic carboxypeptidase B and plasma carboxypeptidase N. Bz-Ala-Arg TFA can be used to screen competitive inhibitors of these two enzymes .
|
- HY-P2244A
-
|
|
YAP
|
Cancer
|
|
YAP-TEAD-IN-1 TFA is a potent and competitive peptide inhibitor of?YAP-TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 TFA is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd= 40 nM) .
|
- HY-P1115A
-
|
|
Akt
|
Others
|
|
AKTide-2T TFA is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T TFA mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position .
|
- HY-P1264
-
|
|
nAChR
|
Neurological Disease
|
|
α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC50 of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM .
|
- HY-P1380A
-
|
|
Apoptosis
|
Cancer
|
|
Difopein (TFA), a specific and competitive inhibitor of 14-3-3 protein (a highly conserved eukaryotic regulatory molecule), blocking the ability of 14-3-3 to bind to target proteins and inhibits 14-3-3/Ligand interactions. Difopein (TFA) leads to induction of apoptosis and enhances the ability of cisplatin to kill cells .
|
- HY-P1178
-
|
|
Trk Receptor
|
Neurological Disease
|
|
Cyclotraxin B, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects .
|
- HY-106103
-
|
MK-678; L-363586
|
Somatostatin Receptor
|
Neurological Disease
Metabolic Disease
|
|
Seglitide (MK-678) is a potent, orally active somatostatin receptor 2 (SSTR2) agonist, and also a competitive antagonist of SSTR14, SSTR25, and SSTR28. Seglitide has antihypertensive effects and can inhibit plasma glucagon and growth hormone. Seglitide can be used for research on diabetes .
|
- HY-106103A
-
|
MK 678 acetate; L 36358 acetate
|
Somatostatin Receptor
|
Neurological Disease
Metabolic Disease
|
|
Seglitide acetate (MK 678; L 36358 acetate) is a potent, orally active somatostatin receptor 2 (SSTR2) agonist, and also a competitive antagonist of SSTR14, SSTR25, and SSTR28. Seglitide acetate has antihypertensive effects and can inhibit plasma glucagon and growth hormone. Seglitide acetate can be used for research on diabetes .
|
- HY-P10630
-
|
|
Amyloid-β
|
Neurological Disease
|
|
Pep63 is a neuroprotective peptide (VFQVRARTVA). Pep63 has a neuroprotective effect on synaptic plasticity and memory. Pep63 can competitively bind with Aβ1-42 oligomers, and can block Aβ fiber formation. Pep63 can be used for Alzheimer’s disease (AD) research .
|
- HY-P1297A
-
|
|
CRFR
|
Neurological Disease
|
|
CRF(6-33)(human) TFA is a CRF binding protein (CRF-BP) ligand inhibitor. CRF(6-33)(human) TFA competitively binds the CRF-BP but not the post-synaptic CRF receptors. CRF(6-33)(human) TFA has anti-obesity effect .
|
- HY-P10392
-
|
|
β-catenin
Wnt
|
Cancer
|
|
aStAx-35R, a stapled peptide, antagonizes nuclear form of β-catenin and inhibits Wnt signaling. aStAx-35R inhibits competitively the binding of β-catenin to TCF4. aStAx-35R selectively induces growth inhibition of Wnt-dependent cancer cells .
|
- HY-P1159
-
|
|
Peptides
|
Neurological Disease
Inflammation/Immunology
|
|
[D-p-Cl-Phe6,Leu17]-VIP is a competitive and selective antagonist of vasoactive intestinal peptide (VIP) receptor, with the IC50 of 125.8 nM. [D-p-Cl-Phe6,Leu17]-VIP has no activity on glucagon, secretin or GRF receptors .
|
- HY-P1178A
-
|
|
Trk Receptor
|
Neurological Disease
|
|
Cyclotraxin B TFA, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B TFA non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B TFA can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects .
|
- HY-P3229
-
SN52
2 Publications Verification
|
NF-κB
|
Cancer
|
|
SN52 is a potent, competitive, and cell-permeable inhibitor of NF-κB2. SN52 is a variant of the SN50 peptide and inhibits the nuclear translocation of p52-RelB heterodimers. SN52 has a strong radiosensitization effect on prostate cancer cells. SN52 can be used for cancer research .
|
- HY-P0205A
-
|
[Sar1,Ala8] Angiotensin II acetate hydrate
|
Angiotensin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Saralasin ([Sar1,Ala8] Angiotensin II) acetate hydrate is an octapeptide analog of angiotensin II. Saralasin acetate hydrate is a competitive angiotensin II receptor antagonist with a Ki value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin acetate hydrate can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension .
|
- HY-P0099
-
|
|
Peptides
|
Others
|
|
Pentapeptide-3 is a pentapeptide fragment of neurotoxin waglerin-1, it can be extracted from the venom of Temple Viper. Pentapeptide-3 is a competitive antagonist of nicotinic acetylcholine receptors (nAChRs), it can blocks nerves at the post-synaptic membrane. Pentapeptide-3 has anti-aging effects and it can be used together with other cosmetic peptides .
|
- HY-P0205
-
|
[Sar1,Ala8] Angiotensin II
|
Angiotensin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Saralasin ([Sar1,Ala8] Angiotensin II) is an octapeptide analog of angiotensin II. Saralasin is a competitive angiotensin II receptor antagonist with a Ki value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension .
|
- HY-P5950
-
|
Adrenocorticotropic hormone (6-24)
|
Peptides
|
Cardiovascular Disease
|
|
ACTH (6-24) (human) (Adrenocorticotropic hormone (6-24)) is an ACTH fragment. ACTH (6-24) (human) is a competitive inhibitor of steroidogenesis induced by ACTH (1-39) and ACTH (5-24) (Kd:13.4 and 3.4 nM). ACTH (6-24) (human) inhibits corticosterone production and cAMP accumulation induced by hPTH 1-34 .
|
- HY-P5038
-
|
c(GRGDSP)
|
Integrin
|
Cancer
|
|
Cyclo(Gly-Arg-Gly-Asp-Ser-Pro) (c(GRGDSP)) is an RGD-containing inhibitory peptide. Cyclo(Gly-Arg-Gly-Asp-Ser-Pro) is a synthetic α5β1 integrin ligand that competitively inhibits the binding of invasin (Inv) to α5β1 integrin expressed on Caco-2 cells .
|
- HY-P0205B
-
|
[Sar1,Ala8] Angiotensin II TFA
|
Angiotensin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Saralasin ([Sar1,Ala8] Angiotensin II) TFA is an octapeptide analog of angiotensin II. Saralasin TFA is a competitive angiotensin II receptor antagonist with a Ki value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin TFA can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension .
|
- HY-P1159A
-
|
|
Peptides
|
Neurological Disease
Inflammation/Immunology
|
|
[D-p-Cl-Phe6,Leu17]-VIP TFA is a competitive and selective antagonist of vasoactive intestinal peptide (VIP) receptor, with the IC50 of 125.8 nM. [D-p-Cl-Phe6,Leu17]-VIP TFA has no activity on glucagon, secretin or GRF receptors .
|
- HY-P2426
-
|
|
Thyroid Hormone Receptor
|
Metabolic Disease
|
|
(D-Trp12,Tyr34)-pTH (7-34) amide (bovine) is a potent and competitive antagonist of parathyroid hormone (PTH), with a Ki of 69 nM in bovine renal cortical membrane. (D-Trp12,Tyr34)-pTH (7-34) amide (bovine) can be used for growth and development regulation .
|
- HY-P5010
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
(D-Arg8)-Inotocin is a potent, selective and competitive antagonist of vasopressin receptor (V1aR), with a Ki of 1.3 nM. (D-Arg8)-Inotocin shows more than 3000-fold selectivity for the human V1aR over the other three subtypes, OTR, V1bR and V2R .
|
- HY-P3248
-
|
Myelin basic protein (85-99) antagonist
|
Biochemical Assay Reagents
|
Inflammation/Immunology
|
|
J5 peptide is an MBP inhibitor that competitively inhibits the binding of MBP85-99 to HLA-DR2. J5 peptide alleviates PLP139-151/MBP85-99-induced experimental autoimmune encephalomyelitis (EAE) in mice. J5 peptide can be used in research on inflammatory and immune diseases .
|
- HY-P1173
-
|
Myristoylated L 803; GSK-3β Inhibitor XIII
|
GSK-3
Amyloid-β
|
Neurological Disease
|
|
L803-mts (Myristoylated L 803) is a selective and substrate-competitive GSK-3 peptide inhibitor (IC50: 40 μM). L803-mts also reduces Aβ deposits and ameliorates cognitive deficits in 5XFAD mice. L803-mts shows antidepressive effect in the forced swimming test .
|
- HY-P10422
-
|
ML-peptide, Multi-Leucine (ML)-peptide
|
Peptides
|
Cancer
|
|
Multi-Leu peptide (ML-peptide) is a potent inhibitor of PACE4 (Ki=22 nM). Multi-Leu peptide can competitively bind to the active site of PACE4 by simulating the substrate sequence of PACE4, thereby inhibiting its catalytic activity. Multi-Leu peptide can be used to study the specific mechanism of PACE4 in the development of prostate cancer .
|
- HY-P10392B
-
|
|
β-catenin
Wnt
|
Cancer
|
|
aStAx-35R TFA, a stapled peptide, antagonizes nuclear form of β-catenin and inhibits Wnt signaling. aStAx-35R TFA inhibits competitively the binding of β-catenin to TCF4. aStAx-35R TFA selectively induces growth inhibition of Wnt-dependent cancer cells .
|
- HY-P10581A
-
|
|
Peptides
|
Inflammation/Immunology
|
|
SIIVFEKL TFA is a variant of the major MHC class I-restricted epitope SIINFEKL. SIIVFEKL TFA is an antigenic peptide, that can stimulate specific T cells in experimental settings to study the competitive interaction between T cells. SIIVFEKL TFA exhibits low affinity for the OT-I T cell receptor (TCR), and can be used for detection of CD8+ T cells .
|
- HY-P10582A
-
|
|
Peptides
|
Inflammation/Immunology
|
|
SIYNFEKL TFA is a variant of major MHC class I-restricted epitope SIINFEKL. SIYNFEKL TFA is an antigenic peptide, that can stimulate specific T cells in experimental settings to study the competitive interaction between T cell. SIYNFEKL TFA exhibits low affinity for the OT-I T cell receptor (TCR), and can be used for detection of CD8+ T cells .
|
- HY-P10600
-
|
|
Peptides
|
Others
|
|
BIMAX2 is a high affinity nuclear localization signal (NLS) peptide. BIMAX2 can mimic the activity of the classical nuclear localization signal (cNLS) and competitively bind to importin α, thereby inhibiting the binding of cNLS-cargo proteins to importin α. BIMAX2 can be used to study the role of RBBP4 in regulating nuclear import efficiency and cell senescence .
|
- HY-P10600A
-
|
|
Peptides
|
Others
|
|
BIMAX2 acetate is a high affinity nuclear localization signal (NLS) peptide. BIMAX2 acetate can mimic the activity of the classical nuclear localization signal (cNLS) and competitively bind to importin α, thereby inhibiting the binding of cNLS-cargo proteins to importin α. BIMAX2 acetate can be used to study the role of RBBP4 in regulating nuclear import efficiency and cell senescence .
|
- HY-100838
-
|
L-CCG III
|
EAAT
|
Neurological Disease
|
|
cis-α-(Carboxycyclopropyl)glycine (L-CCG III) is a potent, competitive glutamate uptake inhibitor. cis-α-(Carboxycyclopropyl)glycine is a substrate of glutamate transporters (GluT) (EC50: 13 μM, 2 μM for EAAT 1 and EAAT 2, respectively). cis-α-(Carboxycyclopropyl)glycine inhibits a Na +-dependent high-affinity L-glutamate uptake in glial plasmalemmal vesicles (GPV) and synaptosomes .
|
- HY-P1740
-
|
|
Integrin
Apoptosis
Caspase
|
Inflammation/Immunology
|
|
RGD peptide (GRGDNP) is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) plays an important role in cell adhesion, migration, growth, and differentiation .
|
- HY-P3143A
-
|
|
PD-1/PD-L1
|
Cancer
|
|
BMSpep-57 hydrochloride is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68?nM. BMSpep-57 hydrochloride binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 hydrochloride facilitates T cell function by in creasing IL-2 production in PBMCs .
|
- HY-P0096
-
|
|
Tyrosinase
Sirtuin
|
Inflammation/Immunology
Endocrinology
|
|
Decapeptide-12, a small oligopeptide, is a tyrosinase inhibitor that interacts with C-terminal residue of tyrosinase (Kd: 61.1 μM). Decapeptide-12 is a competitive inhibitor of mushroom tyrosinase (IC50: 40 μM). Decapeptide-12 also increases transcription of SIRT. Decapeptide-12 reduces melanin content in melanocytes. Decapeptide-12 is used for the research of melanogenesis, senescence, inflammation .
|
- HY-P3850
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
(D-Pro2,D-Trp6,8,Nle10)-Neurokinin B is a competitive antagonist of Neurokinin B (Neurokinin Receptor) with a pA2 of 5.5. (D-Pro2,D-Trp6,8,Nle10)-Neurokinin B shows no influence on Substance P or Neurokinin A .
|
- HY-P5322
-
|
|
Peptides
|
Others
|
|
Thrombospondin (TSP-1)-derived CD36 binding motif is a biological active peptide. (This peptide is derived from thrombospondin and represents a binding motif responsible for thrombospondin-CD36 interaction. It is cyclized through a disulfide bond. Thrombospondin is a matrix-bound glycoprotein involved in cancer metastasis, tumor adhesion, and angiogenesis. This peptide has been shown to competitively inhibit platelet aggregation and tumor metastasis.)
|
- HY-P10668
-
|
|
Dengue virus
Flavivirus
|
Infection
|
|
Ac-EVKKQR-pNA is a competitive chromogenic para-nitroanilide substrate corresponding to the P6-P1 segment amino-terminal to the NS2B-NS3 cleavage site but with a more reactive, hydrolytically cleavable, para-nitroanilide at the P1’ position. Ac-EVKKQR-pNA is promising for research of dengue 2 virus and flavivirus virus infection .
|
- HY-P1318
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
|
- HY-P1318A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
|
- HY-P10465
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
TRPV1-Tat is an antagonistic peptide that fuses the TRPV1 (transient receptor potential vanilla subtype 1) of the cell-penetrating peptide Tat. TRPV1-Tat blocks this phosphorylation process by competitively binding to the AKAP79 binding site of TRPV1, thereby inhibiting the sensitization of TRPV1. TRPV1-Tat can be used in the study of inflammatory pain .
|
- HY-P1230
-
|
|
Dipeptidyl Peptidase
GLP Receptor
|
Metabolic Disease
|
|
HAEGT is the first N-terminal 1-5 residues of glucagon like peptide-1 (GLP-1) peptide, and the sequence is His-Ala-Glu-Gly-Thr. HAEGT acts as a competitive substrate for probing prime substrate binding sites of human dipeptidyl peptidase-IV (DPP-IV) 1, in which the N-terminal His-Ala is catalyzed cleavage by DPP-IV. HAEGT can be used in the research of diabetes, obesity .
|
- HY-P1740A
-
|
|
Integrin
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
RGD peptide (GRGDNP) TFA is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) TFA competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) TFA promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) TFA plays an important role in cell adhesion, migration, growth, and differentiation .
|
- HY-P3143
-
|
|
PD-1/PD-L1
|
Cancer
|
|
BMSpep-57 is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50?of 7.68?nM. BMSpep-57 binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST?and SPR assays, respectively.?BMSpep-57?facilitates T cell function by in creasing IL-2 production in PBMCs .
|
- HY-P0097A
-
|
Melanostatine-5 acetate salt
|
Melanocortin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Nonapeptide-1 (Melanostatine-5) acetate salt, a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 acetate salt is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 acetate salt inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer .
|
- HY-P0097
-
|
Melanostatine-5
|
Melanocortin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Nonapeptide-1 (Melanostatine-5), a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer .
|
- HY-P5455
-
|
|
LIM Kinase (LIMK)
|
Others
|
|
S3 Fragment is a biological active peptide. (This peptide contains the unique amino-terminal phosphorylation site of Xenopus ADF/cofilin, the LIM kinase (LIMK) phosphorylation site. LIMK1 is a key regulator of the actin cytoskeleton through its phosphorylation of ADF/cofilin at serine-3 for inactivation. This peptide is a fragment of the S3 peptide containing the serine-3 sequence of ADF/cofilin that has been widely used as an effective competitive inhibitor of LIMK1.)
|
- HY-P5894
-
|
Galanin-like peptide (3-32)
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
human GALP (3-32) (Galanin-like peptide (3-32)) is a potent galanin receptor agonist with high affinity for both GalR1 (IC50=33 nM) and GalR2 (IC50=15 nM) in a competitive binding study. human GALP (3-32) exhibits the high potency in altering the extracellular acidification rate of SH-SY5Y cells transfected with GalR2 (EC50=360 nM) .
|
- HY-P1321
-
|
1229U91; GW1229
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide Y Y6 receptor (pKi= 8.8) .
|
- HY-P1321A
-
|
1229U91 TFA; GW1229 TFA
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
GR231118 TFA, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide YY receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide YY4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide Y Y2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide YY6 receptor (pKi= 8.8) .
|
- HY-P4160
-
|
THG113.31; ILGHXDYK
|
Prostaglandin Receptor
|
Endocrinology
|
|
PDC31 (THG113.31; ILGHXDYK) is an allosteric and non-competitive inhibitor of FP Prostaglandin Receptor. PDC31 is the D-amino acid-based oligopeptide, is used for smooth muscle contractile agent. PDC31 decreases the strength and duration of uterine contractions in vivo, which can be used for research of preterm labor and primary dysmenorrhea (PD). PDC31 also enhances Ca 2+-dependent large-conductance K +-channel in human myometrial cells .
|
- HY-P5756
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CSD-CH2(1,8)-NH2 is a selective and competitive KOR antagonist (Ki: 6.8 nM). CSD-CH2(1,8)-NH2 inhibits calcium mobilization in DRG neurons. CH2(1,8)-NH2 antagonizes the antinociceptive effect of U50,488. CSD-CH2(1,8)-NH2 can be used for research of neuropsychiatric disorders .
|
- HY-P5272
-
|
|
Bacterial
|
Inflammation/Immunology
|
|
Histatin-3 TFA, a 32 amino acid peptide, possesses powerful antimicrobial properties. Histatin-3 TFA behaves as a substrate for proprotein convertase 1 (PC1), being cleaved by this endoprotease primarily at a site carboxy terminal to the single Arg25 residue (HRGYR decrease SN). Histatin-3 TFA is a moderately potent, reversible and competitive inhibitor of the furin-mediated cleavage of the pentapeptide pGlu-Arg-Thr-Lys-Arg-MCA fluorogenic substrate, with an estimated inhibition constant Ki of 1.98 μM .
|
- HY-P5601
-
|
|
Bacterial
Fungal
|
Infection
|
|
Thanatin is an inducible cationic antimicrobial peptide. Thanatin is a pathogen-inducible single-disulfide-bond-containing β-hairpin AMP. Thanatin displays broad-spectrum activity against both Gram-negative and Gram-positive bacteria as well as against various species of fungi with MICs of 0.3-40 µM, 0.6-40 µM and 0.6-20 µM, respectively. Thanatin has the property of competitive replacement of divalent cations from bacterial outer membrane (OM), leading to OM disruption .
|
- HY-P5601A
-
|
|
Bacterial
Fungal
|
Infection
|
|
Thanatin TFA is an inducible cationic antimicrobial peptide. Thanatin TFA s a pathogen-inducible single-disulfide-bond-containing β-hairpin AMP. Thanatin TFA displays broad-spectrum activity against both Gram-negative and Gram-positive bacteria as well as against various species of fungi with MICs of 0.3-40 µM, 0.6-40 µM and 0.6-20 µM, respectively. Thanatin TFA has the property of competitive replacement of divalent cations from bacterial outer membrane (OM), leading to OM disruption .
|
- HY-P5846
-
|
MT3
|
mAChR
Adrenergic Receptor
|
Neurological Disease
|
|
Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC50s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M1, M4, α1A, α1B, α1D,α2A,α2B and α2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity .
|
- HY-P5158
-
|
|
Adrenergic Receptor
|
Others
|
|
Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α1A-Adrenergic Receptor and α1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype and may provide useful information for the development of novel α1-Adrenergic Receptor subtype-selective drugs .
|
- HY-P2055
-
|
|
Peptides
|
Endocrinology
|
|
A-57696 is a cholecystokinin antagonist with selective activity at cortical CCK-B receptors (IC50 = 25 nM). A-57696 behaves as a competitive antagonist in reversing CCK8-stimulated pancreatic alpha-amylase secretion and phosphatidylinositol degradation. A-57696 fails to induce gallbladder contraction and inhibits CCK8-induced contraction. A-57696 behaves as a partial agonist at CCK-B/gastrin receptors on NCI-H345 cells, achieving 80% of the maximal CCK8 response. A-57696 and CCK8 inhibit each other in a calcium mobilization assay .
|
- HY-P1320
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
|
- HY-P1320A
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2?binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
|
- HY-P0299A
-
|
|
TGF-β Receptor
|
Cancer
|
|
LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier .
|
- HY-P0299
-
|
|
TGF-β Receptor
|
Cancer
|
|
LSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) can readily crosse the blood-brain barrier .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99652
-
|
AK 111
|
Interleukin Related
|
Inflammation/Immunology
|
|
Gumokimab (AK 111) is a monoclonal antibody targeting IL-17A, which can be used in the study of psoriasis, ankylosing spondylitis. Gumokimab competitively blocks the binding of human IL-17A to IL-17R.
|
-
- HY-108847
-
|
|
TNF Receptor
Bacterial
|
Inflammation/Immunology
Cancer
|
|
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis .
|
-
- HY-P99639
-
|
APL-501; CBT-501; GB-226
|
PD-1/PD-L1
|
Cancer
|
|
Geptanolimab (CBT-501) is a humanized IgG4k monoclonal antibody against programmed death-1 (PD-1). Siplizumab inhibits the binding of PD-L1/L2 to PD-1 through a competitive action. Siplizumab can be used in research of cancer .
|
-
- HY-P99345
-
|
TSR-042
|
PD-1/PD-L1
|
Cancer
|
|
Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
- HY-N0575
-
-
- HY-N7114A
-
-
- HY-N3394
-
-
- HY-B0134
-
-
- HY-N0793A
-
-
- HY-N4110
-
-
- HY-N0793
-
-
- HY-Y1787
-
-
- HY-N0598
-
-
- HY-B0199A
-
-
- HY-N9685
-
-
- HY-W010510R
-
-
- HY-N0471
-
-
- HY-N2197
-
-
- HY-N6054
-
-
- HY-N2383
-
|
(1R,2S,3S,4S,6R)-4-Amino-6-(hydroxymethyl)cyclohexane-1,2,3-triol
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
|
Glucosidase
|
|
Validamine competitively inhibits β-glucosidase in a pH-dependent and dose-dependent manner, with an IC50 value of 2.92mM, and the maximum inhibitory ability is at the optimum pH value of this enzyme .
|
-
- HY-N3320
-
-
- HY-N1201R
-
-
- HY-N12736
-
-
- HY-Y0504R
-
-
- HY-20558R
-
-
- HY-N9949
-
-
- HY-13503R
-
-
- HY-135072R
-
-
- HY-N6650
-
-
- HY-N4289
-
-
- HY-N1750
-
-
- HY-N10497
-
|
|
Alkaloids
Leguminosae
Plants
|
nAChR
|
|
Dihydro-β-erythroidine is a a competitive nicotinic receptor antagonist. Dihydro-β-erythroidine blocks the discriminative stimulus properties of nicotine. Dihydro-β-erythroidine inhibits the anxiolytic effect of nicotine induced .
|
-
- HY-N7114
-
-
- HY-N2962
-
-
- HY-B0183R
-
-
- HY-N1860
-
-
- HY-N4225
-
-
- HY-10963
-
-
- HY-N2368
-
-
- HY-N2368A
-
-
- HY-N10488
-
-
- HY-W727627
-
-
- HY-N9075
-
-
- HY-N4195
-
-
- HY-N0471A
-
-
- HY-113514
-
-
- HY-I0096
-
-
- HY-125916
-
-
- HY-N7763
-
-
- HY-16007
-
-
- HY-100786
-
-
- HY-121377
-
-
- HY-N12399
-
-
- HY-N10002
-
-
- HY-100397
-
|
|
Microorganisms
Source classification
|
Elastase
|
|
Elastatinal is a potent and competitive inhibitor of elastase, with a Ki of 0.21 μM. Elastatinal more potently inhibits pancreatic elastase versus leucocyte elastase. Elastatinal shows no activity on human leucocyte chymotrypsin-like protease .
|
-
- HY-W011184
-
-
- HY-113054
-
-
- HY-100513A
-
-
- HY-N7740
-
-
- HY-W661499
-
-
- HY-N0021R
-
-
- HY-N0575R
-
-
- HY-N2463
-
-
- HY-N9506
-
-
- HY-116750
-
-
- HY-130199
-
-
- HY-B0134R
-
-
- HY-18963
-
-
- HY-N4193
-
-
- HY-N7377
-
-
- HY-W010378
-
-
- HY-N0793R
-
-
- HY-N7114AR
-
-
- HY-P0027
-
-
- HY-B1729
-
|
|
Microorganisms
Source classification
|
Oxidative Phosphorylation
Bacterial
|
|
Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al .
|
-
- HY-W051513
-
-
- HY-P1293
-
-
- HY-113038B
-
-
- HY-N10489
-
-
- HY-N6054R
-
-
- HY-B0371
-
-
- HY-107339
-
-
- HY-N1193
-
-
- HY-129137
-
|
Cy 3-soph
|
Rosaceae
Plants
Prunus cerasus L.
|
Others
|
|
Cyanidin 3-sophoroside chloride is a potent non-competitive reversible polyphenol oxidase (PPO) inhibitor. Also, Cyanidin 3-sophoroside chloride can be used as an anti-browning agent to inhibit the degree of PPO browning, enhance the antioxidant damage capacity of fruits and prolong the storage period .
|
-
- HY-N7136
-
-
- HY-N7389B
-
-
- HY-N8122
-
-
- HY-113329
-
-
- HY-113038A
-
-
- HY-N0471R
-
-
- HY-101037
-
-
- HY-N0368
-
-
- HY-125833
-
-
- HY-135780
-
-
- HY-P1293A
-
|
|
Natural Products
Animals
Source classification
|
iGluR
|
|
Conantokin G TFA, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G TFA inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G TFA has neuroprotective properties .
|
-
- HY-114203
-
-
- HY-N3136
-
-
- HY-N1919
-
-
- HY-W009156
-
-
- HY-N1919A
-
-
- HY-N8382
-
-
- HY-N9933
-
-
- HY-15141
-
-
- HY-N4037
-
-
- HY-N0192
-
-
- HY-B1295
-
-
- HY-17462
-
-
- HY-135780A
-
-
- HY-122936
-
-
- HY-P99639
-
-
- HY-W685943
-
-
- HY-N0471AR
-
-
- HY-B0290
-
-
- HY-B1205
-
-
- HY-B0290A
-
-
- HY-10406A
-
|
SCIO-469 hydrochloride
|
Classification of Application Fields
Disease Research Fields
Cancer
|
p38 MAPK
|
|
Talmapimod (SCIO-469) hydrochloride is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod hydrochloride shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs .
|
-
- HY-N4042
-
-
- HY-131592
-
-
- HY-N10403
-
-
- HY-P99345
-
-
- HY-B1729R
-
|
|
Microorganisms
Source classification
|
Oxidative Phosphorylation
Bacterial
|
|
Phenoxyethanol (Standard) is the analytical standard of Phenoxyethanol. This product is intended for research and analytical applications. Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al .
|
-
- HY-N12761
-
-
- HY-B0236
-
-
- HY-15237
-
-
- HY-131081
-
-
- HY-N0368R
-
-
- HY-107339R
-
-
- HY-B0394
-
|
Tropine tropate sulfate monohydrate; DL-Hyoscyamine sulfate monohydrate
|
Alkaloids
Structural Classification
Other Alkaloids
Source classification
Atropa belladonna Linn.
Solanaceae
Plants
|
mAChR
|
|
Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .
|
-
- HY-B1205A
-
-
- HY-N10096
-
-
- HY-N7150
-
|
5,7-Dihydroxy-3',4',5'-trimethoxyflavone
|
Structural Classification
Flavonols
Haplopteris anguste-elongata (Hayata) E. H. Crane
Flavonoids
Chrysanthemum × morifolium (Ramat.) Hemsl.
Source classification
Pteridaceae
Plants
Compositae
|
Xanthine Oxidase
|
|
Tricetin 3',4',5'-trimethyl ether (5,7-Dihydroxy-3',4',5'-trimethoxyflavone) is a flavone glucoside, that can be isolated the flowers of Chrysanthemum sinensea. Tricetin 3',4',5'-trimethyl ether displays xanthine oxidase competitive-type inhibitory activity, with an IC50 of 0.51 μM and a Ki of 0.37 μM .
|
-
- HY-N12688
-
-
- HY-101037R
-
-
- HY-17387
-
-
- HY-W008364
-
-
- HY-N0063
-
-
- HY-N1919R
-
-
- HY-N7136R
-
-
- HY-13716
-
-
- HY-A0009
-
|
Galantamine hydrobromide
|
Structural Classification
Alkaloids
Other Alkaloids
Plants
Amaryllidaceae
|
Cholinesterase (ChE)
nAChR
|
|
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
|
-
- HY-122489A
-
|
|
Structural Classification
Alkaloids
Microorganisms
Source classification
Isoquinoline Alkaloids
|
Others
|
|
(S)-Laudanosine is an alkaloid that can be found in poppies and is the S-enantiomer of Laudanosine. Laudanosine acts on the central nervous system and cardiovascular system, inhibiting low-affinity GABA receptors with an IC50 value of 10 μM, and can cause seizures, hypotension, and bradycardia. Additionally, Laudanosine exerts analgesic effects by competitively binding to the opioid Mu-1 receptor (Ki = 2.7 μM) .
|
-
- HY-N0192R
-
-
- HY-W009156R
-
-
- HY-N7389A
-
-
- HY-B1205R
-
|
Tropine tropate (Standard); DL-Hyoscyamine (Standard)
|
Source classification
Atropa belladonna Linn.
Solanaceae
Plants
Endogenous metabolite
|
mAChR
Endogenous Metabolite
|
|
Atropine (Standard) is the analytical standard of Atropine. This product is intended for research and analytical applications. Atropine (Tropine tropate) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine inhibits ACh-induced relaxations in human pulmonary veins. Atropine can be used for research of anti-myopia and bradycardia .
|
-
- HY-N11706
-
-
- HY-B0290R
-
-
- HY-N4110R
-
|
|
Structural Classification
Natural Products
Celastraceae
Maytenus ilicifolia
Plants
|
Cytochrome P450
|
|
Friedelin (Standard) is the analytical standard of Friedelin. This product is intended for research and analytical applications. Friedelin is isolated from isolated from the leaves of Maytenus ilicifolia(Mart). Friedelin is a noncompetitive inhibitor of CYP3A4 with IC50 and Kivalues of 10.79 ?μM and 6.16? μM, respectively. Friedelin is also a competitive inhibitor of CYP2E1 with IC50 and Ki values of 22.54? μM and 18.02 μM, respectively .
|
-
- HY-N0241
-
-
- HY-129997
-
-
- HY-N12109
-
|
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
|
Others
|
|
Albizziin is an amino acid analog with activity as a competitive inhibitor of asparagine synthetase. Albizziin has been used to isolate Chinese hamster ovary cell mutants with altered levels of the target enzyme. Several mutational classes of albizziin can be distinguished based on cross-resistance to β-aspartic hydroxamic acid. Studies on asparagine synthetase have shown that resistance to albizziin may be associated with altered regulation of asparagine synthetase, structural mutations of the enzyme, and gene amplification .
|
-
- HY-B0442
-
-
- HY-B0442A
-
-
- HY-W015309
-
-
- HY-101193
-
-
- HY-N1483
-
-
- HY-B0442C
-
-
- HY-B1205AR
-
|
|
Alkaloids
Structural Classification
Other Alkaloids
Source classification
Atropa belladonna Linn.
Solanaceae
Plants
|
mAChR
|
|
Atropine (sulfate) (Standard) is the analytical standard of Atropine (sulfate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate can be used for research of anti-myopia and bradycardia .
|
-
- HY-N0063R
-
|
|
Structural Classification
Punica granatum L.
Source classification
Phenols
Polyphenols
Punicaceae
Plants
|
SARS-CoV
HBV
|
|
Punicalagin (Standard) is the analytical standard of Punicalagin. This product is intended for research and analytical applications. Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a reversible and non-competitive 3CLpro inhibitor and inhibits SARS-CoV-2 replication in vitro. Punicalagin is an anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects. Punicalagin has the potential for the research of COVID-19 .
|
-
- HY-W008364R
-
-
- HY-B0394R
-
|
|
Alkaloids
Structural Classification
Other Alkaloids
Source classification
Atropa belladonna Linn.
Solanaceae
Plants
|
mAChR
|
|
Atropine (sulfate monohydrate) (Standard) is the analytical standard of Atropine (sulfate monohydrate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .
|
-
- HY-13716R
-
|
|
Structural Classification
Alkaloids
Source classification
Quinoline Alkaloids
Papaver somniferum Linn.
Plants
Papaveraceae
|
Opioid Receptor
Apoptosis
|
|
Noscapine (Standard) is the analytical standard of Noscapine. This product is intended for research and analytical applications. Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier [4] .
|
-
- HY-16569
-
-
- HY-N0142
-
-
- HY-17504A
-
|
ZD 4522
|
Classification of Application Fields
Disease Research Fields
Cancer
|
HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
Bacterial
|
|
Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-N0215
-
-
- HY-N0235
-
-
- HY-N1584
-
-
- HY-N0376
-
-
- HY-N2278
-
-
- HY-N2071
-
-
- HY-113038
-
-
- HY-B0442B
-
-
- HY-A0009R
-
|
Galantamine hydrobromide (Standard)
|
Structural Classification
Alkaloids
Other Alkaloids
Source classification
Plants
Amaryllidaceae
|
nAChR
Cholinesterase (ChE)
|
|
Galanthamine (hydrobromide) (Standard) is the analytical standard of Galanthamine (hydrobromide). This product is intended for research and analytical applications. Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
|
-
- HY-100542
-
-
- HY-N1584A
-
-
- HY-121197
-
|
Ophiocordin; Azepinostatin
|
Structural Classification
Natural Products
Microorganisms
Source classification
|
MARCKS
PKA
PKC
|
|
Balanol (Ophiocordin; Azepinostatin) is a potent and ATP competitive PKC/PKA inhibitor against human PKC isozymes α, β-I, β-II, γ, δ, ε, η (IC50s=4-9 nM) and ζ (IC50=150 nM). Balanol also blocks the phosphorylation of cyclic AMP response element-binding protein (CREB) and myristoylated alanine-rich C kinase substrate (MARCKS). Balanol can be isolated from the fungus Verticillium balanoides .
|
-
- HY-N2071R
-
|
|
Structural Classification
Cedrus deodara (Roxburgh) G. Don
Pinaceae
Terpenoids
Sesquiterpenes
Source classification
Plants
|
Cytochrome P450
Fungal
Apoptosis
Caspase
|
|
Cedrol (Standard) is the analytical standard of Cedrol. This product is intended for research and analytical applications. Cedrol is a potent competitive inhibitor of cytochrome P-450(CYP) enzyme. Cedrol plays an anticancer role by inducing cell cycle arrest and Caspase-dependent apoptosis. Cedrol acts as a neutrophil agonist that can desensitize cells to subsequent stimulation of N-formyl peptides. Cedrol prevents neuropathic pain caused by chronic contractile injury by inhibiting oxidative stress and inflammation. In addition, Cedrol has antibacterial, hair loss prevention and anti-anxiety properties.
|
-
- HY-W015309R
-
|
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
iGluR
Tyrosinase
c-Met/HGFR
Glutaminase
|
|
Decanoic acid (Standard) is the analytical standard of Decanoic acid. This product is intended for research and analytical applications. Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .
|
-
- HY-B0442R
-
|
|
Structural Classification
Natural Products
Source classification
Endogenous metabolite
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
|
Vardenafil (Standard) is the analytical standard of Vardenafil. This product is intended for research and analytical applications. Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-W011428
-
|
|
Classification of Application Fields
Disease Research Fields
Cancer
|
CDK
|
|
Olomoucine is an ATP competitive inhibitor of CDKs. Olomoucine is a purine (HY-34431) derivative and inhibits CDC2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E (both IC50=7 μM), CDK/p35 kinase (IC50=3 μM) and ERK1/p44 MAP kinase (IC50=25 μM) . Olomoucine regulates cell cycle and shows anti-melanin tumor activity .
|
-
- HY-N0142R
-
-
- HY-16569R
-
|
|
Structural Classification
Natural Products
other families
Source classification
Plants
|
Microtubule/Tubulin
NOD-like Receptor (NLR)
Autophagy
Apoptosis
|
|
Colchicine (Standard) is the analytical standard of Colchicine. This product is intended for research and analytical applications. Colchicine, an orally active alkaloid, is a potent tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs). Colchicine prevents non-steroidal anti-inflammatory drug (NSAID)-induced small intestinal injury by inhibiting activation of the NLRP3 inflammasome. Colchicine has extensive anti-inflammatory, immunosuppressive and strong anti-fibrosis effects and has the potential for gouty arthritis research .
|
-
- HY-N0215R
-
|
|
Structural Classification
Microorganisms
Animals
Source classification
Amino acids
Endogenous metabolite
|
Calcium Channel
iGluR
Endogenous Metabolite
|
|
L-Phenylalanine (Standard) is the analytical standard of L-Phenylalanine. This product is intended for research and analytical applications. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals .
|
-
- HY-N0235R
-
|
|
Structural Classification
Monophenols
Leguminosae
Source classification
Phenols
Psoralea corylifolia L.
Plants
|
Carboxylesterase
p38 MAPK
Autophagy
UGT
|
|
Bakuchiol (Standard) is the analytical standard of Bakuchiol. This product is intended for research and analytical applications. Bakuchiol is a phytoestrogen that can be obtained from psoralen seeds. Bakuchiol has been proven to be a non-competitive inhibitor of multiple enzymes, including UDP-glucuronosyltransferase 2B7 (UGT2B7) and human carboxylesterase 2 (hCE2) , with IC50s values of 40.9 μM and 7.28 μM, respectively. Bakuchiol exhibits significant research and application potential in areas such as anti-inflammatory , antibacterial , antitumor therapies, as well as drug metabolism regulation.
|
-
- HY-B0442BR
-
|
|
Structural Classification
Natural Products
Source classification
Endogenous metabolite
|
Endogenous Metabolite
Phosphodiesterase (PDE)
|
|
Vardenafil (hydrochloride trihydrate) (Standard) is the analytical standard of Vardenafil (hydrochloride trihydrate). This product is intended for research and analytical applications. Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes - .
|
-
- HY-N1584AR
-
-
- HY-N0226
-
|
|
Alkaloids
Source classification
Ranunculaceae
Coptis chinensis Franch.
Plants
Isoquinoline Alkaloids
|
Cholinesterase (ChE)
Beta-secretase
|
|
Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and can be used for the research of Alzheimer disease . Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberinecan be used for the research of diabetic disease .
|
-
- HY-N0226A
-
-
- HY-N5072
-
|
4',6,7-Trihydroxyisoflavone
|
Flavonoids
Classification of Application Fields
Leguminosae
Glycine max (L.) merr
Source classification
Phenols
Polyphenols
Plants
Disease Research Fields
Isoflavones
Cancer
|
CDK
PI3K
PKC
|
|
Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities.
Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity . Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1) . Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes .
|
-
- HY-N1957
-
-
- HY-N1957R
-
|
|
Structural Classification
Xanthones
Guttiferae
Phenols
Polyphenols
Garcinia mangostana Linn.
Plants
|
5-HT Receptor
COX
Transthyretin (TTR)
|
|
Gamma-Mangostin (Standard) is the analytical standard of Gamma-Mangostin. This product is intended for research and analytical applications. Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer . Gamma-Mangostin inhibits [3H] spiperone binding to cultured rat aortic myocytes (IC50=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC50=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .
|
-
- HY-30004
-
|
|
Structural Classification
Microorganisms
Classification of Application Fields
Ketones, Aldehydes, Acids
Source classification
Metabolic Disease
Endogenous metabolite
Disease Research Fields
|
Endogenous Metabolite
|
|
1-Aminocyclopropane-1-carboxylic acid is an endogenous metabolite. In the presence of low concentrations (1 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a small molecule agonist of NMDA receptors with an EC50 of 0.7-0.9 μM. At high concentrations (10 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a competitive antagonist of NMDA receptors with an EC50 of 81.6 nM. 1-Aminocyclopropane-1-carboxylic acid exerts neuroprotective activity by moderately activating NMDA receptors to prevent neuronal cell death in ischemic animal models. Additionally, 1-Aminocyclopropane-1-carboxylic acid is an antagonist of NMDA receptors, inducing blood pressure reduction and antioxidant effects in stroke-prone hypertensive rats. 1-Aminocyclopropane-1-carboxylic acid enhances object recognition memory and cognitive flexibility dependent on the prefrontal cortex, but does not affect impulsivity nor exhibit an antipsychotic-like profile. 1-Aminocyclopropane-1-carboxylic acid shows promise for research in the field of neurotoxicity. .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-10450S
-
|
|
|
Dapagliflozin-d5 is a deuterium labeled Dapagliflozin. Dapagliflozin is a competitive SGLT2 inhibitor[1].
|
-
-
- HY-B0437AS
-
|
|
|
Sotalol-d6 (hydrochloride) is a deuterium labeled Sotalol hydrochloride. Sotalol hydrochloride is an orally active, non-selective competitive β-adrenergic receptor blocker. Sotalol hydrochloride is a potent antiarrhythmic agent that can be used for the research of pediatric arrhythmias. Sotalol hydrochloride blocks β-receptors, and potassium KCNH2 channels[1][2].
|
-
-
- HY-B0242S1
-
|
|
|
Sulfanilamide-d4 is the deuterium labeled Sulfanilamide. Sulfanilamide is a competitive inhibitor for bacterial enzyme dihydropteroate synthetase with IC50 of 320 μM.
|
-
-
- HY-14664AS
-
|
|
|
Fluvastatin-d6 (sodium) is deuterium labeled Fluvastatin sodium. Fluvastatin sodium (XU 62320) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM.
|
-
-
- HY-15656S
-
|
|
|
Ceritinib-d7 is a deuterium labeled Ceritinib. Ceritinib is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor[1].
|
-
-
- HY-14806S
-
|
|
|
Teneligliptin-d8 is a deuterium labeled Teneligliptin (MP-513). Teneligliptin is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor[1].
|
-
-
- HY-P2625S1
-
|
|
|
GLP-2(3-33) (Leu- 13C6, 15N) TFA is 13C and 15N labeled GLP-2(3-33) (HY-P2625). GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC50=5.8 nM).
|
-
-
- HY-P2625S
-
|
|
|
GLP-2(3-33) (Leu- 13C6, 15N) is 13C and 15N labeled GLP-2(3-33) (HY-P2625). GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC50=5.8 nM).
|
-
-
- HY-B0437S
-
|
|
|
Sotalol-d6 is the deuterium labeled Sotalol. Sotalol is an orally active, non-selective β-adrenergic receptor blocker. Sotalol is a potent antiarrhythmic agent that can be used for the research of pediatric arrhythmias. Sotalol blocks β-receptors, and potassium KCNH2 channels. Antiepileptic Agent[1][2][3][4].
|
-
-
- HY-14806S1
-
|
|
|
Teneligliptin-d4 is deuterium labeled Teneligliptin. Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM[1].
|
-
-
- HY-17502S
-
|
|
|
Simvastatin-d11 is the deuterium labeled Simvastatin. Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM[1][2].
|
-
-
- HY-16060S
-
|
|
|
Apalutamide-d4 is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[1].
|
-
-
- HY-17502S1
-
|
|
|
Simvastatin-d3 is the deuterium labeled Simvastatin[1]. Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM[2].
|
-
-
- HY-N1201S
-
|
|
|
Apigenin-d5 is a deuterated labeled Apigenin . Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a Ki of 2 μM.
|
-
-
- HY-B0882S
-
|
|
|
Edrophonium-d5 (chloride) is the deuterium labeled Edrophonium chloride. Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
|
-
-
- HY-16168AS
-
|
|
|
Degarelix-d7 (FE 200486-d7 free base) is deuterium labeled Degarelix. Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
|
-
-
- HY-B0165CS
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Pravastatin-d3 (sodium) is the deuterium labeled Pravastatin sodium salt. Pravastatin (CS-514) sodium salt is a competitive HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM[1][2].
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- HY-B0394S
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Atropine-d5 is the deuterium labeled Atropine (sulfate monohydrate). Atropine (Tropine tropate) sulfate monohydrate is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect[1].
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- HY-16060S3
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Apalutamide-d7 is deuterated labeled Apalutamide (HY-16060). Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM .
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- HY-B0322S1
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Sulfamethoxazole- 13C6 is a 13C labeled Sulfamethoxazole. Sulfamethoxazole (Ro 4-2130) is a sulfonamide bacteriostatic antibiotic, used for bacterial infections. Sulfonamides is a competitive antagonist of para-aminobenzoic acid (PABA)[1].
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- HY-16060S1
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Apalutamide-d3 is the deuterium labeled Apalutamide[1]. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[2].
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- HY-B0165S
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Pravastatin-d9 sodium is deuterated labeled Pravastatin (HY-B0165). Pravastatin (CS-514) is a competitive HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM .
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- HY-17000S
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Tolvaptan-d7 is the deuterium labeled Tolvaptan. Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation[1][2].
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- HY-W015309S
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Decanoic acid-d3 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
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- HY-W015309S2
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Decanoic acid-d2 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
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- HY-W015309S1
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Decanoic acid-d199 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
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- HY-W015309S3
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Decanoic acid-d5 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
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- HY-12432S1
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Gilteritinib-d8 is deuterium labeled Gilteritinib. Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC50s of 0.29 nM/0.73 nM, respectively.
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- HY-16060S2
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Apalutamide- 13C,d3 is the 13C- and deuterium labeled Apalutamide. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[1].
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- HY-B0183S
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Ellagic acid- 13C12 is 13 C-labeled Ellagic acid (HY-B0183). Ellagic acid is a natural antioxidant and acts as a potent and ATP-competitive inhibitor of CK2 and SHP2, with an IC50 of 40 nM and a Ki of 20 nM .
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- HY-15345AS
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Tetrahydrouridine-d3 is the deuterium labeled Tetrahydrouridine[1]. Tetrahydrouridine dihydrate is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine[2][3].
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- HY-111095S2
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D-(-)-Lactic acid- 13C-1 is the 13C labeled D-(-)-Lactic acid. D-(-)-Lactic acid is a normal intermediate in the fermentation (oxidation, metabolism) of sugar. D-(-)-Lactic acid is identified to be a competitive inhibitor of ProDH (proline dehydrogenase) in plants .
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- HY-14660S
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Dabrafenib-d9 is the deuterium labeled Dabrafenib. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively[4].
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- HY-B0377S
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Famotidine- 13C,d3 is the 13C- and deuterium labeled Famotidine. Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
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- HY-Y0978S2
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Boc-Glycine-2- 13C is a 13C-labeled Linuron. Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive a
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- HY-139145S
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Etbicyphat- 13C3 is the 13C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors[1][2].
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- HY-B0334AS
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Sulbactam-d5 (sodium) is the deuterium labeled Sulbactam sodium. Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex[1][2].
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- HY-N0471S
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L-Hyoscyamine-d3 is the deuterium labeled L-Hyoscyamine. L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205)[1][2].
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- HY-135103S
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Tauro-β-muricholic acid-d4 (sodium) is the deuterium labeled Tauro-β-muricholic acid sodium. Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM[1][2][3].
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- HY-13966S
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2-Deoxy-D-glucose-d is the deuterium labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1][2].
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- HY-16569S
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Colchicine-d6 is the deuterium labeled Colchicine. Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM[1][2][3]. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs)[4].
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- HY-B0574S1
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Mefenamic Acid-d3 is the deuterium labeled Mefenamic acid. Mefenamic acid is a non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively.
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- HY-16569S1
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Colchicine-d3 is the deuterium labeled Colchicine. Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM[1][2][3]. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs)[4].
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- HY-10512S
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AR-A014418-d3 is the deuterium labeled AR-A014418. AR-A014418 is a potent, selective, and ATP-competitive GSK3β inhibitor (IC50=104 nM; Ki=38 nM)[1].
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- HY-13966S2
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2-Deoxy-D-glucose- 13C is the 13C labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1][2].
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- HY-B0334AS1
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Sulbactam-d2 (sodium) is the deuterium labeled Sulbactam sodium[1]. Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex[2][3].
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- HY-B0199AS
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Mycophenolate Mofetil-d4 hydrochloride is deuterated labeled Mycophenolate mofetil hydrochloride (HY-B0199A). Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD) type I/II with IC50s of 39 nM and 27 nM, respectively.
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- HY-B0574S2
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Mefenamic acid- 13C6 is the 13C-labeled Mefenamic acid. Mefenamic acid is a non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively.
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- HY-10805S
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Almorexant- 13C,d3 is the 13C- and deuterium labeled Almorexant. Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM, respectively.
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- HY-B0461S
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Trospium-d8 (chloride) is the deuterium labeled Trospium chloride. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors[1][2].
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- HY-D0145S
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7-Ethoxyresorufin-d5 is deuterium labeled 7-Ethoxyresorufin. 7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase[1][2].
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- HY-113468AS
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3-O-Methyldopa-d3 is deuterium labeled 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine[1].
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- HY-B0574S
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Mefenamic acid-d4 is a deuterium labeled Mefenamic acid. Mefenamic acid is a non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively[1][2].
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- HY-10163S1
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Dabigatran-d3 is the deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
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- HY-B0251S
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Eplerenone-d3 is the deuterium labeled Eplerenone. Eplerenone (Epoxymexrenone) is a selective, competitive and oreally active aldosterone antagonist with an IC50 of 138 nM. Eplerenone has low affinity for progesterone, androgen, estrogen and glucocorticoid receptors. Eplerenone can be used for hypertension and heart failure after myocardial infarction reserch[1][2].
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- HY-10163S
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Dabigatran-d4 is deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
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- HY-13966S4
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2-Deoxy-D-glucose- 13C-1 is the 13C labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1][2].
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- HY-B0113S
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Omeprazole-d3 is deuterium labeled Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].
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- HY-10195BS
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Ruboxistaurin-d6 (hydrochloride) is the deuterium labeled Ruboxistaurin hydrochloride. Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC50 of 5.9 nM[1][2].
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- HY-113468AS1
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3-O-Methyldopa-d3 (hydrate) is the deuterium labeled 3-O-Methyldopa. 3-O-Methyldopa (3-Methoxy-L-tyrosine) is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine[1].
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- HY-17395S
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Terbinafine-d3 (hydrochloride) is the deuterium labeled Terbinafine hydrochloride. Terbinafine hydrochloride (TDT 067 hydrochloride) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM[1][2]. Terbinafine hydrochloride also antibacterial activity against certain Gram-positive and Gram-negative bacteria[3].
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- HY-17395AS
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Terbinafine-d7 is the deuterium labeled Terbinafine. Terbinafine (TDT 067) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM[1][2]. Terbinafine also antibacterial activity against certain Gram-positive and Gram-negative bacteria[3].
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- HY-10255AS
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Sunitinib-d10 is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
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- HY-144354S
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S-Benzyl-DL-cysteine-2,3,3-d3 is a deuterium labeled Benzylcysteine. Benzylcysteine is an ASCT2 inhibitor that binds to ASCT2 with an apparent Ki of 780 μM. Benzylcysteine inhibit ASCT2 function based on a competitive mechanism, indicating that Benzylcysteine binds to the substrate-binding site of ASCT2[1].
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- HY-B0371S
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Terazosin-d8 is deuterium labeled Terazosin. Terazosin is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin works by relaxing blood vessels and the opening of the bladder. Terazosin has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment[1][2][3].
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- HY-10163S2
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Dabigatran- 13C6 is the 13C labeled Dabigatran[1]. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[2][3].
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- HY-B1729S
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Phenoxyethanol-d2 is the deuterium labeled Phenoxyethanol[1]. Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al[2].
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- HY-B1729S1
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Phenoxyethanol-d4 is the deuterium labeled Phenoxyethanol[1]. Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al[2].
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- HY-W728545
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Labetalol-d6 hydrochloride (AH5158-d6 hydrochloride; Sch-15719W-d6) is a deuterium labeled Labetalol (HY-121383). Labetalol is an orally active α1- and β-adrenergic receptors competitive antagonist, which exhibits anti-hypertensive property .
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- HY-117743S
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Eprosartan-d3 is the deuterium labeled Eprosartan. Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively [1].
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- HY-10873S
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N-Desethyl Sunitinib-d5 is the deuterium labeled N-Desethyl Sunitinib. N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively[1].
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- HY-10255AS1
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Sunitinib-d4 is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
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- HY-101037S1
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Sarcosine-d3 is the deuterium labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia[1][2].
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- HY-I0096S
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Indole-2-carboxylic acid- 13C is the 13C-labeled Indole-2-carboxylic acid. Indole-2-carboxylic acid is a strong inhibitor of lipid peroxidation. Indole-2-carboxylic acid (I2CA) specifically and competitively inhibits the potentiation by glycine of NMDA-gated current[1][2].
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- HY-10163S3
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Dabigatran- 13C,d3 is the 13C- and deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
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- HY-A0166S
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Cilastatin- 15N,d3 is a 15N-labeled and deuterium labeled Cilastatin. Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct[1][2][3].
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- HY-B0192S
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Alfuzosin-d7 is the deuterium labeled Alfuzosin[1]. Alfuzosin (SL 77499-10) is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin can be used in study of benign prostatic hyperplasia (BPH)[2][3].
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- HY-W758126
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(R)-Brivanib alaninate-d4 is the deuterium-labeled Brivanib (alaninate) (HY-10336). Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ .
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- HY-10873S2
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N-Desethyl Sunitinib-d5 (hydrochloride) is a deuterated labeled N-Desethyl Sunitinib . N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively .
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- HY-103392S
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Stiripentol-d9 is the deuterium labeled Stiripentol. Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediatated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59±0.07 and 0.516±0.065 μM and IC50 of 1.58 and 3.29 μM, respectively[1][2].
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- HY-101037S
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Sarcosine- 15N is the 15N-labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia[1][2].
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- HY-N0368S
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Linalool-d3 is the deuterium labeled Linalool[1]. Linalool is natural monoterpene in essential olis of coriander, acts as a competitive antagonist of Nmethyl d-aspartate (NMDA) receptor, with anti-tumor, anti-cardiotoxicity activity[2].Linalool is a PPARα ligand that reduces plasma TG levels and rewires the hepatic transcriptome and plasma metabolome[3].
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- HY-10917S
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GW2580-d6 is the deuterium labeled GW2580. GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling .
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- HY-17504AS
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Rosuvastatin-d3 is a deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM[1]. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals[2].
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- HY-14281S
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Trilostane-d3 is the deuterium-labeled Trilostane (HY-14281). Trilostane-d3 (Win 24540) is a competitive and orally active 3-β-hydroxysteroiddehydrogenase (3β-HSD) inhibitor. Trilostane-d3 is a synthetic nonhormonal steroid. Trilostane-d3 can be used for the research of breast cancer and prostate cancer .
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- HY-10119S
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Vorapaxar-d5 is deuterated labeled Vorapaxar (HY-10119). Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
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- HY-117743S1
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Eprosartan-d6 is deuterated labeled Eprosartan (HY-117743). Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
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- HY-W010201S
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Citronellol-d6 is deuterated labeled Linalool (HY-N0368). Linalool is a natural monoterpene which is a competitive NMDA receptor antagonist. Linalool is orally active and crosses the blood-brain barrier. Linalool has anticancer, antibacterial, anti-inflammatory, neuroprotective, anxiolytic, antidepressant, anti-stress, cardioprotective, hepatoprotective, nephroprotective and pulmonary protective activities .
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- HY-116852S
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Thiocolchicine-d3 is deuterium labeled Thiocolchicine. Thiocolchicine, a derivative modified in the C Ring of Colchicine (HY-16569) with enhanced biological properties. Thiocolchicine is a potent inhibitor of tubulin polymerization (IC50=2.5 µM) and competitively binds to tubulin with a Ki of 0.7 µM. Thiocolchicine induces cell apoptosis[1][2]. Thiocolchicine can be used as an ADC cytotoxin in ADC technology.
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- HY-B0290S1
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Pranlukast-d4 is deuterium labeled Pranlukast. Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [3H]LTE4, [3H]LTD4, and [3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
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- HY-N0192S
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Arbutin-d4 is deuterium labeled Arbutin. Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase in melanocytes, with Kiapp values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents[1]. Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties[2][3].
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- HY-12542S
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Dantrolene- 13C3 is the 13C3 labeled Dantrolene. Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyte glutathione reductase. Ki and IC50 values are 111.6 μM and 52.3 μM, respectively. Dantrolene is a ryanodine receptor antagonist and Ca2+ signaling stabilizer. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.
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- HY-113038AS
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α-Hydroxyglutaric acid- 13C5 (sodium) is the 13C labeled α-Hydroxyglutaric acid sodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) sodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid sodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[2].
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- HY-A0030S
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Fesoterodine-d7 (fumarate) is the deuterium labeled Fesoterodine fumarate[1]. Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB)[2][3].
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- HY-W011834S
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2'-O-Methylcytidine-d3 is deuterium labeled 2'-O-Methylcytidine (HY-W011834). 2'-O-Methylcytidine is a 2'-substituted nucleoside as a inhibitor of HCV replication. 2'-O-Methylcytidine inhibits RNA-dependent RNA polymerase (NS5B)-catalyzed RNA synthesis in vitro, in a manner that is competitive with substrate nucleoside triphosphate.
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- HY-14664DS
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(3S,5R)-Fluvastatin-d6 is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
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- HY-13011S
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Alectinib-d8 is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
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- HY-13011S1
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Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
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- HY-113038AS1
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α-Hydroxyglutaric acid-d4 (disodium) is the deuterium labeled α-Hydroxyglutaric acid disodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[2].
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- HY-14664CS
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(3S,5R)-Fluvastatin-d6 (sodium) is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
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- HY-W401531S
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(R)-3-O-Methyldopa-d3 is a deuterium labeled (R)-3-O-Methyldopa, and (R)-3-O-Methyldopa is an R-enantiomer of 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of L-DOPA and dopamine[1][2].
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- HY-W401531S1
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(R)-3-O-Methyldopa-d3 (hydrochloride) is a deuterium labeled (R)-3-O-Methyldopa, and (R)-3-O-Methyldopa is an R-enantiomer of 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of L-DOPA and dopamine[1][2].
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- HY-B0091S
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Adapalene-d3 is the deuterium labeled Adapalene. Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity[1][2][3].
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- HY-50878S
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Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
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- HY-B0236S1
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6-Aminocaproic acid-d10 is the deuterium labeled 6-Aminocaproic acid. 6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders[1][2].
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- HY-13635S
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Finasteride-d9 is deuterium labeled Finasteride. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia[1][2][3].
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- HY-B0236S
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6-Aminocaproic acid-d6 is deuterium labeled 6-Aminocaproic acid. 6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders[1][2].
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- HY-B0368S
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Captopril-d3 is deuterium labeled Captopril. Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM[1][2][3].
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- HY-B0442S
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Vardenafil-d5 is deuterium labeled Vardenafil. Vardenafil is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction[1][2].
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- HY-B1126S
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Orphenadrine-d3 (hydrochloride) is the deuterium labeled Orphenadrine hydrochloride[1]. Orphenadrine hydrochloride is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine hydrochloride relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine hydrochloride is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases[2][3].
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- HY-W010410S
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Oct-1-en-3-ol-d3 is deuterated labeled Linalool (HY-N0368). Linalool is a natural monoterpene which is a competitive NMDA receptor antagonist. Linalool is orally active and crosses the blood-brain barrier. Linalool has anticancer, antibacterial, anti-inflammatory, neuroprotective, anxiolytic, antidepressant, anti-stress, cardioprotective, hepatoprotective, nephroprotective and pulmonary protective activities .
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- HY-B0113S1
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Omeprazole-d3-1 is the deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
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- HY-N0215S6
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DL-Phenylalanine-d5 (hydrochloride) is the deuterium labeled DL-Phenylalanine hydrochloride. L-Phenylalanine hydrochloride is an essential amino acid isolated from Escherichia coli. L-Phenylalanine hydrochloride is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine hydrochloride is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine hydrochloride is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
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- HY-A0009S
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Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD)[1][2][3].
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- HY-17504BS2
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Rosuvastatin- 13C,d3 sodium is 13C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
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- HY-17387S1
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(-)-Huperzine A-d4 hydrochloride is deuterated labeled (-)-Huperzine A (HY-17387). (-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease .
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- HY-N6948S
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Linalyl acetate-d6 is deuterated labeled Omeprazole (HY-B0113). Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
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- HY-B0113S4
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Omeprazole-d3 sodium is deuterated labeled Omeprazole (HY-B0113). Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
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- HY-13716S
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Noscapine-13C,d3 is a deuterated labeled Noscapine . Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier .
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- HY-B0113S3
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Omeprazole- 13C,d3 is a 13C-labeled and deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
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- HY-17623S
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Tegoprazan (CJ-12420; RQ-00000004), a potassium-competitive acid blocker, is a reversible, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H +/K +-ATPases in vitro. Tegoprazan significantly improves colitis in mice and enhances the intestinal epithelial barrier function. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases .
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- HY-17422S1
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Acyclovir-d4 is the deuterium labeled Acyclovir. Acyclovir (Aciclovir) is a guanosine analogue and an orally active antiviral agent. Acyclovir inhibits HSV-1 (IC50 of 0.85 μM), HSV-2 (IC50 of 0.86 μM) and varicella-zoster virus. Acyclovir can be phosphorylated by viral thymidine kinase (TK), and Acyclovir triphosphate interferes with viral DNA polymerization through competitive inhibition with guanosine triphosphate and obligatory chain termination[1][2][3]. Acyclovir prevents bacterial infections during induction therapy for acute leukaemia[4].
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- HY-N0215S13
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L-Phenylalanine-d is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
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- HY-B0442AS
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Vardenafil-d5 hydrochloride is deuterated labeled Vardenafil hydrochloride (HY-B0442A). Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
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- HY-B0267BS
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Oxybutynin-d5 hydrochloride is deuterated labeled (R)-Oxybutynin hydrochloride (HY-B0267B). (R)-Oxybutynin hydrochloride, a (R)-isomer of Oxybutynin hydrochloride, is an orally active muscarinic receptor antagonist. (R)-Oxybutynin hydrochloride has antimuscarinic, antispasmodic and anticholinergic activity, competitively antagonizes Carbachol-induced contractions. (R)-Oxybutynin hydrochloride can be used for researching incontinence due to neurogenic bladder dysfunction . (R)-Oxybutynin hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-N0215S3
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L-Phenylalanine-d2 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
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- HY-N0215S2
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L-Phenylalanine- 13C is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
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- HY-N0215S
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L-Phenylalanine-d7 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
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- HY-N0215S1
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L-Phenylalanine-d8 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
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- HY-18346S
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Mozavaptan-d6 (OPC-31260-d6) is the deuterium labeled Mozavaptan. Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment .
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- HY-N0215S5
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L-Phenylalanine- 15N is the 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
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- HY-N0215S10
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L-Phenylalanine- 13C9 is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
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- HY-N0215S12
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1 Publications Verification
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L-Phenylalanine-d5 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
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- HY-N0215S7
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L-Phenylalanine-3- 13C is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
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- HY-N0215S8
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L-Phenylalanine- 13C6 is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
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- HY-50878AS
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Crizotinib-d9 hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
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- HY-101193S
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Zinc Protoporphyrin-d2, 15N2 is 15N and deuterated labeled Zinc Protoporphyrin (HY-101193). Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is an orally active and competitive heme oxygenase-1 (HO-1) inhibitor and markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2 . Zinc Protoporphyrin is used as a screening marker of iron deficiency in individual pregnant women and children, but also to assess population iron status in combination with haemoglobin concentration . Zinc Protoporphyrin has anti-cancer activity .
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- HY-N0215S11
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L-Phenylalanine- 13C9, 15N is the 13C- and 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
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- HY-N0215S14
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L-Phenylalanine- 15N,d8 is the deuterium and 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca2+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
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- HY-N0215S9
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L-Phenylalanine- 13C9, 15N,d8 is the deuterium, 13C-, and 15-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
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Product Name |
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Classification |
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- HY-23460
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4-Ethynyl-L-phenylalanine
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Alkynes
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p-Ethynylphenylalanine (4-Ethynyl-L-phenylalanine) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a Ki of 32.6 μM . p-Ethynylphenylalanine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-23460A
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4-Ethynyl-L-phenylalanine hydrochloride
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Alkynes
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p-Ethynylphenylalanine hydrochloride (4-Ethynyl-L-phenylalanine hydrochloride) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a Ki of 32.6 μM . p-Ethynylphenylalanine (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-104066
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Xiliertinib; HMPL-309
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Alkynes
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Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-149880
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Alkynes
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c-Met-IN-18 is ATP competitive type-III c-MET inhibitor of WT and D1228V mutant c-MET. c-Met-IN-18 has inhibitory for WT/D1228V with an IC50 value of 0.013/0.20 e.c-Met-IN-18 can be used for the research of c-MET driven cancers . c-Met-IN-18 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-123311
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Azide
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CP59430 is an azide analog of the α-adrenaline receptor antagonist Prazosin (HY-B0193). P59430 behaves as a competitive antagonist of α1-adrenaline receptor before photolysis. After photolysis, it specifically and irreversibly labels α1-adrenaline receptor and exhibits non-competitive antagonist activity. CP59430 can be used for the study of receptor molecular characterization .
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- HY-123199
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SABA
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Azide
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Serotonin azidobenzamidine is an arylazido derivative of 5-hydroxytryptamine (HY-B1473A). Serotonin azidobenzamide competitively inhibits [3H]5-hydroxytryptamine uptake by rat cortical synaptosomes in the dark with a Ki of 130 nM .
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- HY-104066A
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Xiliertinib tartrate; HMPL-309 tartrate
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Alkynes
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Theliatinib (Xiliertinib) tartrate is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib (tartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-146691
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Alkynes
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hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible hMAO-B inhibitor, with an IC50 of 4 nM. hMAO-B-IN-2 shows low toxicity and good neuroprotective effects in SH-SY5Y cell. hMAO-B-IN-2 can be used for alzheimer’s disease research . hMAO-B-IN-2 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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| Cat. No. |
Product Name |
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Classification |
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- HY-W011834
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Nucleosides and their Analogs
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2'-O-Methylcytidine is a 2'-substituted nucleoside as a inhibitor of HCV replication. 2'-O-Methylcytidine inhibits RNA-dependent RNA polymerase (NS5B)-catalyzed RNA synthesis in vitro, in a manner that is competitive with substrate nucleoside triphosphate .
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- HY-13859
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L-FMAU
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Nucleosides and their Analogs
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Clevudine (L-FMAU), a nucleoside analog of the unnatural L-configuration, has potent anti-HBV activity with long half-life, low toxicity. Clevudine is a non-competitive inhibitor that is not incorporated into the viral DNA but rather binds to the polymerase. Clevudine is active against cowpox virus respiratory infection in mice .
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- HY-W097792
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5'-O-DMT-dU
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Nucleoside Phosphoramidites
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5'-O-(4,4'-Dimethoxytrityl)-2'-deoxyuridine (5'-O-DMT-dU) is a competitive inhibitor of E. coli dUTP nucleotidohydrolase (dUTPase), with the Ki higher than 1000 μM. 5'-O-(4,4'-Dimethoxytrityl)-2'-deoxyuridine can be used in machine-assisted DNA synthesis by synthesizing nucleosidic phosphoramidite blocks .
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