Search Result
Results for "
dose-dependently
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
14
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-107627
-
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Melanocortin Receptor
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Inflammation/Immunology
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MCL0020 is a potent and selective melanocortin MC4 receptor antagonist, with an IC50 of 11.63 nM. MCL0020 dose-dependently and significantly attenuates restraint stress-induced anorexia without affecting food intake .
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-
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- HY-136676
-
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Renin
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Cancer
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Cgp 38560 methanesulfonate is a well-tolerated renin inhibitor. Cgp 38560 methanesulfonate caused a dose-dependent decrease in angiotensin II and plasma renin activity, and a dose-dependent increase in active renin.
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-
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- HY-142052
-
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5a(6)-Anhydrotetracycline
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Antibiotic
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Infection
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Anhydrotetracycline shows dose-dependent and potent inhibition of tetracycline destructases in vitro .
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-
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- HY-118683
-
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Others
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Others
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KR-31378 is a neuroprotectant with dose-dependent pharmacokinetic properties and relevant activity in rats. After intravenous and oral administration of KR-31378 in rats, its pharmacokinetic parameters showed dose-dependent changes, such as decreased clearance with increasing doses, good oral absorption, and comparable AUCs for intravenous and oral administration at different doses.
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-
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- HY-N11922
-
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Others
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Neurological Disease
|
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Ipalbidine is an alkaloid extracted from ipomoea Hardwickki Hemsl. Ipalbidine has dose-dependent analgesic effects .
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-
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- HY-157533
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Bacterial
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Others
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AcrB-IN-5 (compound 8) inhibits AcrB and blocks the efflux pump in a dose-dependent manner .
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-
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- HY-W127334
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Biochemical Assay Reagents
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Others
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N-Palmitoyl phosphatidylethanolamine (Tripelargonin) is endogenous lipid anorectic hormone, significantly reduces food intake in a dose-dependent manner
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-
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- HY-19539
-
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Ras
|
Cancer
|
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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 .
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-
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- HY-117019
-
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COX
|
Cancer
|
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LY150310 inhibits thromboxane synthase, cyclooxygenase, and thrombin activation. LY150310 inhibits spontaneous lung metastasis in a dose-dependent manner.
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-
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- HY-101440A
-
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CHF-3381
|
iGluR
|
Neurological Disease
|
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Indantadol (CHF-3381) hydrochloride is a novel putative NMDA antagonist. Indantadol blocks the NMDA receptor in a dose-dependent and prevents cell damage .
|
-
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- HY-101595
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Others
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Others
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RPH-2823, a basic triamterene derivative, induces a dose-dependent decrease in short-circuit current (SCC) and increase in transepithelial electrical resistance .
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-
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- HY-N5099
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Others
|
Metabolic Disease
|
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N-Vanillyldecanamide, a capsaicinoid isolated from the fruits of Capsicum annuum, significantly reduced the radical length of Lactuca sativa seedling in a dose-dependent manner .
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-
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- HY-N8816
-
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NF-κB
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Inflammation/Immunology
|
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Stipuleanoside R2 inhibits NF-κB activation stimulated by TNFα in a dose-dependent manner with IC50 value of 4.1 μM .
|
-
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- HY-103188
-
|
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Adenosine Receptor
|
Neurological Disease
|
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PD81723 is an adenosine receptor binding enhancer. PD81723 enhances the inhibition of exogenous adenosine in a dose-dependent manner in hippocampal brain sections .
|
-
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- HY-B0163
-
-
-
- HY-B0163A
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-
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- HY-12289A
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VS-6063 hydrochloride; PF 04554878 hydrochloride
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FAK
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Cancer
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Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.
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- HY-111408
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Deubiquitinase
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Cancer
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EOAI3402143 is a deubiquitinase (DUB) inhibitor, which inhibits dose-dependently inhibits Usp9x/Usp24 and Usp5.
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-
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- HY-123786
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Others
|
Cancer
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NSC745887 (compound 25) is an anti-cancer agent. NSC745887 exhibits dose-dependent inhibition of proliferation in all 60 cancer cell lines .
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- HY-167872
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Cytochrome P450
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Others
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Bifeprofen, a cytochrome P450 2C9 (CYP2C9) inhibitor, exhibits dose-dependent inhibition (75 μM, 50%) .
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-
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- HY-N0775
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7-Isocorynoxeine
|
5-HT Receptor
|
Neurological Disease
|
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Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM.
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-
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- HY-104073
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-
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- HY-N6621
-
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Topoisomerase
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Cancer
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Hippeastrine, an active alkaloid, exhibits a good dose-dependent inhibitory effect against topoisomerase I (Top I) with an IC50 at 7.25 μg/mL. Antiproliferative and anticancer activities .
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-
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- HY-N1159
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NF-κB
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Inflammation/Immunology
|
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Teuclatriol is an NF-κB inhibitor can be isolated from salvia mirzayanii, has anti-inflammatory effects. Teuclatriol inhibits TNF-α secretion in a dose-dependent manner .
|
-
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- HY-B1914
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-
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- HY-136644
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Others
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Others
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PD-217014-methyl ester is an α?δ ligand with visceral analgesic activity and can inhibit visceral hypersensitivity, and its anti-hyperalgesic effect is dose-dependent.
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-
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- HY-136644A
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Others
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Others
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PD-217014 is an α2δ ligand with visceral analgesic activity and can inhibit visceral hypersensitivity reactions. Its anti-allodynic effect is dose-dependent.
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- HY-124597
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Others
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Inflammation/Immunology
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ARN726 is a potent NAAA (N-acylethanolamine acid amidase) inhibitor with an IC50 of 0.073 µM. ARN726 decreases alcohol self-administration in a dose-dependent manner .
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- HY-P3730
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CDK
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Cancer
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Cdk2/Cyclin Inhibitory Peptide I (Tat-LFG), a CDK2 inhibitor, kills U2OS osteosarcoma cells in a dose-dependent manner .
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-
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- HY-P3731
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CDK
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Cancer
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Cdk2/Cyclin Inhibitory Peptide II (Tat-LDL), a CDK2 inhibitor, kills U2OS osteosarcoma cells in a dose-dependent manner .
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-
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- HY-122874
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-
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- HY-N11950
-
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Others
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Others
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N-Vanillyloctanamide is a capsaicinoid that has the activity of inhibiting the root growth of plant seedlings. N-Vanillyloctanamide significantly reduces the root length of Lactuca sativa (seedling) in a dose-dependent manner .
|
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- HY-N2383
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(1R,2S,3S,4S,6R)-4-Amino-6-(hydroxymethyl)cyclohexane-1,2,3-triol
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Glycosidase
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Metabolic Disease
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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 .
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- HY-121866
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Topoisomerase
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Cancer
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Hippeastrine hydrobromide is an active alkaloid that exhibits a good dose-dependent inhibitory effect on topoisomerase I (Top I) with an IC50 of 7.25 μg/mL. Hippeastrine hydrobromide exhibits antiproliferative and anticancer activities.
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-
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- HY-118364
-
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RAR/RXR
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Metabolic Disease
|
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AGN 190727 is a structural isomer of AGN 190121 and has no activating effect on RAR/RXR. AGN 190121 is a RAR-specific agonist that causes a dose-dependent increase in serum triglycerides, leading to hypertriglyceridemia.
|
-
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- HY-116560
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-
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- HY-169210
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Apoptosis
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Cancer
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ECDD-S18 (compund ECDD-S18) induces apoptosis in a dose-dependent manner, effectively targets vacuolar ATPase (V-ATPase), and impairs lysosomal acidification .
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-
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- HY-137131
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DC-Cholesterol hydrochloride
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Amyloid-β
Liposome
|
Neurological Disease
|
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DC-Chol hydrochloride could inhibit Aβ40 fibril formation under appropriate experimental conditions. DC-Chol hydrochloride strongly inhibits amyloidogenesis of oxidized hCT in a dose-dependent manner .
|
-
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- HY-107164
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4-Hydroxythiomarinol C
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Antibiotic
Bacterial
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Infection
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Thiomarinol A (4-Hydroxythiomarinol C) is a potent antibiotic. Thiomarinol A is a hybrid of dithiolopyrrolone and marinolic acid. Thiomarinol A shows antimicrobial activity. Thiomarinol A inhibits MRSA IleRS in a dose-dependent with a Ki app value of 19 nM .
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-
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- HY-158051
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PKC
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Neurological Disease
|
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CIDD-0072424 selectively inhibits Protein Kinase C-epsilon (PKCε) (Ki=54 nM). CIDD-0072424 reduces ethanol consumption and preference in a dose-dependent manner .
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-
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- HY-13809
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XL-139
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Smo
Apoptosis
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Cancer
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BMS-833923 (XL-139) is an orally biocompatible Smoothened (Smo) inhibitor with anti-tumor activity. It can inhibit the binding of BODIPY cyclopamine to SMO in a dose-dependent manner with an IC50 of 21 nM .
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- HY-110241
-
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nAChR
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Neurological Disease
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Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of agents that includes varenicline and cytisine for smoking cessation. Dianicline dihydrochloride increases cessation rates in a dose-dependent manner .
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-
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- HY-111317
-
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Sirtuin
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Metabolic Disease
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SIRT1 activator 3 is a potent activator of Sirt1 and suppresses TNF-α in a dose-dependent manner. SIRT1 activator 3 has the potential for anti-obesity or anti-diabetic researches .
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-
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- HY-12956B
-
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Prostaglandin F2β; PGF2β
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Endogenous Metabolite
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Others
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(5R)-Dinoprost is a metabolite produced by cyclooxygenase metabolism of arachidonic acid. (5R)-Dinoprost (Prostaglandin F2β) induces dose-dependent release of hexose containing mucin .
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- HY-123767
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HBV
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Infection
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HEC72702 is a potent and orally active hepatitis B virus capsid inhibitor with an EC50 values of 0.039 µM. HEC72702 dose-dependently reduced HBV DNA in both the plasma and livers .
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- HY-118541
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Others
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Others
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RH-5849 is an orally active agonist for non-steroidal ecdysteroid, which inhibits the larval growth of Plodia inferpuncteila in a dose-dependent manner. RH-5849 exhibits molting hormone activity .
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- HY-N6621A
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Topoisomerase
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Cancer
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Hippeastrine hydrobromide is an active alkaloid that exhibits a good dose-dependent inhibitory effect on topoisomerase I (Top I) with an IC50 of 7.25?μg/mL. Hippeastrine hydrobromide exhibits antiproliferative and anticancer activities .
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- HY-123239
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GPR55
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Neurological Disease
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KLS-13019 is an orally active GPR55 receptor antagonist and a structural analogue of cannabidiol (CBD). It can prevent and reverse chemotherapy-induced peripheral neuropathy (CIPN) in a dose-dependent manner in rats .
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- HY-159885
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Others
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Cancer
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MG-B-28 is an inhibitor of BTLA-HVEM with an IC50 value of 906 nM. MG-B-28 promotes T-cell activation in a dose-dependent manner by blocking the BTLA-HVEM interaction .
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- HY-W416440
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ASL-8123 hydrochloride
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Adrenergic Receptor
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Cardiovascular Disease
Metabolic Disease
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Esmolol acid (ASL-8123) hydrochloride is a weak β-adrenoceptor antagonist. Esmolol acid hydrochloride dose-dependently inhibits the heart rate and diastolic pressure responses to isoproterenol and can be used in renal failure studies .
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- HY-N6681
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Caspase
Bacterial
Apoptosis
Antibiotic
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Infection
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15-acetoxyscirpenol, one of acetoxyscirpenol moiety mycotoxins (ASMs), strongly induces apoptosis and inhibits Jurkat T cell growth in a dose-dependent manner by activating other caspases independent of caspase-3 .
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- HY-N5060
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4-Allylanisole
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Parasite
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Neurological Disease
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Estragole (4-Allylanisole), a relatively nontoxic volatile terpenoid ether, is a major component of the essential oil of many plants. Estragole dose-dependently blocks nerve excitability . Estragole displays anti-toxoplasma activity .
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- HY-100585
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Splitomycin
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HDAC
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Cancer
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Splitomicin (Splitomycin) is a selective Sir2p inhibitor. Splitomicin inhibits NAD +-dependent HDAC activity of Sir2 protein. Splitomicin induces dose-dependent inhibition of HDAC in the yeast extract with an IC50 of 60 μM .
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- HY-119819
-
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Bacterial
Parasite
Antibiotic
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Infection
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Psicofuramine a nucleoside antibiotic and has the inhibition of xanthosine 5'-phosphate aminase. Psicofuranine also specifically inhibits GMP synthase, and interrupts parasite growth. Psicofuranine exhibits a dose-dependent inhibition of P. falciparum growth .
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- HY-121377
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-
- HY-122049
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-
- HY-P10032
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- HY-121007
-
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Web2170
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Others
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Others
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Bepafant (Web2170) is a platelet-activating factor (PAF) antagonist that protects against anaphylactic lethality in active and passive anaphylaxis models in mice and guinea pigs in a dose-dependent manner and attenuates bronchoconstriction and blood pressure changes in anaphylaxis.
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- HY-137820
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DNA/RNA Synthesis
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Others
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Brr2-IN-3 is a potent and selective Brr2 helicase allosteric Inhibitor. Brr2-IN-3 inhibits helicase activity in dose-dependent manner with an IC50 value of 1.3 μM .
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- HY-114850A
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Prostaglandin F2β tromethamine; PGF2β tromethamine
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Endogenous Metabolite
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Others
|
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(5R)-Dinoprost tromethamine (Prostaglandin F2β tromethamine) is a metabolite produced by the metabolism of arachidonic acid cyclooxygenase. (5R)-Dinoprost tromethamine induces dose-dependent release of hexosaccharide containing mucin .
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- HY-10845
-
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Others
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Others
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CGI-17341 is a 5-nitroimidazole antibacterial agent that has the activity of inhibiting sensitive and multidrug-resistant strains of Mycobacterium tuberculosis in vitro and prolonging the survival time of mice infected with Mycobacterium tuberculosis in vivo in a dose-dependent manner.
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- HY-121931
-
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Lipoxygenase
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Cancer
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AA863 is a 5-lipoxygenase inhibitor with activity in inhibiting the proliferation of human glioma cells. AA863 exhibits significant and dose-dependent inhibitory effects in monolayer cultured glioma cells with an IC50 of 9.0 micromolar .
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- HY-137831
-
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Apoptosis
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Cancer
|
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TLBC, a boronic-chalcone derivative, shows a dose-dependent inhibition with IC50 values of 5.5-25.5 μM in various glioma cell lines. TLBC induces apoptosis independent of changes to the tumor suppressor p53 .
|
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- HY-10787
-
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H 376/95
|
Thrombin
|
Cardiovascular Disease
|
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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 .
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- HY-103101
-
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5-HT Receptor
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Others
|
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LP44 (hydrochloride) is a selective 5-HT7 agonist with Ki of 0.22 nM. LP44 (hydrochloride) induces hypothermic effect in a dose-dependent manner by intracerebroventricular injection. LP44 (hydrochloride) not causes considerable hypothermic response by intraperitoneal administration .
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- HY-P3462A
-
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CGRP Receptor
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Metabolic Disease
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Cagrilintide acetate is a non-selective AMYR/CTR agonist and long-acting acylated amylase analogue. Cagrilintide acetate causes a reduction in food intake and significant weight loss in a dose-dependent manner. Cagrilintide acetate can be used in obesity studies .
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- HY-149856
-
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Microtubule/Tubulin
Apoptosis
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Cancer
|
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Tubulin inhibitor 33, a tubulin polymerization inhibitor, inhibits tubulin polymerization in a dose-dependent manner with an IC50 of 9.05 μM. Tubulin inhibitor 33 has antitumor effects and induces cell apoptosis that can be used for antitumor research .
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- HY-157124
-
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Tyrosinase
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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 .
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-
- HY-106347
-
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CR 2945
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Cholecystokinin Receptor
|
Inflammation/Immunology
|
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Itriglumide (CR 2945) is an anthranilic acid derivative. Itriglumide is a potent and selective CCKB receptor antagonist, with an IC50 of 2.3 nM. Itriglumide antagonizes the response to gastrin in a dose-dependent manner with an IC50 of 5.9 nM. Itriglumide shows antisecretory and antiulcer activity .
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- HY-B0163AR
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Adrenergic Receptor
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Neurological Disease
Endocrinology
|
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Detomidine (hydrochloride) (Standard) is the analytical standard of Detomidine (hydrochloride). This product is intended for research and analytical applications. Detomidine hydrochloride, an imidazole derivative, is a potent α2-adrenergic agonist. Detomidine hydrochloride produces dose-dependent analgesic effects .
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- HY-167858
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Thrombin
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Cardiovascular Disease
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LK-732 is a thrombin inhibitor with anti-thrombotic activity.LK-732 has a dose-dependent inhibition of hypercoagulability in the model, with an IC50 of 1.3 mg/kg. LK-732 can be used in cardiovascular and cerebrovascular research .
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- HY-159989
-
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Epigenetic Reader Domain
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Cancer
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UNC10142 (Compound 44) is a first-in-class small molecule antagonist of CHD1 that binds with an IC50 value of 1.7 μM. UNC10142 leads to a dose-dependent reduction in viability in PTEN-deficient prostate cancer cells .
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- HY-121356
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- HY-143468
-
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Apoptosis
MEK
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Cancer
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MEK-IN-5 is a potent MEK inhibitor and NO donor. MEK-IN-5 significantly reduces the levels of pMEK and pERK in a dose-dependent and time-dependent manner. MEK-IN-5 induces apoptosis in MDA-MB-231 cells .
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- HY-W042191
-
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Fungal
Apoptosis
Caspase
Bcl-2 Family
MDM-2/p53
PARP
|
Infection
Cancer
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Oxychloroaphine could be isolated from the bacterium Pantoea agglomerans naturally present in soil. Oxychloroaphine has broad-spectrum antifungal activity. Oxychloroaphine has cytotoxicity in a dose-dependent manner and induces apoptosis. Oxychloroaphine can be used in research of cancer .
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- HY-14919A
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MN-029
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Others
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Cancer
|
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Denibulin (MN-029) hydrochloride is an anti-angiogenic agent with anticancer activity. It can cause rapid closure of blood vessels in solid tumors and lead to dose-dependent killing of tumor cells, effectively enhancing the antitumor effects of radiation and cisplatin chemotherapy .
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-
- HY-114748
-
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Bacterial
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Infection
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AHU1 is a compound that inhibits the expression of Shiga toxin type 2 in Escherichia coli O157:H7, demonstrating a dose-dependent reduction in toxin activity by interfering with the SOS response through its effects on RecA.
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-
- HY-P1235A
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Atrial Natriuretic Peptide (ANP) (1-28), human, porcine acetate
|
Endothelin Receptor
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Cardiovascular Disease
Endocrinology
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Carperitide acetate (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine acetate) is a 28-amino acid hormone, that is normally produced and secreted by the human heart in response to cardiac injury and mechanical stretch. Carperitide acetate inhibits endothelin-1 secretion in a dose-dependent way.
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- HY-P1329
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Opioid Receptor
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Neurological Disease
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CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity .
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-
- HY-146681
-
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PAK
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Cancer
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PAK1-IN-1 is a potent and selective PAK1 inhibitor with an IC50 of 9.8 nM. PAK1-IN-1 inhibits the migration and invasion of PAK1-related tumour cells in a dose-dependent manner .
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-
- HY-108436
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Phosphodiesterase (PDE)
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Cancer
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Deltazinone 1, a pyrazolopyridazinone, is a highly selective PDEδ inhibitor with a KD of 8 nM. Deltazinone 1 inhibits the PDEδ-Ras interaction. Deltazinone 1 shows a dose-dependent inhibitory response on proliferation in oncogenic KRas-dependent cell lines .
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- HY-N4209
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Others
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Cardiovascular Disease
|
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3α-Dihydrocadambine is a natural product isolated from the heartwoods of Anthocephalus cadamba.3α-Dihydrocadambine exhibits dose-dependent hypotensive and anti-hypertensive effects in anesthetized normotensive rats and in conscious spontaneously hypertensive rats .
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-
- HY-162153
-
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FGFR
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Cancer
|
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CYY292 is an FGFR1 inhibitor that specifically targets the FGFR1/AKT/Snail pathway in GBM cells. CYY292 dose-dependently inhibits cancer cell proliferation, epithelial-mesenchymal transition, stemness, invasion, and migration in vitro .
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- HY-B1914R
-
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Mitochondrial Metabolism
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Neurological Disease
|
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Tebufenpyrad (Standard) is the analytical standard of Tebufenpyrad. This product is intended for research and analytical applications. Tebufenpyrad can induce mitochondrial dysfunction and oxidative damage. Tebufenpyrad induces dose-dependent cell death on N27 cells, with an EC50 value of 3.98 μM .
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- HY-N0775R
-
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5-HT Receptor
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Neurological Disease
|
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Isocorynoxeine (Standard) is the analytical standard of Isocorynoxeine. This product is intended for research and analytical applications. Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM.
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-
- HY-144818
-
|
|
Apoptosis
Microtubule/Tubulin
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Cancer
|
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Tubulin inhibitor 23 is a potent Tubulin inhibitor with an IC50 of 4.8 µM. Tubulin inhibitor 23 induces cell apoptosis. Tubulin inhibitor 23 shows antiangiogenic activity in a dose-dependent manner. Tubulin inhibitor 23 has the potential for the research of leukaemia .
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-
- HY-P5859
-
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α-PMTX
|
Biochemical Assay Reagents
|
Neurological Disease
|
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α-Pompilidotoxin (α-PMTX) is a neurotoxin that can be obtained from the venom of Anoplius safnariensis. α-Pompilidotoxin reversibly and dose-dependently enhances excitatory postsynaptic currents (EPSCs). α-Pompilidotoxin is a useful tool in the field of neuroscience research .
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- HY-P3100
-
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Parasite
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Infection
|
|
Orfamide A is a major metabolite of insecticidal biosurfactant in Pseudomonas sp. F6 and has aphidicidal activity. Orfamide A can be used for aphid control in organic agriculture. Orfamide A exhibits dose-dependent mortality against aphids with an LC50 value of 34.5 μg/mL .
|
-
- HY-116498
-
|
|
Others
|
Infection
|
|
Penigequinolone A is an alkaloid isolated from Penicillium. It is lethal to P. penetrans (LD50=100 mg/L) but has no effect on C. elegans at concentrations up to 1000 mg/L.1 Penigequinolone A also accelerates the root growth of rice seedlings in a dose-dependent manner.
|
-
- HY-B1041
-
|
Pimagedine hydrochloride; GER-11; Aminoguanidinium chloride
|
NO Synthase
Apoptosis
|
Endocrinology
|
|
Aminoguanidine hydrochloride (Pimagedine hydrochloride) is an inhibitor of diamine oxidase and nitric oxide synthase. Aminoguanidine hydrochloride has a dose-dependent inhibitory effect on apoptosis induced by Doxorubicin (HY-15142). Aminoguanidine hydrochloride has antioxidant properties. Aminoguanidine hydrochloride can be used in diabetic nephropathy research .
|
-
- HY-P1329A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity .
|
-
- HY-139692
-
|
|
EAAT
|
Neurological Disease
|
|
EAAT2 activator 1 is the potent activator of excitatory amino acid transporter 2 (EAAT2). EAAT2 is the major glutamate transporter and functions to remove glutamate from synapses. EAAT2 activator 1 increases EAAT2 protein levels dose-dependently .
|
-
- HY-P0262A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
Metabolic Disease
|
|
Galantide TFA is a reversible and non-specific galanin (GAL) receptor antagonist. Galantide TFA dose-dependently shows antagonism to galanin-induced K + conductance with an IC50 value of 4 nM. Galantide TFA can be used for the research of neurological disease and hormone metabolism research .
|
-
- HY-128431
-
|
|
Reactive Oxygen Species
|
Neurological Disease
Metabolic Disease
|
|
Arochlor 1254 is a polychlorinated biphenyl (PCB) mixture with biphenyl and 54% chlorine. Aroclor 1254 reduced cell viability and induced overproduction of intracellular reactive oxygen species in a dose-dependent manner. Arochlor 1254 exposure reduces calcium homeostasis, osteoblast differentiation and bone formation .
|
-
- HY-N11911
-
|
(-)-Verazine
|
Fungal
|
Infection
Neurological Disease
|
|
Verazine ((-)-Verazine) is an anti-Fungal Agent that can be found in the dried roots and rhizoma of Veratrum maackii Regel. Verazine causes DNA damage in the cerebellum and cerebral cortex of mice in a dose-dependent manner. Verazine can be used in the study of fungal infections and neurological diseases .
|
-
- HY-P10032A
-
-
- HY-B1041A
-
|
Pimagedine; GER-11(free base) ; Aminoguanidinium
|
NO Synthase
Apoptosis
|
Endocrinology
|
|
Aminoguanidine (Pimagedine hydrochloride) is an inhibitor of diamine oxidase and nitric oxide synthase. Aminoguanidine has a dose-dependent inhibitory effect on apoptosis induced by Doxorubicin (HY-15142). Aminoguanidine has antioxidant properties. Aminoguanidine can be used in diabetic nephropathy research .
|
-
- HY-125615
-
|
|
Glycoprotein VI
|
Cardiovascular Disease
Others
|
|
DMP 728 methanesulfonate is a platelet glycoprotein (GP) IIb/IIIa receptor antagonist. DMP 728 methanesulfonate shows dose-dependent antiplatelet and antithrombotic effects. DMP 728 methanesulfonate can be used in the study of effective antithrombotic agents in thromboembolic diseases of coronary and peripheral arteries .
|
-
- HY-15297
-
|
OPC-8212
|
Phosphodiesterase (PDE)
|
Infection
Cardiovascular Disease
|
|
Vesnarinone (OPC-8212) is an orally active phosphodiesterase 3 (PDE3) inhibitor. Vesnarinone can increase in calcium flux and decrease in potassium flux. Vesnarinone shows dose-dependent positive inotropic activity. Vesnarinone can be used in heart failure research .
|
-
- 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-144448
-
|
|
FAK
Apoptosis
|
Cancer
|
|
FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC50= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis .
|
-
- HY-121725
-
|
|
STAT
|
Cancer
|
|
MM-206, a STAT3 activity inhibitor, potently inhibits the STAT3 SH2 domain-phosphopeptide interaction with IC50 of 1.2 μM. MM-206 demonstrates dose-dependent induction of apoptosis in acute myeloid leukemia (AML) cell lines .
|
-
- 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-137111
-
|
|
5-HT Receptor
PERK
|
|
|
p-MPPF dihydrochloride is a selective 5-HT antagonist that dose-dependently antagonizes the reduction of phosphorylated Erk1/2 levels in the hippocampus induced by 8-OH-DPAT (HY-112061) in rats. p-MPPF dihydrochloride can be used for neurological disease research .
|
-
- HY-137111A
-
|
|
5-HT Receptor
PERK
|
|
|
p-MPPF is a selective 5-HT antagonist that dose-dependently antagonizes the reduction of phosphorylated Erk1/2 levels in the hippocampus induced by 8-OH-DPAT (HY-112061) in rats. p-MPPF can be used for neurological disease research .
|
-
- HY-15480
-
|
JAK2 Inhibitor V; Z3
|
JAK
|
Cancer
|
|
NSC 42834 (JAK2 Inhibitor V), a novel specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.
|
-
- HY-145846
-
|
|
NO Synthase
Interleukin Related
|
Inflammation/Immunology
|
|
iNOs-IN-1 (YPW) is a potent inducible nitric oxide synthase (iNOS) inhibitor. iNOs-IN-1 can significantly inhibit the expression of IL-6 and iNOS, as well as reduce LPS-induced NO generation with dose-dependent manner in mouse macrophages. Anti-inflammatory effects .
|
-
- HY-126910
-
|
|
Opioid Receptor
|
Metabolic Disease
|
|
Mesyl Salvinorin B is a potent and selective kappa opioid receptor (KOP-r) agonist. Mesyl Salvinorin B prevents the ADE (Alcohol deprivation effect) in mice. Mesyl Salvinorin B dose-dependently reduces alcohol intake and preference in CED (chronic escalation drinking) mice .
|
-
- HY-156466
-
|
|
JAK
|
Inflammation/Immunology
|
|
QL-1200186 is anorally activeand selective inhibitor ofTYK2. Oral administration of QL-1200186, dose-dependently inhibitsinterferon-γ(IFNγ) production afterinterleukin-12(IL-12) challenge and significantly ameliorates skin lesions in psoriatic mice .
|
-
- HY-157508
-
|
|
p97
|
Others
|
|
VCP Activator 1 is a VCP activator that dose-dependently stimulates VCP ATPase activity. VCP Activator 1 binds an allosteric pocket near the C-terminus. In addition, VCP Activator 1 binding site can also be occupied by a phenylalanine residue in the VCP C-terminal tail .
|
-
- HY-N5054
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
(R)-5,7-Dimethoxyflavanone shows potent antimutagenic activity against MeIQ mutagenesis in Ames test using the S. typhimurium TA100 and TA98 strains . And (R)-5,7-Dimethoxyflavanone significantly and dose-dependently inhibits the inflammatory mediato .
|
-
- HY-146433
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 55 is a potent anticancer agent. Anticancer agent 55 shows anticancer activity via reducing the cell viability and cell migration in a dose-dependent manner. Anticancer agent 55 induces apoptosis. Anticancer agent 55 has the potential for the research of prostate cancer and breast cancer .
|
-
- HY-157029S
-
|
|
Ras
|
Cancer
|
|
KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
- HY-157031S
-
|
|
Ras
|
Cancer
|
|
KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
- HY-113820
-
|
|
PPAR
|
Metabolic Disease
|
|
AZD4619 is an orally active, selective peroxisome proliferator-activated receptor α (PPARα) agonist. AZD4619 increases alanine aminotransferase 1 (ALT1) protein expression in a dose-dependent manner in human, but not in rat primary hepatocytes. AZD4619 is a lipid-lowering drug .
|
-
- HY-114766
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Pumafentrine is an orally active, potent dual PDE3/PDE4 inhibitor. Pumafentrine dose-dependently ameliorates the clinical score and colonic TNFα production in murine Dextran sulphate sodium (DSS; HY-116282C)-induced colitis in a preventive setting .
|
-
- HY-B0094
-
|
Qinghaosu; NSC 369397
|
HCV
Parasite
Akt
Ferroptosis
|
Infection
Neurological Disease
Cancer
|
|
Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .
|
-
- HY-B0162A
-
|
|
HCN Channel
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Ivabradine hydrochloride is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine hydrochloride reduces dose-dependently heart rate without modification of blood pressure. Ivabradine hydrochloride shows anticonvulsant, anti-ischaemic and anti-anginal activity .
|
-
- 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-144127
-
|
|
Androgen Receptor
|
Cancer
|
|
AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally .
|
-
- HY-146260
-
|
|
PI3K
|
Cancer
|
|
NVP-CLR457 (compound 40) is an orally active, potent and balanced pan-class I PI3K inhibitor. NVP-CLR457 shows a clear dose-dependent PK/PD/efficacy relationship. NVP-CLR457 has antitumor activity .
|
-
- HY-B0162
-
|
|
HCN Channel
|
Cardiovascular Disease
Cancer
|
|
Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity .
|
-
- HY-151926
-
|
|
Enterovirus
|
Infection
|
|
Antiviral agent 24 is a potent antiviral agent with EC50 values of 0.101, 19.9, 91.2 µM for EV71, CVA21, EV68, respectively. Antiviral agent 24 inhibits METTL3/METTL14 activity in a dose-dependent manner .
|
-
- HY-156500
-
|
|
ICMT
|
Cancer
|
|
ICMT-IN-1 (compound 75) is an inhibitor of ICMT (IC50=0.0013 μM). ICMT-IN-1 dose-dependently induces ICMT accumulation in the cytoplasm of HCT-116 cells and inhibits the proliferation of multiple cancer cell lines expressing K-Ras and N-Ras .
|
-
- HY-149705
-
|
|
ICMT
|
Cancer
|
|
ICMT-IN-7 (compound 74) is an inhibitor of ICMT (IC50=0.015 μM). ICMT-IN-7 dose-dependently induces ICMT accumulation in the cytoplasm of HCT-116 cells and inhibits the proliferation of multiple cancer cell lines expressing K-Ras and N-Ras .
|
-
- HY-111143
-
|
|
nAChR
|
Metabolic Disease
|
|
SCH-900271 is an orally active, potent nicotinic acid receptor (NAR) agonist with an EC50 of 2 nM in the hu-GPR109a assay. SCH-900271 exhibits dose-dependent inhibition of plasma free fatty acid (FFA). SCH-900271 has an improved therapeutic window to flushing .
|
-
- HY-163172
-
|
|
Others
|
Neurological Disease
|
|
Miro1 Reducer is a small molecule that can repair this defect of Miro1 in Parkinson's disease (PD) fibroblasts. Miro1 Reducer reduces the delayed mitophagy phenotype in PD fibroblasts. Miro1 Reducer reduces Miro1 protein levels in dose-dependent manner (IC50 = 7.8 mM) .
|
-
- HY-P10517
-
|
SFT
|
HIV
|
Infection
|
|
Sifuvirtide (SFT) is a potent HIV fusion inhibitor. Sifuvirtide inhibits HIV-1 mediated cell fusion in a dose-dependent manner and is highly potent against infection by primary and laboratory-adapted HIV-1 isolates of multiple genotypes. Sifuvirtide can be used in the research of anti-HIV drugs .
|
-
- HY-N5060R
-
|
|
Parasite
|
Neurological Disease
|
|
Estragole (Standard) is the analytical standard of Estragole. This product is intended for research and analytical applications. Estragole (4-Allylanisole), a relatively nontoxic volatile terpenoid ether, is a major component of the essential oil of many plants. Estragole dose-dependently blocks nerve excitability . Estragole displays anti-toxoplasma activity .
|
-
- HY-169941
-
|
|
Estrogen Receptor/ERR
|
Metabolic Disease
Cancer
|
|
ERα/ERβ antagonist-1 (Compound 10) is partial antagonists of ERα and ERβ. ERα/ERβ antagonist-1 reduces ERα and ERβ activity in a dose-dependent manner in HepG2 liver cells .
|
-
- HY-N0262
-
-
- HY-P2080
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
GIP (1-30) amide,human is a glucose-dependent insulinotropic polypeptide (GIP) fragment. GIP is an incretin hormone that stimulates insulin secretion and reduces postprandial glycaemic excursions. GIP (1-30) amide,human dose-dependently promotes insulin secretion over the range 10 -9-10 -6 M .
|
-
- 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-P2080B
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
GIP (1-30) amide,human acetate is a glucose-dependent insulinotropic polypeptide (GIP) fragment. GIP is an incretin hormone that stimulates insulin secretion and reduces postprandial glycaemic excursions. GIP (1-30) amide,human acetate dose-dependently promotes insulin secretion over the range 10 -9-10 -6 M .
|
-
- HY-P1440A
-
|
|
Potassium Channel
|
Neurological Disease
|
|
BeKm-1 TFA is a potent and selective KV11.1 (hERG) channel blocker. BeKm-1 TFA is selective for KV11.1 over a panel of 14 other potassium channels. BeKm-1 TFA dose-dependently prolongs QTc interval in isolated rabbit heart.
|
-
- HY-146782
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-49 is a potent and selective EGFR inhibitor with IC50s of 65.0 nM and 13.6 nM for EGFR T790M and EGFR T790M/L858R, respectively. EGFR-IN-49 induces late apoptosis in a dose-dependent manner .
|
-
- HY-N7934
-
|
(-)-Trachelogenin
|
HCV
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Trachelogenin ((-)-Trachelogenin) is an HCV entry inhibitor without genotype specificity, and with low cytotoxicity. Trachelogenin inhibits HCVcc infection and HCVpp cell entry in a dose-dependent manner with an IC50 of 0.325 and 0.259 μg/mL in HCVcc and HCVpp models, respectively. Trachelogenin exhibits effective antiviral, anti-inflammatory and analgesic effects .
|
-
- HY-152535
-
|
|
HSV
|
Infection
Inflammation/Immunology
|
|
ATV041 is an orally active Ibuprofen (HY-78131) and nucleotide analogue. ATV041 improves oral pharmacokinetic (PK) profile and tissue distribution with anti-mouse hepatitis virus (MHV) activity. ATV041 reduces viral load, tissue damage and virus-induced inflammation in a dose-dependent manner .
|
-
- HY-154995
-
|
|
Glycosidase
|
Infection
|
|
N-4′-(p-Trifluoromethylphenyl)butyl-DAB (compound 5g) is an agonit of lysosomal acid α-glucosidase (GAA). N-4′-(p-Trifluoromethylphenyl)butyl-DAB increases intracellular GAA activities dose-dependently, in Pompe patient's fibroblasts with the M519V mutation .
|
-
- HY-124022
-
|
|
HDAC
|
Others
|
|
APHA Compound 8 (Compound 4) is a histone deacetylase (HDAC) inhibitor. APHA Compound 8 has antimouse HDAC1 activity with an IC50 value of 0.78 μM. APHA Compound 8, as antiproliferative and cytodifferentiating agent on MEL cells, shows dose-dependent growth inhibition and hemoglobin accumulation effects .
|
-
- 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-P1235
-
|
Atrial Natriuretic Peptide (ANP) (1-28), human, porcine
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Carperitide (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine) is a 28-amino acid hormone, that is normally produced and secreted by the human heart in response to cardiac injury and mechanical stretch. Carperitide (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine) inhibits endothelin-1 secretion in a dose-dependent way.
|
-
- HY-121356S1
-
|
|
Isotope-Labeled Compounds
Histamine Receptor
|
Endocrinology
Cancer
|
|
Carebastine-d5 Methyl Ester is the deuterium labeled Carebastine. Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner[1]. Carebastine suppresses the expression of macrophage migration inhibitory factor[2].
|
-
- HY-121356S
-
|
|
Isotope-Labeled Compounds
Histamine Receptor
|
Endocrinology
Cancer
|
|
Carebastine-d5 is the deuterium labeled Carebastine. Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner[1]. Carebastine suppresses the expression of macrophage migration inhibitory factor[2].
|
-
- HY-N6745
-
|
|
Na+/K+ ATPase
Apoptosis
|
Infection
Cardiovascular Disease
|
|
Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na +/K +-ATPase whereas in microsomes, both Na +/K +-ATPase and Mg 2+-ATPase activities are significantly stimulated in a dose-dependent manner . Citreoviridin inhibits cell proliferation and enhances apoptosis of human umbilical vein endothelial cells .
|
-
- HY-101119
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
GLL398 is a potent, orally bioavailable selective estrogen receptor degrader (SERD) with an IC50 value of 1.14 nM. GLL398 shows a strong dose-dependent binding to ER with a mutation at Y537S (IC50=29.5 nM). GLL398 blocks tumor growth in xenograft models of breast cancer.
|
-
- HY-102051
-
|
|
IAP
|
Cancer
|
|
XIAP/cIAP1 antagonist-1 is a potent and orally active XIAP/cIAP1 antagonist with EC50s of 5.1 nM and 0.32 nM for XIAP and cIAP1, respectively. XIAP/cIAP1 antagonist-1 inhibits the tumor growth in dose-dependent manner in vivo .
|
-
- HY-138054
-
|
|
MDM-2/p53
|
Cancer
|
|
Cjoc42 is a compound capable of binding to gankyrin. Cjoc42 inhibits gankyrin activity in a dose-dependent manner. Cjoc42 prevents the decrease in p53 protein levels normally associated with high amounts of gankyrin. Cjoc42 restores p53-dependent transcription and sensitivity to DNA damage .
|
-
- HY-107551
-
|
|
Gli
|
Cancer
|
|
GLI antagonist-1 is a potent GLI antagonist with an IC50 value of 1.1 µM. GLI antagonist-1 shows anti-proliferative activity. GLI antagonist-1 decreases the GLI1 mRNA expression. GLI antagonist-1 inhibits colony formation in a dose-dependent manner .
|
-
- HY-120727
-
|
|
mGluR
|
Neurological Disease
|
|
VU0364289 is a highly selective mGlu5 positive allosteric modulator (PAM) (binds to the MPEP (HY-14609A) site), with an EC50 of 1.6 µM. VU0364289 can reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, which can be used for schizophrenia and other psychiatric research .
|
-
- HY-138939
-
|
|
Lipoxygenase
|
Cancer
|
|
5-LOX-IN-2, an inhibitor of 5-lipoxygenase (5-LOX) with an IC50 of 0.33 μM, inhibits 5-LOX in a dose-dependent manner . 5-LOX-IN-2, reduces the cell viability of renal cancer cells and induces apoptosis, can be used for cancer research .
|
-
- HY-162001
-
INX-315
1 Publications Verification
|
CDK
|
Cancer
|
|
INX-315 is an orally active and selective CDK2 inhibitor that induces cell cycle arrest in the G1 phase. INX-315 reduces CDK2 substrate phosphorylation and inhibits tumor growth in a dose-dependent manner in xenograft mouse models. INX-315 may be used in cancer research .
|
-
- HY-163106
-
|
|
Ceramidase
|
Cancer
|
|
W000113414_I13 is an acid ceramidase (AC) inhibitor. W000113414_I13 exhibits dose-dependent inhibition of AC with an IC50 value of 6.6?μM. W000113414_I13 can be used for the research of cancer .
|
-
- HY-116431
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
I-BOP is an agonist for thromboxane A2 receptor (TP) with a KD of 0.61 nM. I-BOP promotes proliferation through activation of PI3K pathway in vascular smooth muscle . I-BOP dose-dependently biphasicly affects the excitatory postsynaptic potential (e.p.s.p.) in hippocampal neurons .
|
-
- HY-P10571
-
|
|
Melanocortin Receptor
|
Endocrinology
|
|
GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC50=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R .
|
-
- HY-108716
-
|
CBS9106; SL-801
|
CRM1
Apoptosis
|
Cancer
|
|
CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities. CBS9106, inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells .
|
-
- HY-19517
-
|
|
Others
|
Cardiovascular Disease
|
|
R1663 is a factor Xa inhibitor with anticoagulant activity. R1663 does not affect bleeding time. The pharmacodynamic effects (such as inhibition of thrombin generation) and plasma concentrations of R1663 are dose-dependent. R1663 prolongs clotting time in a concentration-dependent manner and inhibits the peak height of thrombin generation and endogenous thrombin potential .
|
-
- HY-167886
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
GA 0113 is a potent and orally active angiotensin II (Ang II) AT1-receptor antagonist. GA 0113 inhibits the Ang II (HY-13948)-induced pressor response with ID50 of 0.032 mg/kg and dose-dependently increases plasma renin activity for 48 h .
|
-
- HY-N0092R
-
|
|
Adenosine Receptor
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
|
Inosine (Standard) is the analytical standard of Inosine. This product is intended for research and analytical applications. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors . In Vitro:Inosine dose-dependently stimulates cAMP production mediated through the A2AR .
Inosine dose-dependently induces hA2AR-mediated ERK1/2 phosphorylation .
Inosine (100 μM; 24 hours) reduces oxidative stress in MES 23.5 cells cultured with astrocytes .
In Vivo:Inosine (10-100 mg/kg; i.p.) exhibits antinociceptive effect in mice .
|
-
- HY-B0006
-
-
- HY-115579
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
MALAT1-IN-1 (compounds 5) is a potent and specific Malat1 (Metastasis-associated lung adenocarcinoma transcript 1) inhibitor. MALAT1-IN-1 modulated Malat1 downstream genes in a dose-dependent manner without affecting expression of nuclear enriched abundant transcript 1 (Neat1) .
|
-
- HY-103461
-
|
|
FAAH
|
Neurological Disease
|
|
FAAH-IN-6 (compound 21d) is a potent, orally active and cross the blood-brain barrier fatty acid amide hydrolase (FAAH) inhibitor with IC50s of 0.72, 0.28 nM for hFAAH, rFAAH, respectively. FAAH-IN-6 shows dose-dependent analgesic efficacy in animal models of both neuropathic and inflammatory pain .
|
-
- HY-N3734
-
|
|
Beta-secretase
Phosphatase
|
Neurological Disease
|
|
Deoxyneocryptotanshinone, a natural tanshinone, is a high affinity BACE1 (Beta-secretase) inhibitor with an IC50 value of 11.53 μM. Deoxyneocryptotanshinone shows a promising dose-dependent inhibition of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 133.5 μM. Deoxyneocryptotanshinone can be used for Alzheimer's disease research .
|
-
- HY-152035
-
|
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Mycobacterial Zmp1-IN-1 is a mycobacterial zinc metalloprotease-1 (Zmp1) inhibitor. Mycobacterial Zmp1-IN-1 has anti-mycobacterial activity for Mtb H37Ra in dose-dependent inhibition. Mycobacterial Zmp1-IN-1 can be used for the research of tuberculosis (TB) .
|
-
- HY-142088
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Beauverolide Ka, a cyclotetradepsipeptide, is a metabolite of Beauveria bassiana fungus. Beauverolide Ka stimulates glucose uptake in cultured rat L6 myoblasts at 50 μM. Beauverolide Ka exhibits protecting effects on HEI-OC1 cells at 10 μM and shows dose-dependent activity in both L6 myoblasts and myotubes .
|
-
- HY-P2080C
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
GIP (1-30)-Myr is the Myr-modified GIP (1-30), which is a glucose-dependent insulinotropic polypeptide (GIP) fragment. GIP is an incretin hormone that stimulates insulin secretion and reduces postprandial glycaemic excursions. GIP (1-30) dose-dependently promotes insulin secretion over the range 10 -9-10 -6 M .
|
-
- HY-130345
-
|
|
Platelet-activating Factor Receptor (PAFR)
|
Cardiovascular Disease
|
|
C18-PAF, octadecane PAF, is the ligand of platelet-activating factor and PAF G protein-coupled receptor (PAFR). C18-PAF has renovasodilator properties and antihypertensive lipid properties. C18-PAF increases renal blood flow and causes dose-dependent systemic hypotension .
|
-
- HY-125396
-
|
11-Deoxy-PGF2β
|
Endogenous Metabolite
|
Others
|
|
11-Deoxyprostaglandin F2β (11-deoxy PGF2β) is an analog of PGF2β (HY-12956B). PGF2β is a metabolite produced by cyclooxygenase metabolism of arachidonic acid. PGF2β induces dose-dependent release of hexose containing mucin .
|
-
- HY-W013576S
-
|
|
Isotope-Labeled Compounds
|
Cancer
|
|
Methyl 2-Octynoate-d5 is deuterated labeled Estragole (HY-N5060). Estragole (4-Allylanisole), a relatively nontoxic volatile terpenoid ether, is a major component of the essential oil of many plants. Estragole dose-dependently blocks nerve excitability . Estragole displays anti-toxoplasma activity .
|
-
- HY-14923
-
|
AVE 7688
|
Angiotensin-converting Enzyme (ACE)
|
Metabolic Disease
|
|
Ilepatril, a dual inhibitor of angiotensin-converting enzyme (ACE) and neutral endopeptidase, has inhibitory effects in the type 2 diabetic nephropathy model in obese Zucker diabetic fatty (ZDF) rats. Ilepatril significantly reduced albuminuria in a dose-dependent manner and may be a strategy distinct from metabolic control to inhibit type 2 diabetic nephropathy .
|
-
- HY-N13202
-
|
|
Others
|
Inflammation/Immunology
|
|
Black Currant Extract is a black currant extract, and its components include: Anthocyanidins. Black Currant Extract is an anti-inflammatory agent that can neutralize the cytotoxic effects of nicotine on epithelial cells and fibroblasts in a dose-dependent manner. Black Currant Extract can also inhibit LPS-induced IL-6 secretion by human macrophages. .
|
-
- HY-N12481
-
|
|
Others
|
Inflammation/Immunology
|
|
Cephalandole B is an indigo alkaloid that has the activity of inhibiting IL-17A gene expression. Cephalandole B significantly inhibited the activity of IL-17A luciferase reporter gene in Jukat cells, and this inhibitory effect was dose-dependent. Cephalandole B may have important application prospects in inflammation-related research .
|
-
- HY-108630
-
U-73343
4 Publications Verification
|
Phospholipase
|
Others
|
|
U-73343, works as a protonophore, is an inactive analog of U-73122 and can be used as a negative control. U-73343 dose-dependently inhibits acid secretion irrespective of the stimulant. U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC50 of 1-2.1 μM for PLC .
|
-
- HY-135899
-
|
|
Sirtuin
Apoptosis
|
Cancer
|
|
SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway. .
|
-
- HY-B2145
-
|
IY-81149 sodium
|
Proton Pump
TOPK
|
Inflammation/Immunology
Cancer
|
|
Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
|
-
- HY-122678
-
|
|
Survivin
Apoptosis
|
Cancer
|
|
LQZ-7F, a survivin dimerization inhibitor, induces spontaneous apoptosis and synergizes with Docetaxel in prostate cancer cells. LQZ-7F dose-dependently inhibits survival of both PC-3 and C4-2 cells with IC50s of 2.99 and 2.47 µM, respectively .
|
-
- HY-122112
-
|
|
Sigma Receptor
|
Cancer
|
|
CM572 is a selective irreversible partial sigma-2 receptor agonist. CM572 has antitumor activity. CM572 induces dose-dependent cell death, with an EC50 of 7.6 μM in SK-N-SH neuroblastoma cells. CM572 can be used for the research of kinds of diseases such as neuroblastoma, breast cancer .
|
-
- HY-B2145A
-
|
IY-81149 sodium hydrate
|
Proton Pump
TOPK
|
Inflammation/Immunology
Cancer
|
|
Ilaprazole (IY-81149) sodium hydrate is an orally active proton pump inhibitor. Ilaprazole sodium hydrate irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium hydrate is used for the research of gastric ulcers. Ilaprazole sodium hydrate is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
|
-
- HY-161740
-
|
|
AUTOTACs
Estrogen Receptor/ERR
Autophagy
|
Cancer
|
|
PHTPP-1304 is a PHTPP-based autophagy targeting chimera (AUTOTAC) that induces p62 self-oligomerization and degradation of estrogen receptor ERβ (DC50:~2 nM, HEK293T). PHTPP-1304 also induces the formation of p62 +ERβ + puncta that are affected by autophagic flux in a dose-dependent manner .
|
-
- HY-117952
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
L 743310 is a non-peptide, selective antagonist of the human neurokinin hNK1 receptor, with high affinity for primate and cloned human hNK1 receptors and lower affinity for rodent NK1 receptors. L 743310 inhibits resiniferatoxin-induced plasma protein extravasation in guinea pig esophagus. L 743310 has a dose-dependent inhibitory effect on cisplatin-induced emesis .
|
-
- HY-100724
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
YM-17690 is a LTD4 and LTE4 agonist, with a pKi value of 9.28 for [3H]LTD4. It induces dose-dependent contractions in guinea pig ileum, lung parenchyma, and trachea, with EC50 values of 16, 3.9, and 22 nM, respectively. YM-17690 can be used in research related to asthma and inflammation .
|
-
- HY-162882
-
|
|
Xanthine Oxidase
Reactive Oxygen Species
|
Metabolic Disease
|
CC15009 is a xanthine oxidoreductase (XOR) inhibitor, with an IC50 value of 0.237 nM. CC15009 can inhibit the oxidative subtype of XOR, thereby reducing the production of the byproduct ROS and exhibiting antioxidant activity. CC15009 has demonstrated a good dose-dependent uric acid-lowering effect in two different mouse models of hyperuricemia induced by XOR substrates .
|
-
- HY-124185
-
|
|
Others
|
Others
|
|
LC 6 is an anti-allergic compound that has the activity of inhibiting passive cutaneous allergic reactions in rats. Its half effective dose (ED50) is 35 mg/kg body weight. Oral administration is effective and long-lasting, and the effect is obviously dose-dependent. Its long-term binding to mast cells makes it a valuable tool for studying allergic reaction receptors.
|
-
- HY-168614
-
|
|
IKZF Family
|
Cancer
|
|
MGD-4 is an orally active, Cereblon (CRBN)-dependent IKAROS protein degrader that degrades IKZF1 (DC50=67.2 nM), IKZF2 (DC50=918.2 nM), and IKZF3 (DC50=95.8 nM) in a dose-dependent manner. MGD-4 effectively inhibits the growth of multiple myeloma .
|
-
- HY-W008820R
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Glutaric acid (Standard) is the analytical standard of Glutaric acid. This product is intended for research and analytical applications. Glutaric acid, C5 dicarboxylic acid, is an intermediate during the catabolic pathways of lysine and tryptophan. Glutaric acid affects pericyte contractility and migration. Glutaric acid is an indicator of glutaric aciduria type I .
In Vitro: Glutaric acid (GA) at concentrations of 1 and 2 mM is able to reduce TRAP measurement by up to 28% in a dose-dependent manner (β=0.77; P<0.001). Furthermore, a significantly inverse correlation is also verified between chemiluminescence and TRAP (β=0.81; P<0.001). Glutaric acid does not alter the activities of Cat and SOD, but strongly inhibits (up to 46%) the activity of GPx even at the lower concentration used (0.5 mM). It is observed that the metabolite inhibits this activity in a dose-dependent manner at concentrations as low as 0.05 mM .
|
-
- HY-10974
-
|
|
γ-secretase
|
Neurological Disease
Cancer
|
|
MK-0752 is a potent, orally active and specific γ-secretase inhibitor, showing dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. MK-0752 crosses the blood-brain barrier. MK-0752 reduces newly generated CNS Aβ in vivo .
|
-
- HY-11062
-
Icilin
1 Publications Verification
AG-3-5
|
TRP Channel
|
Neurological Disease
Inflammation/Immunology
|
|
Icilin (AG-3-5) is a super-agonist of the transient receptor potential M8 (TRPM8) ion channel. Icilin activates TRPM8 in EGTA in a dose-dependent manner (EC50=1.4 μM). Icilin is a "super-cooling agent" . Icilin attenuates autoimmune neuroinflammation through modulation of the T-cell response .
|
-
- HY-18056
-
|
|
Others
|
Metabolic Disease
|
|
PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively .
|
-
- HY-12953
-
-
- HY-B0094S
-
|
Qinghaosu-d3; NSC 369397-d3
|
Akt
Ferroptosis
HCV
Parasite
|
Infection
Neurological Disease
Cancer
|
|
Artemisinin-d3 is the deuterium labeled Artemisinin. Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants[1]. Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects[2].
|
-
- HY-N2252
-
-
- HY-131334
-
|
|
AMPK
|
Metabolic Disease
|
|
AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect .
|
-
- HY-145153
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
S-777469 is a selective and orally available cannabinoid type 2 receptor (CB2) agonist with a Ki of 36 nM. S-777469 significantly suppresses compound 48/80-induced scratching behavior in mice in a dose-dependent manner. S-777469 produces its antipruritic effects by inhibiting itch signal transmission through CB2 agonism .
|
-
- HY-144657
-
|
|
PROTACs
Ras
|
Cancer
|
|
(4S)-PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 significantly inhibits the tumor growth in vivo .
|
-
- HY-144797
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 22 (compound 4c) is a potent inhibitor of tubulin with anti-angiogenesis and anti-cancer properties. Tubulin inhibitor 22 arrests MGC-803 cell cycle at G2/M phase. Tubulin inhibitor 22 dose-dependently causes Caspase-induced apoptosis of MGC-803 cells through mitochondrial dysfunction .
|
-
- HY-146203
-
|
|
FAK
|
Cancer
|
|
Compound 26F not only optimized the effective inhibitory enzyme (ic50= 28.2 nm), but also showed relatively less cytotoxicity (ic50= 3.32 μ M) And induced MDA-MB-231 cell apoptosis in a dose-dependent manner, effectively blocking MDA-MB-231 cells in g0/g1 phase.
|
-
- HY-101960A
-
|
AG-183
|
EGFR
|
Cancer
|
|
Tyrphostin A51 is a potent protein tyrosine kinase (PTK) inhibitor. Tyrphostin A51 inhibits the volume-dependent release of [ 3H]taurine in a dose-dependent manner. Tyrphostin A51 markedly reduces cellular tyrosyl phosphorylation level. Tyrphostin A51 inhibits both basal and EGF-induced human bone cell proliferation .
|
-
- HY-123714
-
|
|
MAP4K
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
TL4-12 is a selective MAP4K2/GCK inhibitor, dose-dependently downregulates IKZF1 and BCL-6 and leads to MM cell proliferation inhibition (IC50=37 nM) accompanied by induction of apoptosis. TL4-12 can be used to overcome immunomodulatory agent resistance in multiple myeloma (MM) .
|
-
- HY-139451
-
|
|
Others
|
Neurological Disease
|
|
ELOVL6-IN-1 is a potent, orally active and selective ELOVL6 inhibitor. ELOVL6-IN-1 dose-dependently inhibits mouse ELOVL6 activities, with an IC50 value of 0.350 μM. ELOVL6-IN-1 inhibits ELOVL6 in a noncompetitive manner for malonyl-CoA (Ki=994 nM) and palmitoyl-CoA .
|
-
- HY-107037
-
|
RX71107
|
Vasopressin Receptor
Angiotensin Receptor
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Tolmesoxide (RX71107) is a peripheral vascular dilator with blood pressure lowering activity. Tolmesoxide has shown direct vasodilation in the human forearm arterial bed and dorsal hand vein. Tolmesoxide can dose-dependently increase blood flow in the forearm and produce dilation during contraction of the dorsal hand veins. Tolmesoxide can be used to study high blood pressure and angina .
|
-
- HY-118765
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
Ro 23-3423 is a thromboxane synthase inhibitor with an IC50 value of 0.33 μM for human platelet microsomal thromboxane synthase. Ro 23-3423 increases plasma levels of PGF and PGE2 in a dose-dependent manner, accompanied by a decrease in mean systemic arterial pressure and systemic vascular resistance. Ro 23-3423 can be used in the study of general anesthesia .
|
-
- HY-10975
-
|
|
γ-secretase
|
Neurological Disease
Cancer
|
|
MK-0752 sodium is a potent, orally active and specific γ-secretase inhibitor, showing dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. MK-0752 sodium crosses the blood-brain barrier. MK-0752 sodium reduces newly generated CNS Aβ in vivo .
|
-
- HY-167924
-
|
|
Kallikrein
Thrombin
Ser/Thr Protease
|
Inflammation/Immunology
|
|
Ono 3307 Free base is a novel synthetic protease inhibitor that exhibits protective effects against acute pancreatitis by preventing hyperamylasemia and pancreatic edema. Ono 3307 Free base also inhibits the redistribution of lysosomal enzymes in acinar cells and mitigates lactic dehydrogenase discharge. Ono 3307 Free base effectively reduces cathepsin B leakage from lysosomes in a dose-dependent manner.
|
-
- HY-167846
-
|
|
JAK
|
Cancer
|
|
YLIU-4-105-1 is a Type II JAK2 inhibitor. YLIU-4-105-1 binds to the ATP-binding pocket of JH1. YLIU-4-105-1 has in vivo pharmacodynamic activity as evidenced by inhibiting pSTAT5, reducing spleen to body weight, and lowering blood reticulocyte counts in a dose-dependent manner .
|
-
- HY-P10710
-
|
|
IFNAR
Interleukin Related
COX
|
Inflammation/Immunology
|
|
BMP-4 is a penetrating heparin-binding peptide with anti-inflammatory and anti-chondrogenic functions. In murine chondrocytes and macrophages, BMP-4 regulates the iNOS-IFN-IL6 signaling pathway to inhibit the expression of inflammatory proteins such as iNOS, COX2, IFN, and IL6 in a dose-dependent manner, effectively suppressing inflammation and alleviating various arthritis symptoms .
|
-
- HY-B1246
-
|
|
Bacterial
Proton Pump
|
Infection
|
|
Thonzonium bromide is an antibacterial agent that is structurally similar to Farnesol (HY-Y0248A). Thonzonium bromide is also a monocationic surface-active agent, which inhibits RANKL-induced osteoclast formation and bone resorption in vitro and prevents LPS-induced bone loss in vivo. Thonzonium bromide inhibits proton transport in a dose-dependent manner (EC50=69 μM) .
|
-
- HY-101664
-
|
IY-81149
|
Proton Pump
TOPK
|
Inflammation/Immunology
Cancer
|
|
Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
|
-
- HY-12995A
-
|
|
FLAP
|
Inflammation/Immunology
|
|
(S)-BI 665915 is an orally active oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.7 nM for FLAP binding. (S)-BI 665915 inhibits FLAP functional in human whole blood with an IC50 of 45 nM. (S)-BI 665915 demonstrates an excellent cross-species agent metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition of LTB4 production .
|
-
- HY-B0162S
-
|
|
HCN Channel
|
Cardiovascular Disease
|
|
Ivabradine-d6 is the deuterium labeled Ivabradine[1]. Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity[2][3][4][5].
|
-
- HY-155417
-
|
|
Others
|
Neurological Disease
|
|
GPR34 receptor antagonist 3 (Compound 5e) is a class of GRP34 antagonists, IC50 is 0.680 μM. GPR34 receptor antagonist 3 inhibited ERK1/2 phosphorylation induced by lysophosphatidylserine in a dose-dependent way without obvious cytotoxicity. GPR34 receptor antagonist 3 shows antisensory activity in mouse neuropathic pain model .
|
-
- HY-P10228
-
|
|
Fungal
Bacterial
|
Infection
|
|
S-Thanatin is an insect antimicrobial peptide with potent broad-spectrum antibacterial activity. S-Thanatin can inhibit the activity of Gram-negative bacteria, Gram-positive bacteria, and fungi, without cytotoxicity. The antibacterial activity of S-Thanatin is not affected by PH value, but monovalent cations (Na +/K +) can reduce its antibacterial activity against Gram-negative bacteria in a dose-dependent manner .
|
-
- 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-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-B0162AR
-
|
|
HCN Channel
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Ivabradine (hydrochloride) (Standard) is the analytical standard of Ivabradine (hydrochloride). This product is intended for research and analytical applications. Ivabradine hydrochloride is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine hydrochloride reduces dose-dependently heart rate without modification of blood pressure. Ivabradine hydrochloride shows anticonvulsant, anti-ischaemic and anti-anginal activity .
|
-
- HY-B0094R
-
|
|
HCV
Parasite
Akt
Ferroptosis
|
Infection
Neurological Disease
Cancer
|
|
Artemisinin (Standard) is the analytical standard of Artemisinin. This product is intended for research and analytical applications. Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .
|
-
- HY-N0262R
-
|
|
TNF Receptor
MMP
Bacterial
Autophagy
Antibiotic
|
Infection
Inflammation/Immunology
Cancer
|
|
Cordycepin (Standard) is the analytical standard of Cordycepin. This product is intended for research and analytical applications. Cordycepin (3'-Deoxyadenosine) is a nucleoside derivative and inhibits IL-1β-induced MMP-1 and MMP-3 expression in rheumatoid arthritis synovial fibroblasts (RASFs) in a dose-dependent manner . Cordycepin kills Mycobacterium tuberculosis through hijacking the bacterial adenosine kinase .
|
-
- HY-129668
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
Bremazocine is a potent opioid kappa receptor agonist with analgesic activity. Bremazocine induces peripheral analgesia by releasing endogenous norepinephrine. The analgesic effect of bremazocine is associated with interaction with adenosine receptors. Bremazocine produces a dose-dependent peripheral analgesia after topical application. The effect of bremazocine is affected by nonselective α(2) adrenaline receptor antagonists, suggesting that it acts through a norepinephrine pathway .
|
-
- HY-N3504
-
|
|
Sirtuin
|
Cancer
|
|
Ophiopogonin D', isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D' shows cytotoxic activity against two human tumor cell lines MG-63 and SNU387 with IC50s of 3.09 μM and 3.63 μM, respectively . Ophiopogonin D' activates SIRT1 in a dose-dependent manner .
|
-
- HY-110100
-
CPYPP
2 Publications Verification
|
DOCK
|
Inflammation/Immunology
|
|
CPYPP is a DOCK2-Rac1 interaction inhibitor. CPYPP binds to DOCK2 DHR-2 domain and inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2 DHR-2 for Rac1 in a dose-dependent manner with an IC50 of 22.8 μM. CPYPP also inhibits DOCK180 and DOCK5 and less inhibits DOCK9 .
|
-
- HY-113439
-
12-HETE
1 Publications Verification
|
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
|
|
12-HETE, a major metabolic product of arachidonic acid using 12-LOX catalysis, inhibits cell apoptosis in a dose-dependent manner. 12-HETE promotes the activation and nuclear translocation of NF-κB through the integrin-linked kinase (ILK) pathway .12-HETE has both anti-thrombotic and pro-thrombotic effects . 12-HETE is a neuromodulator .
|
-
- HY-143653
-
|
|
BCL6
|
Cancer
|
|
BCL6-IN-6 is a potent inhibitor of transcriptional repressor B-cell lymphoma 6 (BCL6). BCL6-IN-6 significantly blocks the interaction of BCL6 with its corepressors and reactivates BCL6 target genes in a dose-dependent manner. BCL6-IN-6 has the potential for the research of diffuse large B-cell lymphoma (DLBCL) .
|
-
- HY-144657A
-
|
|
PROTACs
Ras
|
Cancer
|
|
(4S)-PROTAC SOS1 degrader-1 (diTFA) is a potent PROTAC SOS1 degrader. (4S)-PROTAC SOS1 degrader-1 (diTFA) decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. (4S)-PROTAC SOS1 degrader-1 (diTFA) significantly inhibits the tumor growth in vivo .
|
-
- HY-160853
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 42 (Compound 14b) dose-dependently inhibited the activity of β-microtubulin (IC50 = 3.5 µM).Tubulin inhibitor 42 interferes with microtubule dynamic homeostasis, resulting in the arrest of the cancer cell cycle in the G2/M phase and inducing apoptosis. Tubulin inhibitor 42 significantly inhibits the angiogenic process in vitro and in vivo, preventing vascularization and tumor growth .
|
-
- HY-113763
-
|
|
Others
|
Others
|
|
TWEAK-Fn14-IN-1 (Compound L524-0366) is a specific dose-dependent TWEAK-Fn14 inhibitor. TWEAK-Fn14-IN-1 binds specifically to the Fn14 surface with a KD of 7.12 μM. TWEAK-Fn14-IN-1 inhibits TWEAK induced glioma cell migration without any potential cytotoxic effects .
|
-
- HY-117251
-
|
|
|
Neurological Disease
|
|
LP-403812 is a high affinity proline transporter (PROT) inhibitor that produces dose-dependent inhibition of hPROT (IC50=0.11 μM; Ki=0.12 μM) and also inhibits the activity of mouse brain synaptosomal mPROT with the same potency (IC50=0.23 μM). LP-403812 can be used to study the function of PROT in the brain .
|
-
- 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-10119AR
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar (sulfate) (Standard) is the analytical standard of Vorapaxar (sulfate). This product is intended for research and analytical applications. 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-101906
-
|
|
Free Fatty Acid Receptor
Apoptosis
|
Metabolic Disease
|
|
DC260126 is a potent antagonist of GPR40 (FFAR1). DC260126 dose-dependently inhibits GPR40-mediated Ca 2+ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC50: 6.28, 5.96, 7.07, 4.58 μM, respectively) . DC260126 could protect MIN6 β cells from palmitate-induced ER stress and apoptosis .
|
-
- HY-B0006S
-
|
|
Adrenergic Receptor
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Carvedilol-d3 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker[1]. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome[3].
|
-
- HY-B0006S1
-
|
BM 14190-d4
|
Adrenergic Receptor
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Carvedilol-d4 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker[1]. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome[3].
|
-
- HY-134539
-
IMT1
3 Publications Verification
|
Oxidative Phosphorylation
Mitochondrial Metabolism
DNA/RNA Synthesis
|
Metabolic Disease
Cancer
|
|
IMT1 is a first-in-class specific and noncompetitive human mitochondrial RNA polymerase (POLRMT) inhibitor. IMT1 causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro. IMT1 reduces deoxynucleoside triphosphate levels and citric acid cycle intermediates, resulting in a marked depletion of cellular amino acid levels. IMT1 has the potential for mitochondrial transcription disorders related diseases .
|
-
- HY-B0006S2
-
-
- HY-152019
-
|
|
EGFR
|
Cancer
|
|
EGFR/C797S-IN-1 is a potent EGFR-C797S inhibitor with an IC50 value of 0.128 µM. EGFR/C797S-IN-1 shows anti-proliferative activity and anti-tumor activity. EGFR/C797S-IN-1 inhibits the expression of p-EGFR in a dose-dependent manner .
|
-
- HY-108554
-
|
|
Protease Activated Receptor (PAR)
|
Others
|
|
Q94 hydrochloride, a selective PAR1 antagonist (IC50=916 nM), can selectively block PAR1/Gαq interaction and signalling. Q94 hydrochloride blocks PAR1-mediated increases in both CCL2 mRNA and protein levels in a dose-dependent manner. Q94 hydrochloride also completely blocks thrombin-induced ERK1/2 and MLC phosphorylation .
|
-
- HY-B0006R
-
|
BM 14190 (Standard)
|
Adrenergic Receptor
Autophagy
Bacterial
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Carvedilol (Standard) is the analytical standard of Carvedilol. This product is intended for research and analytical applications. Carvedilol (BM 14190) is a non-selective β/α-1 blocker . Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure . Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome .
|
-
- HY-107036
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
BMS-394136 (compound 1) is a potent inhibitor of Kv 1.5, with an IC50 of 0.05 μM. BMS-394136 is a selective IKur inhibitor. BMS-394136 dose-dependently prolongs atrial effective refractory period (AERP) and action potential duration (APD) without effecting ventricular effective refractory period (VERP). BMS-394136 can be used for acute atrial ischemia research .
|
-
- HY-100022A
-
|
eFT508 hydrochloride
|
MNK
PD-1/PD-L1
|
Cancer
|
|
Tomivosertib hydrochlorideis a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib hydrochloride treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines . Tomivosertib hydrochloride also dramatically downregulates PD-L1 protein abundance .
|
-
- HY-19042
-
|
YM 638
|
Leukotriene Receptor
|
Inflammation/Immunology
|
YM-16638 is an orally active leukotriene (LT) antagonist. YM-16638 can inhibit the production of LTC4, LTD4, and LTE4 in guinea pig trachea, with IC50 values of 0.05 μM, 0.16 μM, and 0.096 μM, respectively. YM-16638 has a dose-dependent inhibitory effect on antigen-induced early and late respiratory responses in allergic sheep .
|
-
- HY-117955
-
|
WAY 141839; Co 2-6749
|
GABA Receptor
|
Neurological Disease
|
|
GMA-839 is a selective modulator of the γ-aminobutyric acid A receptor (GABAA) with an IC50 value of 230 nM. GMA-839 exhibits potent anxiolytic-like activity, demonstrating significant dose-dependent anxiolytic effects in animal models, with an effective oral dose of 1.6 mg/kg. Significant increases in punished responding were observed in squirrel monkeys and pigeons. GMA-839 shows promise for research in the field of anxiolytics .
|
-
- HY-122215
-
|
N-696
|
Others
|
Endocrinology
|
|
Tilisolol hydrochloride (N-696) is a non-selective β-adrenergic antagonist with vasodilatory and hypotensive activities. Tilisolol hydrochloride exerts its effects in canine coronary arteries by opening ATP-sensitive K+ channels. Tilisolol hydrochloride exhibits concentration-dependent relaxation in KCl-precontracted rat thoracic aorta. Tilisolol hydrochloride reduces diastolic blood pressure in a dose-dependent manner and slightly increases heart rate in spinal cord stimulated rats .
|
-
- HY-103484
-
|
|
Others
|
Cardiovascular Disease
|
|
GATA4-NKX2-5-IN-1 (Compound 3) dose-dependently inhibits the GATA4–NKX2-5 transcriptional synergy with an IC50 of 3 μM. GATA4-NKX2-5-IN-1 exhibits no activity on the protein kinases involved in the regulation of GATA4 phosphorylation, and it modulates the hypertrophic agonist-induced cardiac gene expression .
|
-
- HY-111751
-
|
|
iGluR
|
Neurological Disease
|
|
JNJ-61432059 is an oral active and selective negative modulator of AMPAR associated with trans-membrane AMPAR regulatory protein (TARP) γ-8, with a pIC50 of 9.7 for GluA1/γ-8. Exhibits time- and dose-dependent AMPAR/γ-8 receptor occupancy in mouse hippocampus, resulting in robust seizure protection in corneal kindling and pentylenetetrazole (PTZ) anticonvulsant models .
|
-
- HY-N0407
-
|
6'-Cinnamoylcatalpol
|
STAT
|
Inflammation/Immunology
|
|
Picroside I is the major ingredient of Picrorhiza scrophulariiflora. Picrorhiza scrophulariiflora is a high value medicinal herb due to rich source of hepatoprotective metabolites, Picroside-I and Picroside-II . Picroside I is a promising agent for the management of asthma. Picroside I reduces the inflammation significantly at its higher dose. Picroside I also downregulates pSTAT6 and GATA3 expressions. Picroside I dose-dependently increases the serum levels of IFN-γ .
|
-
- 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-115497
-
BRD5529
2 Publications Verification
|
E1/E2/E3 Enzyme
|
Infection
Inflammation/Immunology
|
|
BRD5529 is an effective dose-dependent CARD9-TRIM62 protein–protein interaction (PPI) inhibitor with an IC50 value of 8.6 μM. BRD5529 has potency and complete inhibition of CARD9 ubiquitinylation in vitro, also has favorable solubility. BRD5529 can be used for the research of inflammatory bowel disease (IBD) such as Crohn’s disease (CD) and ulcerative colitis (UC) .
|
-
- HY-19541A
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
I-CBP112 hydrochloride is a selective inhibitor of CBP/P300 that directly binds their bromodomains (Kds = 142 and 625 nM, respectively). I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. I-CBP112 increases the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin .
|
-
- HY-101960
-
|
(Z)-AG-183
|
EGFR
|
Others
|
|
(Z)-Tyrphostin A51 is the Z configuration of Lanoconazole A51. Tyrphostin A51 is a potent protein tyrosine kinase (PTK) inhibitor. Tyrphostin A51 inhibits the volume-dependent release of [ 3H]taurine in a dose-dependent manner. Tyrphostin A51 markedly reduces cellular tyrosyl phosphorylation level. Tyrphostin A51 inhibits both basal and EGF-induced human bone cell proliferation .
|
-
- HY-150582
-
|
|
c-Met/HGFR
c-Kit
FLT3
Apoptosis
|
Cancer
|
|
c-Met-IN-14 (compound 26af) is a selective inhibitor of c-Met kinase from N-sulfonylamidine-based derivatives, with an IC50 value of 2.89 nM. c-Met-IN-14 shows anticancer activity by blocking phosphorylation of c-Met, and arrests cell cycle at G2/M phase. c-Met-IN-14 induces apoptosis of A549 cells in a dose-dependent manner .
|
-
- HY-161260
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 20 (compound H27) is a low cytotoxicity P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 20 inhibits the efflux function of P-gp in a dose-dependent manner (without affecting the expression of P-gp), thereby reversing the multidrug resistance (MDR) of MCF-7/ADR cells, with an IC50 value of 46.6 nM. P-gp inhibitor 20 can be used for cancer research .
|
-
- HY-B0094S3
-
|
Qinghaosu-13C,d4; NSC 369397-13C,d4
|
Ferroptosis
Akt
Parasite
HCV
Isotope-Labeled Compounds
|
Infection
Neurological Disease
Cancer
|
|
Artemisinin- 13C,d4 is 13C and deuterated labeled Artemisinin (HY-B0094). Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .
|
-
- HY-W015912S
-
|
2-Furyl methyl ketone-d3
|
Isotope-Labeled Compounds
|
Others
|
|
2-Acetylfuran-d3 is deuterated labeled Citreoviridin (HY-N6745). Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na +/K +-ATPase whereas in microsomes, both Na +/K +-ATPase and Mg 2+-ATPase activities are significantly stimulated in a dose-dependent manner . Citreoviridin inhibits cell proliferation and enhances apoptosis of human umbilical vein endothelial cells .
|
-
- HY-161894
-
|
|
CFTR
|
Inflammation/Immunology
|
|
CFTR corrector 13 (SVQ18) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector (EC50=3.14 μM). CFTR corrector 13 enhances the function of CFTR channels, especially when used in combination with Lumacaftor (HY-13262), it can produce a dose-dependent increase in CFTR function. CFTR corrector 13 can be used in the study of cystic fibrosis (CF) and other CFTR-related diseases .
|
-
- HY-100022
-
|
eFT508
|
MNK
PD-1/PD-L1
|
Cancer
|
|
Tomivosertib (eFT508) is a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib (eFT508) treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines . Tomivosertib (eFT508) also dramatically downregulates PD-L1 protein abundance .
|
-
- HY-145814
-
|
|
HSP
Fungal
|
Infection
|
|
HSP90-IN-9 is a potent and selective HSP90 inhibitor. HSP90-IN-9 displays a fungicidal effect in a dose-dependent manner. HSP90-IN-9 inhibits fungal biofilm formation and fungal morphological changes after being combined with FLC. HSP90-IN-9 recovers FLC resistance by down-regulating the expression of related genes (ERG11, CDR1 and CDR2) .
|
-
- HY-143472
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
|
PI3Kδ-IN-11 is a highly potent and selective PI3Kδ inhibitor with IC50 value of 27.5 nM. PI3Kδ-IN-11 dose-dependently blocks the activity of PI3K/Akt pathway. PI3Kδ-IN-11 can be used for researching B or T cell-related malignancies .
|
-
- HY-P4641
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
H-Trp-Phe-OH is a dipeptide consisting of tryptophan and phenylalanine (Trp-Phe). H-Trp-Phe-OH is also an antihypertensive peptide with inhibitory activity on angiotensin-converting enzyme (ACE), dose-dependently increases NO levels, and decreases endothelin-1 (ET-1) levels. H-Trp-Phe-OH (2 mg/kg; subcutaneous injection; 6 injections over 3 days) causes an increase in ovarian weight in female mice .
|
-
- HY-107655
-
|
ABET
|
mAChR
|
Cardiovascular Disease
|
|
Arecaidine but-2-ynyl ester tosylate (ABET) is a selective mAChR M2 agonist that dose-dependently decreases mean arterial pressure and heart rate in rats. Arecaidine but-2-ynyl ester tosylate can be used for cardiovascular disease research . Arecaidine but-2-ynyl ester (tosylate) 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-P4984
-
|
|
Biochemical Assay Reagents
|
Inflammation/Immunology
Cancer
|
|
Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) is a T cell proliferation activator. Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) promotes the in vitro proliferation of human peripheral blood mononuclear cells (PBMC) in a dose-dependent manner. Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) can be used in research on inflammatory and immunity, as well as cancer .
|
-
- HY-162011
-
|
|
EBI2/GPR183
|
Inflammation/Immunology
|
|
GPR183 antagonist-2 (compound 32) is a selective GPR183 antagonist with good water solubility and excellent pharmacokinetic properties. GPR183 antagonist-2 significantly reduces paw and joint swelling and gene expression of pro-inflammatory cytokines (MCP-1, MMPs, and VEGF) in a collagen-induced arthritis (CIA) mouse model in a dose-dependent manner. GPR183 antagonist-2 can be used in the study of autoimmune diseases .
|
-
- HY-101664R
-
|
|
Proton Pump
TOPK
|
Inflammation/Immunology
Cancer
|
|
Ilaprazole (Standard) is the analytical standard of Ilaprazole. This product is intended for research and analytical applications. Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
|
-
- HY-19202
-
|
rac-EMA401; rac-PD-126055; EMA400
|
Angiotensin Receptor
|
Neurological Disease
|
|
rac-Olodanrigan (rac-EMA401; EMA400) is a racemic mixture of the S-enantiomer (EMA401; HY-13106) and R-enantiomer (EMA402). rac-Olodanrigan is a potent and selective AT2 receptor antagonist with IC50s of 75.2 nM and 2918 nM for AT2R and AT1R, respectively. rac-Olodanrigan evokes dose-dependent relief of mechanical allodynia in the ipsilateral hind paws of rats with a chronic constriction injury (CCI) of the sciatic nerve .
|
-
- HY-10281
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
YM-60828 is an FXa inhibitor with antithrombotic properties. In the rat arteriovenous shunt model, YM-60828 does not prolong coagulation time but reduces the levels of thrombin-antithrombin III complex (TAT) in a dose-dependent manner. YM-60828 exhibits only anti-FXa activity and does not show anti-thrombin activity, indicating that its antithrombotic effect is independent of thrombin. Therefore, the antithrombotic effect of YM-60828 can be monitored by TAT .
|
-
- HY-169060
-
|
|
Lactate Dehydrogenase
|
Cancer
|
|
LDHA-IN-8 (Compound 6) is a lactate dehydrogenase (LDHA) inhibitor. LDHA-IN-8 inhibits LDHA catalysis of pyruvate in a dose-dependent manner (EC50 value of 14.54 μM), reduces intracellular lactate levels, and increases intracellular reactive oxygen species (ROS) levels, thereby inhibiting the proliferation of pancreatic cancer cells and lung cancer cells. LDHA-IN-8 holds promise for research in the field of LDHA-related antitumor therapies .
|
-
- HY-119379
-
|
HOE-720 free acid
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Fonsartan (HOE-720) free acid is an orally active angiotensin II receptor (AT1R) antagonist with an IC50 value of 0.48 nM, exhibiting potent antihypertensive activity. Fonsartan free acid dose-dependently inhibits angiotensin II-induced pressor response in rats (ID50 = 0.11 mg/kg) and shows significant long-lasting blood pressure-lowering effects in high-renin animal models. Fonsartan free acid is primarily used in research on hypertension and cardiovascular diseases .
|
-
- HY-118665
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
L-736380 is a high affinity CCK-B (cholecystokinin B receptor) receptor antagonist, with IC50 values of 0.054 nM and 400 nM for CCK-B and CCK-A, respectively. L-736380 dose-dependently inhibits gastric acid secretion in anesthetized rats (ID50, 0.064 mg/kg) and ex vivo binding of [125I]CCK-8S in BKTO mice brain membranes (ED50, 1.7 mg/kg) .
|
-
- HY-101390B
-
|
|
Others
|
Cardiovascular Disease
|
|
Niguldipine free base is a calcium channel blocker with activity in regulating cardiovascular function. Niguldipine free base can reduce systolic and diastolic blood pressure, thereby increasing heart rate and cardiac output. Niguldipine free base exhibits dose-dependent and sustained increases in coronary blood flow. Niguldipine free base also increases perfusion in the kidneys and femoral arteries, but the effect is temporary and to a lesser extent. The effect of Niguldipine free base on myocardial metabolism is not significant .
|
-
- HY-P10711
-
|
|
Autophagy
|
Cancer
|
|
ALA-A2 is an anticancer peptide discovered in alpha-lactalbumin that selectively kills cancer cells by inducing Autophagy. ALA-A2 has cell-penetrating capabilities, allowing it to effectively enter cells without relying on membranolytic effects. In A549 lung cancer cells, ALA-A2 demonstrates significant dose-dependent anticancer activity. ALA-A2 holds promise for research in cancer therapy and autophagy regulation .
|
-
- HY-N13739
-
|
|
Tyrosinase
|
Cancer
|
|
Taraxinic acid can be found in the roots of Taraxacum flavostylum and Taraxacum lucidum. It is a Tyrosinase inhibitor that dose-dependently inhibits Tyrosinase activity, showing approximately 54.5% inhibition at a concentration of 50 μg/mL. Taraxinic acid has an IC50 of 83.2 μM against melanoma cells A375 and HTB140, and an IC50 of 60.4 μM against melanoma cells WM793, with activity being both dose- and time-dependent. Taraxinic acid holds promise for research in the field of anticancer therapy .
|
-
- HY-N0303
-
|
|
Mitochondrial Metabolism
Apoptosis
|
Neurological Disease
|
|
Idebenone, a well-appreciated mitochondrial protectant, exhibits protective efficacy against neurotoxicity and can be used for the research of Alzheimer's disease, Huntington's disease. Idebenone (oxidised form) has a dose-dependent inhibitory effect on the enzymatic metabolism of arachidonic acid in astroglial homogenates (IC50=16.65 μM) . Idebenone, a coenzyme Q10 analog and an antioxidant, induces apoptotic cell death in the human dopaminergic neuroblastoma SHSY-5Y cells . Idebenone quickly crosses the blood-brain barrier.
|
-
- HY-N9182
-
|
Physalien
|
Adiponectin Receptor
P2X Receptor
Autophagy
|
Inflammation/Immunology
|
|
Zeaxanthin dipalmitate (Physalien) is a wolfberry-derived carotenoid, has anti-inflammatory and anti-oxidative stress effects. Zeaxanthin dipalmitate directly interact with p2X7 receptor (Kd=81.2 nM) and adiponectin receptor 1 (AdipoR1; Kd=533 nM) in a positive dose-dependent manner. Zeaxanthin dipalmitate restores mitochondrial autophagy functions suppressed by ethanol intoxication. Zeaxanthin dipalmitate can be used in the research of alcoholic fatty liver disease (AFLD) and retinitis pigmentosa (RP) .
|
-
- HY-108020
-
|
|
Free Fatty Acid Receptor
|
Endocrinology
|
|
LY2881835 is a potent and selective agonist of G protein-coupled receptor 40 (GPR40). LY2881835 has efficacious and durable dose-dependent reductions in glucose levels along with significant increases in insulin and GLP-1 secretion. LY2881835 has the potential for the research of type 2 diabetes mellitus . LY2881835 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-146221
-
|
|
DYRK
|
Neurological Disease
|
|
Dyrk1A-IN-5 (compound 5j) is a potent and selective DYRK1A inhibitor, with an IC50 of 6 nM. Dyrk1A-IN-5 dose-dependently reduces the phosphorylation of Thr434 in SF3B1, with an IC50 of 0.5 μM. Dyrk1A-IN-5 inhibits phosphorylation of tau at Thr212, with an IC50 of 2.1 μM. Dyrk1A-IN-5 can be used for Down syndrome research .
|
-
- HY-118304B
-
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FLT3
Apoptosis
Caspase
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Cancer
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AKN-028 acetate, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 acetate inhibits FLT3 autophosphorylation. AKN-028 acetate induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 acetate induces apoptosisby activation of caspase 3. AKN-028 acetate can be used in research of acute myeloid leukemia (AML).
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- HY-N11910
-
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Biochemical Assay Reagents
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Others
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Kaempferol-3-O-[(6-caffeoyl)-β-glucopyranosyl (1→3) α-rhamnopyranoside]-7-O-α-rhamnopyranoside (Compound 3) is a wound healing agent with dose-dependent wound healing ability. Kaempferol-3-O-[(6-caffeoyl)-β-glucopyranosyl (1→3) α-rhamnopyranoside]-7-O-α-rhamnopyranoside can be used for wound repair research .
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![Kaempferol-3-O-[(6-caffeoyl)-β-glucopyranosyl (1→3) α-rhamnopyranoside]-7-O-α-rhamnopyranoside](//file.medchemexpress.eu/product_pic/hy-n11910.gif)
- HY-157325
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RIP kinase
|
Inflammation/Immunology
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RIPK2-IN-5 (compound 14) is a high affinity and excellent selectivity RIPK2 inhibitor with an IC50 value of 5.1nM. RIPK2-IN-5 has cellular anti-inflammatory effect and can reduce the secretion of MDP-induced TNF-α with a dose-dependent manner. RIPK2-IN-5 shows moderate stability in human liver microsome. RIPK2-IN-5 can be used for the research of immune diseases .
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- HY-158031
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Apoptosis
Polo-like Kinase (PLK)
Epigenetic Reader Domain
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Cancer
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PLK1/BRD4-IN-5 (Compound SC10) is an orally active PLK1 and BRD4 inhibitor with IC50 values of 0.3 nM and 60.8 nM, respectively. PLK1/BRD4-IN-5 can induce MV4-11 cell block in S phase and apoptosis) in a dose-dependent manner. PLK1/BRD4-IN-5 can be used in cancer research .
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- HY-160943A
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SARS-CoV
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Infection
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F594-1001 (compound 6) hydrochloride is a potent and highly selective SARS-CoV-2 Mac1-ADP-ribose inhibitor with IC50s of 8.5 μM, 68 μM and 45 μM for SARS-CoV-2 in AS, FP, and FRET assays, respectively. F594-1001 hydrochloride directly binds to SARS-CoV-2 Mac1 and exhibits a dose-dependent inhibition of Mac1 ADP-ribosylhydrolase activity .
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- HY-160943
-
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SARS-CoV
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Infection
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F594-1001 (compound 6) is a potent and highly selective SARS-CoV-2 Mac1-ADP-ribose inhibitor with IC50s of 8.5 μM, 68 μM and 45 μM for SARS-CoV-2 in AS, FP, and FRET assays, respectively. F594-1001 directly binds to SARS-CoV-2 Mac1 and exhibits a dose-dependent inhibition of Mac1 ADP-ribosylhydrolase activity .
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- HY-B0380B
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GIC-1001
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Others
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Others
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Trimebutine 3-TCBS (GIC-1001) is an innovative formulation designed to release hydrogen sulfide (H2S) in vivo. This compound combines trimebutine with an H2S-releasing antagonist (phenyl 3-thiocarbamate) and exhibits enhanced anti-nociceptive effects in a mouse colonic distension model, superior to conventional trimebutine. GIC-1001 can reduce visceral pain and discomfort associated with lumen distension in a dose-dependent manner, showing potential superiority .
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- HY-B1246R
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Bacterial
Proton Pump
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Infection
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Thonzonium (bromide) (Standard) is the analytical standard of Thonzonium (bromide). This product is intended for research and analytical applications. Thonzonium bromide is an antibacterial agent that is structurally similar to Farnesol (HY-Y0248A). Thonzonium bromide is also a monocationic surface-active agent, which inhibits RANKL-induced osteoclast formation and bone resorption in vitro and prevents LPS-induced bone loss in vivo. Thonzonium bromide inhibits proton transport in a dose-dependent manner (EC50=69 μM) .
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- HY-106963
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LGD1550
|
RAR/RXR
|
Cancer
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ALRT1550 (LGD1550) is a selective retinoic acid receptor (RAR) agonist that binds RARs with exceptional potency, with Kd values of approximately 1-4 nM. ALRT1550 exhibits anti-proliferative activity, with an IC50 value of 0.22 nM in UMSCC-22B squamous carcinoma cells. In a mouse tumor xenograft model, ALRT1550 inhibited tumor growth in a dose-dependent manner, achieving a maximum inhibition rate of 89%. ALRT1550 is applicable for research in the field of cancer .
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- HY-100481
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RPR101048
|
Cholecystokinin Receptor
|
Neurological Disease
|
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RP 72540 is a selective CCK-B receptor antagonist, with IC50 values of 2.4, 1.2, and 3.8 nM for CCK-B receptors in the guinea pig cerebral cortex, rat cerebral cortex, and mouse brain, respectively. RP 72540 effectively inhibits CCK-8-induced neuronal firing and dose-dependently inhibits gastric acid secretion, making it potentially valuable in studies of acid secretion. RP 72540 is an important tool for investigating the physiological functions of CCK B receptors .
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- HY-105271
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S-(+)-S-312-d
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Others
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Others
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S-312-d (S-(+)-S-312-d) is a calcium channel blocker with the activity of protecting the kidney from ischemic acute renal failure. S-312-d (0.01-0.1mg/kg b.wt. iv) administered before ischemia has a dose-dependent protective effect on ischemia-induced renal damage, improves the survival rate of ischemic rats, and reduces renal cortical edema and the increase in renal tissue calcium content.
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- HY-168615
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IKZF Family
Casein Kinase
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Cancer
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MGD-28 is a potent, orally active, Cereblon (CRBN)-dependent IKAROS protein degrader that degrades IKZF1 (DC50=3.8 nM), IKZF2 (DC50=56.3 nM), and IKZF3 (DC50=7.1 nM) in a dose-dependent manner. In addition, MGD-4 also degrades CK1α (DC50=7.8 nM). MGD-28 has antiproliferative activity and can be used in multiple myeloma research .
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- HY-123440
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-
- HY-P0249
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-
- HY-N0528
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-
- HY-113439S
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Apoptosis
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Cardiovascular Disease
Inflammation/Immunology
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12-HETE-d8 is the deuterium labeled 12-HETE. 12-HETE, a major metabolic product of arachidonic acid using 12-LOX catalysis, inhibits cell apoptosis in a dose-dependent manner. 12-HETE promotes the activation and nuclear translocation of NF-κB through the integrin-linked kinase (ILK) pathway[1].12-HETE has both anti-thrombotic and pro-thrombotic effects[2]. 12-HETE is a neuromodulator[3].
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- HY-123972
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KL-2
|
DNA/RNA Synthesis
|
Cancer
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SEC inhibitor KL-2 (KL-2), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-2 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 1.50 μM .
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- HY-118304
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FLT3
Apoptosis
Caspase
|
Cancer
|
|
AKN-028, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6?nM. AKN-028 inhibits FLT3 autophosphorylation. AKN-028 induces dose-dependent cytotoxic response (mean IC50=1?μM). AKN-028 induces apoptosisby activation of caspase 3. AKN-028 can be used in research of acute myeloid leukemia (AML) .
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- HY-146169
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Reactive Oxygen Species
Microtubule/Tubulin
|
Cancer
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Antitumor agent-68 is a potent tubulin inhibitor. Antitumor agent-68 shows potent anticancer activity with IC50s of 3.6 and 3.8 μM for HeLa and MCF-7 cells, respectively. Antitumor agent-68 exhibits good scavenging activity of ROS and DPPH radical in a dose-dependent manner . Antitumor agent-68 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-B2078
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Others
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Inflammation/Immunology
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Eprazinone can enhance lung function and arterial oxygen levels and can be used in the study of chronic bronchitis. Higher doses of eprazinone increased phospholipid levels and decreased neutral lipid content in bronchoalveolar lavage (BAL) fluid, but had no effect on protein and cell levels in BAL. Eprazinone dose-dependently reduced short-circuit current (Isc), primarily by reducing chloride secretion at lower concentrations and affecting sodium and chloride transport at higher doses. Eprazinone may exert its anti-inflammatory effects by regulating BAL lipid composition and airway ion transport .
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- HY-N0407R
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STAT
|
Inflammation/Immunology
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Picroside I (Standard) is the analytical standard of Picroside I. This product is intended for research and analytical applications. Picroside I is the major ingredient of Picrorhiza scrophulariiflora. Picrorhiza scrophulariiflora is a high value medicinal herb due to rich source of hepatoprotective metabolites, Picroside-I and Picroside-II . Picroside I is a promising agent for the management of asthma. Picroside I reduces the inflammation significantly at its higher dose. Picroside I also downregulates pSTAT6 and GATA3 expressions. Picroside I dose-dependently increases the serum levels of IFN-γ .
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- HY-163987
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Sirtuin
|
Neurological Disease
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SIRT3 activator 2 (compound 2a) is a SIRT3 activator. SIRT3 activator 2 improved the thermal stability of SIRT3 in SH-SY5Y cells, indicating that it can directly bind to SIRT3, has SIRT3 dependency in SH-SY5Y to clear α-Syn. SIRT3 activator 2 improves motor function in Parkinson mice, preventing Parkinson (DA) neuron loss in the substantia nigra in a dose-dependent manner .
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- HY-124547
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Endogenous Metabolite
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Others
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2,4-D methyl ester is a bioactive compound with the activity of promoting the accumulation of nutritional and medicinal components. 2,4-D methyl ester can be used to enhance the production of bioactive components in Cordyceps militaris. 2,4-D methyl ester showed an inductive effect on bioactive components at specific concentrations. The application of 2,4-D methyl ester provides an effective strategy to improve the fruit quality of Cordyceps militaris. 2,4-D methyl ester, as a biostimulant, can induce dose-dependent responses in different components .
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- HY-123461
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Others
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Inflammation/Immunology
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Sul-121 hydrochloride is a novel compound with anti-oxidative capacity that effectively inhibits airway inflammation and hyperresponsiveness (AHR) in experimental models of chronic obstructive pulmonary disease (COPD). Sul-121 hydrochloride prevents lipopolysaccharide-induced airway neutrophilia and AHR in a dose-dependent manner. Sul-121 hydrochloride also demonstrates the ability to reduce oxidative stress markers in human airway smooth muscle cells. Sul-121 hydrochloride inhibits nuclear translocation of the NF-κB subunit, p65, thereby diminishing pro-inflammatory cytokine release.
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- HY-168660
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PROTACs
Apoptosis
CDK
|
Cancer
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CPD-10 is a potent CCND1 and CDK4 PROTAC degrader. CPD-10 shows anti-proliferation. CPD-10 induces apoptosis. CPD-10 decreases the protein expression of cyclin D1, cyclin D3, CDK4, P-Rb(5807/811) in a dose-dependent manner. (Pink: ligand for target protein (HY-50767); black: linker (HY-22391); Blue: E3 ligase ligand (HY-168667)) .
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- HY-P0249B
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-
- HY-12624
-
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ON123300
|
CDK
AMPK
PDGFR
|
Cancer
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Narazaciclib (ON123300), a strong and brain-penetrant multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent Narazaciclib causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors . Narazaciclib inhibits CDK6 with an IC50 of 9.82 nM .
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- HY-N10439
-
|
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Glycosidase
|
Inflammation/Immunology
|
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3β-Acetoxy-hop-22(29)-ene (compound 1) is a potent anti-inflammatory agent. 3β-Acetoxy-hop-22(29)-ene shows high inhibitory activity of yeast α-glucosidase, with an IC50 of 5.74 μM. 3β-Acetoxy-hop-22(29)-ene inhibits MPO (myeloperoxidase) activity in a dose-dependent manner in mouse ear edema model induced by 12-O-tetradecanoylphorbol acetate (TPA), with an IC50 of 0.23 μmol/ear .
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- HY-155027
-
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Dipeptidyl Peptidase
TNF Receptor
Interleukin Related
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Inflammation/Immunology
Cancer
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DPP-4-IN-8 (compound 27) is a potent and selective DPP4 (dipeptidyl peptidase 4) inhibitor, with a Ki of 0.96 μM. DPP-4-IN-8 blocks the dipeptidase activity of DPP4 in both Caco-2 and HepG-2 cells. DPP-4-IN-8 also dose-dependently suppresses the expression levels of the chemokines tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-1β (IL-1β) .
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- HY-19210
-
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Endothelin Receptor
|
Cardiovascular Disease
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SB-209670 is an extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist. SB 209670 selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (Ki=0.2 and 18 nM, respectively). SB 209670 produces a dose-dependent reduction in blood pressure in hypertensive rats, protects from ischemia-induced neuronal degeneration in a gerbil stroke model, and attenuates neointima formation following rat carotid artery balloon angioplasty .
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- HY-135783
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nAChR
|
Neurological Disease
|
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AT 1001 is a high-affinity and selective antagonist of the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) (Ki=2.64 nM). AT 1001 reversibly blocks inward currents induced by Epibatidine (HY-101078) in HEK cells transfected with α3β4 nAChR. AT-1001 dose-dependently inhibits nicotine self-administration behavior in rats without affecting food-reinforced responding. AT 1001 can be utilized in the research of nicotine addiction and smoking cessation therapies .
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- HY-121586
-
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Bay g 6575
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Others
|
Cardiovascular Disease
|
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Nafazatrom (Bay g 6575) is an orally active cardioprotective agent that protects against ischemic damage. Nafazatrom dose-dependently inhibits neutrophil aggregation, superoxide anion generation, arachidonic acid metabolism, and to a lesser extent the release of β-glucosidase, platelet aggregation or arachidonic acid in vitro. Acid metabolism has no significant effect. In a dog ischemia-reperfusion model, Nafazatrom (10 mg/kg; po) reduced infarct size and the occurrence of arrhythmias and rescued ischemic myocardial function without affecting any hemodynamic changes. The basis of Nafazatrom's cardioprotection may be inhibition of neutrophil function and cellular infiltration in vitro .
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- HY-136634
-
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Others
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Others
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BTM-1042 is a newly synthesized compound with antispasmodic effects. It can inhibit the twitch reaction of the guinea pig ileum under electrical stimulation and is not affected by naloxone. It has similar effects to atropine and can block muscarinic receptors, but has less effect on other types of receptors. BTM-1042 also has an inhibitory effect on the ileal reaction caused by nicotine and 5-hydroxytryptamine. BTM-1042 showed a dose-dependent inhibitory effect on the spontaneous movement of the rabbit stomach. In general, BTM-1042 is a agent with a strong antispasmodic effect.
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- HY-164525
-
|
SC-81490; PF-02881307
|
MMP
|
Cancer
|
|
SD-7300 (SC-81490) is an orally active inhibitor of MMP-2, MMP-9, and MMP-13 with Ki values ??of 0.03, 0.01, and 0.03 nM, respectively. SD-7300 can reduce the degradation of extracellular matrix by tumor cells, thereby inhibiting the invasion and metastasis of tumor cells. In addition, SD-7300 is also a dose-dependent inhibitor of mouse corneal angiogenesis and an inhibitor of interleukin-1-induced bovine cartilage degradation. SD-7300 can be used in breast cancer research .
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-
- HY-135555
-
|
5-CT
|
5-HT Receptor
|
Neurological Disease
|
|
5-Carboxamidotryptamine (5-CT) is a 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5A, 5-HT7 receptor agonist . 5-Carboxamidotryptamine has a Ki value of 4.6 nM for cloned human 5-HT5A receptor. 5-Carboxamidotryptamine causes a dose-dependent reduction in rectal temperature of mice .
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-
- HY-118304A
-
|
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FLT3
Apoptosis
Caspase
|
Cancer
|
|
AKN-028 TFA, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6?nM. AKN-028 TFA inhibits FLT3 autophosphorylation. AKN-028 TFA induces dose-dependent cytotoxic response (mean IC50=1?μM). AKN-028 TFA induces apoptosisby activation of caspase 3. AKN-028 TFA can be used in research of acute myeloid leukemia (AML) .
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- HY-167848
-
|
XL-118
|
Others
|
Cardiovascular Disease
|
|
DMP-728 free base (XL-118) is a highly potent and selective GPIIb/IIIa antagonist with antiplatelet and antithrombotic activities. DMP-728 free base can inhibit ADP-induced human platelet aggregation in vitro, with an IC50 of 46 nmol/L, and can significantly reduce the interaction between fibrinogen and human platelets or Binding of purified human GPIIb/IIIa receptors. DMP-728 free base exhibits dose-dependent antiplatelet effects in anesthetized mongrel dogs, effectively inhibiting ADP-induced platelet aggregation and prolonging template bleeding time .
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-
- HY-150739A
-
-
- HY-112650
-
-
- HY-119977
-
|
|
Reactive Oxygen Species
|
Others
|
|
APF is a fluorescence probe that can selectively, and dose dependently detect certain species among ROS and that are highly resistant to autoxidation. APF can be used in enzymatic and cellular systems .
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-
- HY-147391
-
|
|
Sodium Channel
|
Neurological Disease
|
|
ASIC-IN-1 is a potent acid sensing ion channel inhibitor with an IC50 value of < 10 µM. ASIC-IN-1 causes a dose- dependent reduction of the pain intensity .
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- HY-124798
-
|
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mTOR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Rheb inhibitor NR1 is a Rheb inhibitor with an IC50 of 2.1 µM in the Rheb-IVK assay. Rheb inhibitor NR1 can directly bind Rheb in the switch II domain and selectively inhibit the activation of mechanistic target of rapamycin complex 1 (mTORC1). Rheb inhibitor NR1 inhibits the phosphorylation of mTORC1 driven T389pS6K1 and increases the phosphorylation of S473pAKT in a dose-dependent manner. Rheb inhibitor NR1 does not influence mTORC2 activity .
(Rheb-IVK: Rheb-dependent mTORC1 kinase activity)
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-
- HY-148252
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
ADRA1D receptor antagonist 1 (free base) (compound (R)-9s) is an orally active, potent and selective human α1D-adrenoceptor (α1D-AR) antagonist (Ki=1.6 nM). ADRA1D receptor antagonist 1 (free base) dose-dependently inhibits bladder contraction with an IC30 value of 15 nM. ADRA1D receptor antagonist 1 (free base) can be used in studies of overactive bladder disorders such as urinary urgency, frequency and incontinence.
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-
- HY-151799
-
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p62
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
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|
P62-RNF168 agonist-1 (compound 5a) is a low cytotoxicity P62-RNF168 agonist that enhances the interaction between P62 and RNF168. P62-RNF168 agonist-1 induces a reduction in H2A ubiquitination mediated by RNF168 and impairs homologous recombination-mediated DNA repair. P62-RNF168 agonist-1 also inhibits the growth of xenograft tumors in mice in a dose-dependent manner .
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-
- HY-163527
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13 regulates endogenous FGFR1(IC50=0.20±0.02 nM) and FGFR4(IC50=0.40±0.03 nM) mediated signaling pathways by inhibiting the expression of key proteins. FGFR-IN-13 inhibits total-PARP and Bcl-2 protein expressions, and promote Cleaved-PARP and Bax protein expressions in a dose-dependent manner. FGFR-IN-13 has significant antitumor activity and oral activity .
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- HY-N0303R
-
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|
Mitochondrial Metabolism
Apoptosis
|
Neurological Disease
|
|
Idebenone (Standard) is the analytical standard of Idebenone. This product is intended for research and analytical applications. Idebenone, a well-appreciated mitochondrial protectant, exhibits protective efficacy against neurotoxicity and can be used for the research of Alzheimer's disease, Huntington's disease. Idebenone (oxidised form) has a dose-dependent inhibitory effect on the enzymatic metabolism of arachidonic acid in astroglial homogenates (IC50=16.65 μM) . Idebenone, a coenzyme Q10 analog and an antioxidant, induces apoptotic cell death in the human dopaminergic neuroblastoma SHSY-5Y cells . Idebenone quickly crosses the blood-brain barrier.
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- HY-121634
-
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Polo-like Kinase (PLK)
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Others
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DAP-81 is an inhibitory agent targeting Polo-like kinases (Plks), a class of evolutionarily conserved serine/threonine kinases. DAP-81 dose-dependently increases the number of monopolar spindles in treated cells. High-resolution live-cell microscopy revealed that Plk activity is required for the assembly and maintenance of bipolar mitotic spindles. Plk inhibition destabilizes centromeric microtubules while stabilizing other spindle microtubules, leading to the formation of monopolar spindles. Further testing of compounds based on "privileged scaffolds" such as the DAP scaffold may lead to the discovery of new cell division probes and anti-microtubule agents.
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- HY-115860
-
|
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Others
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Neurological Disease
|
|
TAS-4 is a potent and selective mGluR4 positive allosteric modulator with significant anti-Parkinson's disease activity. TAS-4 is able to show efficacy when used alone or in combination with l-DOPA. TAS-4 is able to reverse haloperidol-induced spasticity when administered alone. TAS-4 enhances the contralateral rotation behavior induced by l-DOPA in a dose-dependent manner. TAS-4 combined with low-dose l-DOPA shows anti-Parkinson's effects similar to full-dose l-DOPA without exacerbating abnormal motor side effects .
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-
- HY-18940
-
|
Cilo
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Others
|
Cardiovascular Disease
|
|
Cilobradine (Cilo) is a HCN channel blocker with heart rate reducing activity. Cilobradine blocks the slow inward current of human HCN1, HCN2, HCN3, and HCN4 channels. Cilobradine has a slightly higher efficiency in blocking endogenous If in mouse sinoatrial node cells (IC50 value is 0.62μM). Cilobradine can dose-dependently reduce the heart rate from 600 to 200 bpm with an ED50 value of 1.2 mg/kg. Cilobradine induces arrhythmias at doses greater than 5 mg/kg, which are characterized by periodic fluctuations between T waves and P waves .
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-
- HY-18957C
-
|
BGB-283 hydrochloride
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Others
|
Cancer
|
|
Lifirafenib hydrochloride (BGB-283 hydrochloride) is a novel, reversible B-RAFV600E inhibitor with antitumor activity. Lifirafenib has shown potent antitumor activity against solid tumors with B-RAFV600E mutations, such as melanoma, thyroid cancer, and low-grade serous ovarian cancer. Lifirafenib exhibits selective cytotoxicity in vitro, preferentially inhibiting the proliferation of cancer cells with B-RAFV600E and EGFR mutations/amplification. Lifirafenib can achieve dose-dependent inhibition of tumor growth in animal models, accompanied by partial and complete tumor shrinkage .
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-
- HY-101317A
-
|
SB-205607
|
Opioid Receptor
|
Metabolic Disease
|
|
TAN-67 (SB-205607) is a non-peptidic delta-opioid receptor agonist that exhibits significant antinociceptive activity in both diabetic and non-diabetic mice. TAN-67 demonstrates a marked and dose-dependent reduction in acetic acid-induced abdominal constrictions, with a notably stronger effect in diabetic mice compared to their non-diabetic counterparts. TAN-67's antinociceptive properties are primarily mediated through the activation of delta 1-opioid receptors, as indicated by the pronounced antagonism observed upon administration of a selective delta 1-opioid receptor antagonist.
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-
- HY-150739
-
-
- HY-12443
-
|
|
Casein Kinase
|
Neurological Disease
|
|
PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC50s of 3.9 nM and 17.0 nM, respectively. PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selectivity. PF-5006739 attenuats opioid agent-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner . PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity .
|
-
- HY-W007223
-
|
D-5-HTP; 5-Hydroxy-D-tryptophan
|
5-HT Receptor
|
Neurological Disease
|
|
D-5-Hydroxytryptophan (D-5-HTP) is the D-isomer of 5-HTP and can be isolated from DL-5-hydroxytryptophan by continuous separation. Compared with intraperitoneal administration of L-5-Hydroxytryptophan, which can induce dose-dependent backward walking behavior in mice, D-5-Hydroxytryptophan has no significant effect on mouse behavior and is a negative control. D-5-Hydroxytryptophan is also a 5-HT ligand, capable of binding to the 5-HT site with affinity in the micromolar range .
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-
- HY-155066
-
|
|
PI3K
mTOR
|
Cancer
|
|
FD274 is a highly potent PI3K/mTOR dual inhibitor with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research .
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-
- HY-157164
-
|
|
PROTACs
Histone Methyltransferase
|
Cancer
|
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PROTAC EZH2 Degrader-2 (compound E-3P-MDM2), an EZH2 inhibitor, is a PROTAC composed of Tazemetostat (EPZ6438) and an E3 ligase system ligand. PROTAC EZH2 Degrader-2 degrades EZH2 in SU-DHL-6 cells in a dose-dependent manner, inhibits the expression of H3K27me3, and simultaneously degrades EED and SUZ12 proteins without affecting their mRNA levels. PROTAC EZH2 Degrader-2 has anti-cancer and anti-proliferative activity .
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-
- HY-157295
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PI3K
HDAC
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Cancer
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|
PI3K/HDAC-IN-3 (36) is a PI3K and HDAC dual inhibitor, with IC50 values of 0.23 nM and 172 nM for PI3Kα and HDAC1, respectively. PI3K/HDAC-IN-3 (36) suppresses AKT phosphorylation and increased H3 acetylation in MV4-11 cells. PI3K/HDAC-IN-3 (36) exhibits significant and dose-dependent anticancer efficacy in a MV4-11 xenograft model .
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-
- HY-162103
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TAM Receptor
Apoptosis
|
Cancer
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|
Axl-IN-18 (compound 25c) is a potent and selective type II AXL inhibitor. Axl-IN-18 shows excellent AXL inhibitory activity (IC50=1.1 nM) and 343-fold selectivity over the highly homologous kinase MET in biochemical assays (IC50=377 nM). Axl-IN-18 significantly inhibits AXL-driven cell proliferation, dose-dependently suppresses 4T1 cell migration and invasion, and induces apoptosis. Axl-IN-18 shows noticeable antitumor efficacy in a BaF3/TEL-AXL xenograft model .
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- HY-121998
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Aurora Kinase
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Others
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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-125172
-
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Polyglutamine Aggregation inhibitor III
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Huntingtin
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Others
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|
C2-8 is an inhibitor of polyglutamine (polyQ) aggregation (IC50s=25 and 0.05 μM for recombinant HDQ51 and in PC12 cells, respectively). It also inhibits polyQ aggregation in organotypic hippocampal slice cultures isolated from R6/2 transgenic mice and reduces neurodegeneration in a dose-dependent manner in a Drosophila model of Huntington's disease. C2-8 (100 and 200 mg/kg) reduces huntingtin aggregate size, reduces neuronal atrophy, and improves motor performance in a rotarod test in the R6/2 transgenic mouse model of Huntington's disease.
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- HY-12191
-
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Histamine Receptor
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Metabolic Disease
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|
A-331440 is a potent and selective histamine H3 receptor antagonist that regulates neurotransmitter release by inhibiting presynaptic H3 receptors. In preclinical studies involving mice on a high-fat diet, A-331440 demonstrated dose-dependent effects on weight reduction and fat loss. At 5 mg/kg, it effectively decreased body weight comparable to dexfenfluramine, while at 15 mg/kg, it significantly reduced body fat and improved insulin tolerance, similar to mice on a low-fat diet. These findings suggest that A-331440 holds promise as an antiobesity agent by modulating histaminergic pathways involved in food intake and metabolic regulation .
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- HY-118775
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Others
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Others
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LEK 8804 is a compound with 5-HT1A receptor agonist and 5-HT2 receptor antagonist properties, and has the activity of modulating related receptor-mediated behavioral responses. LEK 8804 can induce spontaneous tail-flick response in rats in a dose-dependent manner, showing complete 5-HT1A agonist activity, and can inhibit 5-HTP-induced head twitch response in mice, probably through antagonism of 5-HT2 receptors rather than agonism of 5-HT1A receptors.
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- HY-113817
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Phosphatase
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Inflammation/Immunology
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SHIP1 activator 1 is an SH3 domain-containing inositol 5-phosphatase regulator with SHIP1 activating activity. SHIP1 activator 1 retains its SHIA-1 activating ability by removing unnecessary functional groups. SHIP1 activator 1 is able to activate SHIP1 in vitro, inhibit Akt phosphorylation in MOLT-4 cells, and show dose-dependent activity in a mouse model of inflammation. SHIP1 activator 1 is an important chemical tool for evaluating the potential of SHIP1 activators as inhibitors of hematopoietic diseases involving abnormal PI3K cell signaling .
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- HY-N6954
-
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ATM/ATR
STAT
CDK
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Cancer
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|
Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia that is used as an anti-inflammatory, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, while efficiently inhibiting the expression levels of cyclin B1, cyclin D1, cyclin E2, cdc2, Stat3 and CDK7. Garcinone C significantly inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner .
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- HY-P5900
-
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m3-HwTx-IV
|
Sodium Channel
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Neurological Disease
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|
m3-Huwentoxin IV (m3-HwTx-IV) is a potent NaV inhibitor with IC50s of 3.3, 6.8, 7.2, 8.4, 11.9 and 369 nM against hNaV1.7, hNaV1.6, hNaV1.3, hNaV1.1, hNaV1.2 and hNaV1.4, respectively in QPatch assay. m3-Huwentoxin IV dose-dependently suppresses spontaneous pain induced by the NaV1.7 activator OD1 in a rodent pain model .
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-
- HY-N7210
-
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Apoptosis
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Cancer
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|
Kahweol acetate, a bioactive compound found in coffee, has been identified for its potent anti-cancer properties, particularly in inhibiting the proliferation and migration of prostate cancer cells. Alongside cafestol, it shows dose-dependent effects in suppressing tumor growth and metastasis in both in vitro and in vivo studies. Mechanistically, kahweol acetate and cafestol induce apoptosis, inhibit epithelial-mesenchymal transition, and reduce androgen receptor activity, especially in androgen receptor-positive cells. They also downregulate chemokine receptors CCR2 and CCR5, crucial for cancer progression, without altering their ligand levels. These findings suggest that kahweol acetate, in combination with cafestol, may serve as promising therapeutic agents against prostate cancer .
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-
- HY-169059
-
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Ferroptosis
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Inflammation/Immunology
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Ferroptosis-IN-12 (Cpd-A1) is a ferroptosis inhibitor. Ferroptosis-IN-12 exhibits effective ferroptosis inhibition in Erastin (HY-15763)-treated mouse tubular epithelial cells (mTECs) and improves kidney function, alleviates renal tubular damage, and reduces inflammation in a dose-dependent manner in acute kidney injury (AKI) mouse models induced by ischemia/reperfusion (I/R) or cecal ligation and puncture (CLP). Ferroptosis-IN-12 demonstrates good plasma stability and high distribution in kidney tissues in pharmacokinetic studies in mice. Ferroptosis-IN-12 holds promise for research in the field of acute kidney injury (AKI) .
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- HY-N0528R
-
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TNF Receptor
Cholinesterase (ChE)
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Neurological Disease
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|
Linarin (Standard) is the analytical standard of Linarin. This product is intended for research and analytical applications. Linarin (Buddleoside), isolated from the flower extract of Mentha arvensis, shows selective dose dependent inhibitory effect on acetylcholinesterase (AChE) .
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- HY-149010
-
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Keap1-Nrf2
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Neurological Disease
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|
NXPZ-2 is an orally active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with a Ki value of 95 nM, EC50 value of 120 and 170 nM. NXPZ-2 can dose-dependently ameliorate Aβ[1-42]-Induced cognitive dysfunction, improve brain tissue pathological changes in Alzheimer’s disease (AD) mouse by increasing neuron quantity and function. NXPZ-2 can inhibit oxidative stress by increasing Nrf2 expression levels and promoting its cytoplasm to nuclear translocation, which is helpful for Keap1-Nrf2 PPI inhibitors and AD associated disease research .
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-
- HY-169103
-
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NO Synthase
COX
Cholinesterase (ChE)
Amyloid-β
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Neurological Disease
Inflammation/Immunology
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Neuroprotective agent 5 (compound 28) is a brain permeabilizing agent with anti-neuritis, anti-oxidative damage and neuroprotective effects. Neuroprotective agent 5 exhibits a potent NO inhibitory effect (EC50=0.49 μM), inhibits the release of proinflammatory factors PGE2 and TNF-α, downregulates the expression of iNOS and COX-2 proteins, and promotes the polarization of BV-2 cells from the proinflammatory M1 phenotype to the anti-inflammatory M2 phenotype. In addition, Neuroprotective agent 5 can also inhibit acetylcholinesterase (AChE) activity and Aβ42 aggregation in a dose-dependent manner. Neuroprotective agent 5 can be used for the study of Alzheimer's disease .
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- HY-124547R
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Endogenous Metabolite
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Others
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2,4-D methyl ester (Standard) is the analytical standard of 2,4-D methyl ester. This product is intended for research and analytical applications. 2,4-D methyl ester is a bioactive compound with the activity of promoting the accumulation of nutritional and medicinal components. 2,4-D methyl ester can be used to enhance the production of bioactive components in Cordyceps militaris. 2,4-D methyl ester showed an inductive effect on bioactive components at specific concentrations. The application of 2,4-D methyl ester provides an effective strategy to improve the fruit quality of Cordyceps militaris. 2,4-D methyl ester, as a biostimulant, can induce dose-dependent responses in different components .
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- HY-124726
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Autophagy
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Neurological Disease
Cancer
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|
Aumitin is a diaminopyrimidine-based autophagy inhibitor which inhibits mitochondrial respiration by targeting complex I. Aumitin inhibits starvation- and rapamycin induced autophagy dose dependently with IC50s of 0.12 μM and 0.24 μM, respectively .
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-
- HY-113953
-
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Caspase
Apoptosis
|
Inflammation/Immunology
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|
Z-Asp-CH2-DCB is an irreversible broad spectrum caspase inhibitor. Z-Asp-CH2-DCB also inhibits proteases with caspase-like activity. Z-D-CH2-DCB blocks the production of IL-1β, TNF-α, IL-6, and IFN-γ in staphylococcal enterotoxin B (SEB)-stimulated peripheral blood mononuclear cells (PBMC), and reduces SEB-1-stimulated T-cell proliferation in a dose-dependent manner. Z-Asp-CH2-DCB prevents SU5416-induced septal cell apoptosis and emphysema development .
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- HY-143494
-
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RSV
Influenza Virus
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Infection
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|
RSV/IAV-IN-3 (compound 14'i) is a dual inhibitor of respiratory syncytial virus (RSV) and influenza A virus (IAV) with EC50 values of 2.92 µM and 1.90 µM,respectively. RSV/IAV-IN-3 has antiviral effect against H1N1 and H3N2 with EC50 values of 3.25 µM and 1.50 µM in MDCK cells, respectively. RSV/IAV-IN-3 significantly inhibits the activity of luciferase in a dose-dependent manner, with an EC50 of 3.89 µM. RSV/IAV-IN-3 inhibits IAV infectivity and RdRp activity. RSV/IAV-IN-3 inhibits IAV and RSV replication at the post-entry stage .
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-
- HY-147862
-
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EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-62 (compound 9h) is a potent and reversible EGFR kinase inhibitor, with IC50 values of 10 nM (L858R/T790 M), 29 nM (WT), and 242 nM (L858R/T790 M/C797S), respectively. EGFR-IN-62 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.53 and 1.56 μM, respectively. EGFR-IN-62 induces dose-dependent apoptosis process, G1/G0-phase arrestation, and the inhibition of motility on A549 and/or H1975 cell lines .
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- HY-126638
-
|
NSC 324645
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Parasite
|
Infection
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|
Marcfortine A is an indole alkaloid originally isolated from P. roqueforti. It has nematocidal activity against the parasitic nematode H. contortus (LD99=0.06 μg/mL) and inhibits motility of adult worms (EC50=2 μM). Marcfortine A eliminates H. contortus, T. colubriformis, and O. ostertagi from experimentally infected jirds (ED95s=0.33, 0.11, and 2.5 mg/animal, respectively). It dose-dependently inhibits nicotine-induced calcium mobilization in SH-SY5Y and TE-671 cells expressing α3 subunit-containing human nicotinic acetylcholine receptors (nAChRs) and muscle-type nAChRs, respectively.
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- HY-130229
-
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(±)5,6-DiHETrE lactone
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Others
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Cardiovascular Disease
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|
5,6-DiHET lactone ((±)5,6-DiHETrE lactone) is a lactonized form of 5,6-EET and 5,6-DiHET. In solution, 5(6)-EET degrades into 5(6)-DiHET and 5(6)-δ-lactone, which can be converted to 5(6)-DiHET and quantified by GC-MS.1 5,6-DiHET potently induces vasodilation of isolated canine coronary arterioles, with 41 and 100% inhibition occurring at 0.01 and 100 pM, respectively. It also induces vasodilation in isolated human microvessels and increases intracellular calcium levels in a dose-dependent manner, an effect that can be blocked by the nitric oxide scavenger L-NAME.
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-
- HY-12193
-
|
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Histamine Receptor
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Others
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|
A-349821 is a histamine H3 receptor antagonist characterized as a radioligand ([3H]-A-349821) for in vivo receptor occupancy assessment. In rats, [3H]-A-349821 penetrated the brain, showing higher levels in the cortex compared to the cerebellum, indicating selective H3 receptor binding. Its cortical occupancy was saturable, correlating with in vitro binding data. Inhibition studies with ABT-239 and other H3 antagonists showed dose-dependent reductions in receptor occupancy, matching blood levels associated with cognitive efficacy in preclinical models. [3H]-A-349821 thus serves as a valid tracer for H3 receptor occupancy, aiding in the development and clinical interpretation of H3 receptor antagonists .
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-
- HY-117921
-
|
|
Others
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Inflammation/Immunology
|
|
DA-E 5090 is an orally effective inhibitor of IL-1 production that can be converted into a pharmacologically active deacetylated form (DA-E5090) in vivo. In this study, the effects of DA-E5090 on IL-1 production in vitro were examined by LPS-stimulated human monocytes. The results showed that DA-E5090 could dose-dependently inhibit the production of IL-1α and IL-1β (1-10 μM) by LPS-stimulated human monocytes, as determined by LAF assay and ELISA. Northern blotting analysis showed that DA-E5090 inhibited the transcription of IL-1α and IL-1β mRNA.
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- HY-N6954R
-
|
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ATM/ATR
STAT
CDK
|
Cancer
|
|
Garcinone C (Standard) is the analytical standard of Garcinone C. This product is intended for research and analytical applications. Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia that is used as an anti-inflammatory, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, while efficiently inhibiting the expression levels of cyclin B1, cyclin D1, cyclin E2, cdc2, Stat3 and CDK7. Garcinone C significantly inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time? and dose?dependent manner .
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-
- HY-169006
-
|
|
Apoptosis
PKC
|
Cancer
|
|
Evo312 is a dose-dependent inhibitor of protein kinase CβⅠ (PKCβⅠ) (IC50 is 117.34 nM). Evo312 induces PANC-GR (acquired gemcitabine-resistant PC cells) cell cycle arrest and apoptosis by inhibiting PKCβ1 protein expression. Evo312 has antiproliferative effects in pancreatic cancer cells PANC-1 and PANC-GR cells with IC50 of 0.08 μM and 0.07 μM, and in human normal pancreatic ductal epithelial cells HPDE6-c7 with IC50 of 2.95 μM. Evo312 exhibits antitumor activity in a PANC-GR cell transplantation mouse model .
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-
- HY-117578
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
KB 5666 is a benzoxazine derivative with lipid peroxidation inhibitory activity. KB 5666 showed protective effects against post-ischemic neuronal death. KB 5666 effectively protected CA1 neurons when injected 5 minutes before or immediately after ischemia. KB 5666 also showed a dose-dependent protective effect when injected within 1 hour after ischemia. KB 5666 effectively prevented the significant decrease in microtubule-associated protein 2 immunoreactivity within the dendritic field of CA1 pyramidal cells. KB 5666 prevented the decrease in [3H]PDBu binding activity in different layers of the CA1 region after ischemia. The application of KB 5666 showed the ability to improve the cellular and functional consequences of ischemia .
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-
- HY-167939
-
|
|
Others
|
Inflammation/Immunology
|
|
(R)-Bambuterol is a β2-receptor agonist with anti-asthmatic and colitis-improving activity. (R)-Bambuterol is indicated for the treatment of asthma and chronic obstructive pulmonary disease and has the advantage of a once-daily dosing and a favorable side effect profile. (R)-Bambuterol significantly reduced disease severity in a mouse model of colitis, more effectively than (RS)-Bambuterol or (S)-Bambuterol. (R)-Bambuterol can significantly reduce the levels of inflammatory cytokines and reduce the infiltration of macrophages in mice with colitis. (R)-Bambuterol also increases β2-adrenoceptor levels and reduces the expression of IL-6, IL-17 and other related proteins in colon tissue in a dose-dependent manner .
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-
- HY-159945
-
|
|
Amyloid-β
α-synuclein
|
Neurological Disease
|
|
Tau Protein/α-synuclein-IN-2 (Compound 14T) is a blood-brain barrier penetrating tau and α-syn inhibitor. Through its thiourea linker structure, Tau Protein/α-synuclein-IN-2 dose-dependently reduces α-syn oligomerization. In biosensor cells, Tau Protein/α-synuclein-IN-2 prevents the seeding effect of tau aggregation. In the M17D neuroblastoma model, Tau Protein/α-synuclein-IN-2 exhibits anti-inclusion effects. Additionally, Tau Protein/α-synuclein-IN-2 reduces Aβ plaque formation. Tau Protein/α-synuclein-IN-2 holds promise for Alzheimer's disease and Parkinson's disease research.
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-
- HY-16074
-
ATN-224
3 Publications Verification
Bis(choline)tetrathiomolybdate
|
SOD
|
Cancer
|
|
ATN-224 is an oral Cu 2+/Zn 2+-superoxide dismutase 1 (SOD1) inhibitor. ATN-224 inhibits SOD1 activity in endothelial cells, an effect that is dose dependent with an IC50 of 17.5±3.7 nM.
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-
- HY-N5045
-
|
|
Others
|
Inflammation/Immunology
|
|
Jionoside A1 isolated from Radix Rehmanniae Praeparata displays dose dependent immune-enhancement activity and possesses moderate protective activities on H2O2-treated SH-SY5Y cells .
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-
- HY-144668
-
|
|
Influenza Virus
|
Infection
|
|
RdRP-IN-4 (compound 11q), an aryl benzoyl hydrazide analog, is an orally active influenza A virus RNA-dependent RNA polymerase (RdRp) inhibitor by interacting with the PB1 subunit. RdRP-IN-4 exhibits potent inhibitory activity against the avian H5N1 flu strain with an EC50 of 18 nM in MDCK cells. RdRP-IN-4 displays excellent potency against the the H1N1 (A/PR/8/34) Flu A strain and Flu B strain (B/Lee/1940) with EC50 values of 53 nM and 20 nM, respectively. RdRP-IN-4 significantly inhibits the expression level of viral nucleoprotein (NP) in a dose-dependent manner. RdRP-IN-4 exhibits significant antiviral activity in infected mice .
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-
- HY-155297
-
|
FLA-136
|
Histamine Receptor
|
Cardiovascular Disease
|
|
Nebidrazine is a centrally-acting hypotensive agent compared to clonidine, demonstrating weaker cardiovascular effects in rats. It induces dose-dependent hypotension and bradycardia when administered intracerebroventricularly (i.c.v.), with significantly lower sedative potential than clonidine in conscious rats. Yohimbine attenuates the cardiovascular effects of both Nebidrazine and clonidine, suggesting involvement of central alpha-autoreceptors sensitive to yohimbine. Unlike clonidine, Nebidrazine does not affect peripheral alpha-adrenoceptors in pithed rats, indicating a selective central mechanism. Chemical sympathectomy reduces Nebidrazine's cardiovascular effects more than clonidine's, and metiamide diminishes responses to both drugs, implicating central histamine receptors. These findings highlight Nebidrazine's distinct pharmacological profile and potential therapeutic application in managing hypertension through central alpha-autoreceptor stimulation .
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-
- HY-138232
-
|
LTNAM
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Others
|
Neurological Disease
|
|
Lys-psi(CH2NH)-Trp(Nps)-OMe is a lysine-tryptophan (Nps) pseudodipeptide analog. It is obtained by replacing the peptide bond in the Lys-Trp(Nps) molecule with an aminomethylene bond and has analgesic activity. Lys-psi(CH2NH)-Trp(Nps)-OMe induces a dose-dependent and naloxone-reversible analgesia after intracerebroventricular administration in mice, and its analgesic effect lasts longer than that of the original compound. It protects methionine enkephalin from degradation in rat striatal slices and binds to low-dose opioid peptides to produce analgesia. Lys-psi(CH2NH)-Trp(Nps)-OMe effectively inhibits brain aminopeptidase activity both in vitro and in vivo. The enhanced resistance of this pseudodipeptide to proteolysis may explain its prolonged analgesic activity.
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-
- HY-116062A
-
|
|
Histone Methyltransferase
|
Neurological Disease
|
|
JNJ-7925476 is a triple reuptake inhibitor that selectively and potently inhibits the activity of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). JNJ-7925476 is rapidly absorbed into the blood and its concentration in the brain is 7-fold higher than that in plasma. The occupancy ED(50) values of JNJ-7925476 for SERT, NET, and DAT in the rat brain are 0.18, 0.09, and 2.4 mg/kg, respectively. JNJ-7925476 rapidly induces a significant increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex in a dose-dependent manner. JNJ-7925476 exhibits potent antidepressant-like activity in the mouse tail suspension test. These results suggest that JNJ-7925476 has in vivo efficacy in biochemical and behavioral models of depression .
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-
- HY-106200
-
|
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Lipoxygenase
|
Inflammation/Immunology
|
|
CJ-13,610, a nonredox-type 5-LO inhibitor, dose dependently suppresses 5-LO product formation in ionophore A23187-stimulated PMNL in the absence of exogenous AA with an IC50 of about 70 nM . PMNL: polymorphonuclear leukocytes; AA: arachidonic acid
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-
- HY-152524
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 7 is an effective androgen receptor (AR) antagonist with an IC50 value of 1.18 µM. Androgen receptor antagonist 7 has biological activity in vitro and inhibits the expression of AR target in a time and dose dependent manner with an GI50 value of 7.9 µM .
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-
- HY-129421
-
|
|
PACAP Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
PA-9 is a pituitary adenylate cyclase-activating polypeptide (PACAP) type I (PAC1) receptor antagonist. PA-9 dose dependently inhibits PACAP-induced cAMP elevation with an IC50 of 5.6 nM. PA-9 can be used for the research of neuropathic and/or inflammatory pain .
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-
- HY-144132
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
αβ-Tubulin-IN-1 is a potent and orally active αβ-Tubulin inhibitor. αβ-Tubulin-IN-1 induces cell cycle arrest at G2/M and efficient apoptosis. αβ-Tubulin-IN-1 inhibits tumor cell migration and Metastasis. αβ-Tubulin-IN-1 shows significant antitumor efficacy in a dose dependent manner .
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-
- HY-139342
-
|
|
CDK
|
Cancer
|
|
CDK7-IN-4 (compound I) is a potent CDK7 (Cyclin-dependent kinase 7) inhibitor. CDK7-IN-4 shows anticancer activity. CDK7-IN-4 inhibits the in vitro growth of cancer cell lines from a variety of histologies including colon , breast , lung , ovary and stomach , in a dose dependent manner .
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-
- HY-15616
-
|
|
Melanocortin Receptor
|
Cancer
|
|
BMS-470539 is a synthetic MC-1R agonist with potent anti-inflammatory properties. BMS-470539 selectively activates human and murine MC-1R with EC50 values ??of 16.8 nM and 11.6 nM, respectively. In vitro studies have shown that BMS-470539 is able to dose-dependently inhibit TNF-alpha-induced NF-kB activation in human melanoma cells expressing MC-1R. In vivo, subcutaneous injection of BMS-470539 into BALB/c mice effectively inhibited LPS-induced TNF-alpha production with an ED50 of approximately 10 μmol/kg and a pharmacodynamic half-life of approximately 8 hours. It also significantly reduced leukocyte infiltration in a lung inflammation model and attenuated paw swelling in a delayed-type hypersensitivity model, highlighting its efficacy as an anti-inflammatory agent through MC-1R modulation .
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-
- HY-19471
-
|
|
Others
|
Cancer
|
|
(rac)-ZK-304709 is an isomer of ZK-304709. It is a first-in-class oral multi-target tumor growth inhibitor that inhibits multiple cell cycle-dependent kinases (Cdks), vascular endothelial growth factor receptor kinases (VEGF-RTKs), and platelet-derived growth factor receptor kinase β (PDGF-RTKβ). (rac)-ZK-304709 can dose-dependently inhibit the proliferation and colony formation of neuroendocrine tumor (NET) cells. It directly acts on NET cells by inducing G2 cell cycle arrest and apoptosis, while reducing the expression of MCL1, survivin, and HIF1α. In an orthotopic BON tumor model, (rac)-ZK-304709 reduced primary tumor growth by 80% and reduced tumor microvascular density. These results suggest that (rac)-ZK-304709 can effectively control tumor growth by inducing apoptosis and inhibiting tumor-induced angiogenesis, and may be a potential agent for the treatment of NET.
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-
- HY-111137
-
|
XC-302 free base
|
Akt
|
Cancer
|
|
Puquitinib (XC-302 free base) is a multi-target inhibitor with the activity of inducing autophagy in nasopharyngeal carcinoma cells by inhibiting the PI3K/AKT/mTOR signaling pathway. Puquitinib was able to inhibit the proliferation of CNE-2 cells, showing a dose-dependent antiproliferative effect. Puquitinib induced the formation of autophagosomes and autolysosomes in CNE-2 cells, which were observed by fluorescence microscopy and electron microscopy. Puquitinib promoted the formation of LC3-II and increased the expression of beclin 1, while reducing the level of p62. Puquitinib inhibited the PI3K/AKT/mTOR pathway by reducing the expression of p-AKT and p-mTOR. Puquitinib also induced apoptosis in CNE-2 cells, and when autophagy was inhibited, the apoptosis rate was reduced, which means that autophagy may interact with apoptosis to induce cell death .
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-
- HY-111527
-
|
|
Others
|
Neurological Disease
|
|
PPZ2 is a diacylglycerol (DAG)-activated TRPC3/TRPC6/TRPC7 channel activator with activity in promoting neuronal development and survival. PPZ2 activates recombinant TRPC3/TRPC6/TRPC7 channels in a dose-dependent manner without affecting other TRPC channels. PPZ2 elicits cation currents and calcium ion (Ca(2+)) influx in cultured central neurons. PPZ2 is able to induce BDNF-like neurite outgrowth and neuroprotection, an effect that disappears after TRPC3/TRPC6/TRPC7 knockdown or inhibition. PPZ2 also increases the activation of the calcium-dependent transcription factor cAMP response element binding protein. The effects of PPZ2 suggest that calcium signaling mediated by activation of DAG-activated TRPC channels plays an important role in its neurotrophic effects .
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-
- HY-159941
-
|
|
Tau Protein
α-synuclein
Amyloid-β
|
Neurological Disease
|
|
tau-0N4R-IN-1 (Compound 6T) is an BBB-penetrable inhibitor of tau 0N4R oligomerization. tau-0N4R-IN-1 effectively inhibits the fibrosis of tau 0N4R, 2N3R, and 2N4R, exhibits an anti-seeding effect on tau in vitro, reduces the oligomerization of α-syn dose-dependently, and prevents formation of α-syn inclusions. tau-0N4R-IN-1 is stable in mouse microsomes and reduces Aβ plaques in brain tissues from AD patients. tau-0N4R-IN-1 has good pharmacokinetic properties in mice .
|
-
- HY-122720
-
|
KL-1
|
Apoptosis
|
Cancer
|
|
SEC inhibitor KL-1 (KL-1) is a peptide-like lead compound that is an effective selective SEC inhibitor. SEC inhibitor KL-1 promotes apoptosis and has anti-tumor activity. SEC inhibitor KL-1 doses dependently inhibits the AFF4-CCNT1 interaction, with a Ki value of 3.48 μM .
|
-
- HY-145865
-
|
|
Apoptosis
|
Cancer
|
|
Antiproliferative against-3 (comp 33) shows a prominent activity against Hela (IC50 = 0.21 µM), A549 (IC50 = 0.39 µM), and MCF-7 (IC50 = 0.33 µM), respectively. Antiproliferative against-3 (comp 33) also dose dependently induces apoptosis by arresting A549 cells at G1 phase .
|
-
- HY-144731
-
|
|
HIV
|
Inflammation/Immunology
|
|
gp120-IN-2 (compound 4i) is a potent HIV-1 gp120 inhibitor with an IC50 of 7.5 µM and CC50 of 112.93 µM. gp120-IN-2 shows anti-HIV-1 activity. gp120-IN-2 shows cytotoxicity in a dose dependent manner in SUP-T1 cells .
|
-
- HY-111140
-
|
|
PGE synthase
Lipoxygenase
|
Inflammation/Immunology
|
|
YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC50=3.4 μM) and 5-lipoxygenase (5-LOX; IC50=6.5 μM). YS121 dose- dependently reduces PGE2 production with EC50=12 μM in IL-1β-stimulated A549 cells .
|
-
- HY-P0262
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Galantide, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide appears to bind to a single population of SP receptors (KD~40 nM) .
|
-
- HY-N9541
-
|
|
Others
|
Inflammation/Immunology
|
|
Chaetoglobosin Vb is a novel cytotoxic alkaloid with anti-inflammatory and antioxidant activities. Chaetoglobosin Vb can inhibit oxidative stress induced by LPS stimulation, reduce the production of reactive oxygen species and increase the expression of the antioxidant enzyme superoxide dismutase (SOD). Chaetoglobosin Vb significantly reduced the gene and protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) induced by LPS, and alleviated the production of proinflammatory cytokines such as TNF-α, IL-6 and IL-1β. Chaetoglobosin Vb exerts its biological activity through the TLR4-mediated MyD88-dependent signaling pathway and the TRIF-dependent signaling pathway, which is specifically manifested by inhibiting the phosphorylation of p38, ERK, and JNK MAPK and the translocation of NF-κB p65 subunit to the nucleus. Chaetoglobosin Vb showed no cytotoxic effect in the concentration range of 25-100 μM and promoted SOD enzyme activity and phosphorylation of p38, ERK1/2 and JNK in a dose-dependent manner .
|
-
- HY-137055
-
|
|
Others
|
Others
|
|
PF-3774076 is a highly central nervous system (CNS) penetrant, potent, and selective human α1A-adrenoceptor partial agonist. It exhibits good potency and selectivity in multiple binding and functional assays. PF-3774076 increases peak urethral pressure in anesthetized female dogs in a dose-dependent manner via a central mechanism. PF-3774076 affects both the proximal and distal portions of the urethra in vivo. These properties suggest that PF-3774076 may have significant benefit in the treatment of stress urinary incontinence (SUI) as a CNS-penetrant α1A receptor partial agonist. However, despite its partial agonism and selectivity for α1A receptors, PF-3774076 failed to provide adequate safety differences in in vivo models of cardiovascular function. This may be due to the simultaneous activation of both peripheral and central α1A receptors. These data suggest that while central α1A partial agonists may have significant benefit in the treatment of SUI, this class of agents may have difficulty achieving the desired urethral selectivity without affecting cardiovascular function.
|
-
- HY-144730
-
|
|
HIV
|
Inflammation/Immunology
|
|
gp120-IN-1 (compound 4e) is a potent HIV-1 gp120 inhibitor with an IC50 of 2.2 µM and CC50 of 100.90 µM. gp120-IN-1 shows anti-HIV-1 activity. gp120-IN-1 shows cytotoxicity in a dose dependent manner in SUP-T1 cells. gp120-IN-1 shows inhibition of gp120-mediated virus enter into cells .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-137131
-
|
DC-Cholesterol hydrochloride
|
Drug Delivery
|
|
DC-Chol hydrochloride could inhibit Aβ40 fibril formation under appropriate experimental conditions. DC-Chol hydrochloride strongly inhibits amyloidogenesis of oxidized hCT in a dose-dependent manner .
|
-
- HY-W127334
-
|
|
Biochemical Assay Reagents
|
|
N-Palmitoyl phosphatidylethanolamine (Tripelargonin) is endogenous lipid anorectic hormone, significantly reduces food intake in a dose-dependent manner
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-107627
-
|
|
Melanocortin Receptor
|
Inflammation/Immunology
|
|
MCL0020 is a potent and selective melanocortin MC4 receptor antagonist, with an IC50 of 11.63 nM. MCL0020 dose-dependently and significantly attenuates restraint stress-induced anorexia without affecting food intake .
|
-
- HY-P3030
-
|
|
Peptides
|
Inflammation/Immunology
|
|
CPN-219, a next-generation hexapeptidic NMUR2 agonist, achieves a dose-dependent and selective activation of NMUR2 with an EC50 value of 2.2 nM .
|
-
- HY-P3462A
-
|
|
CGRP Receptor
|
Metabolic Disease
|
|
Cagrilintide acetate is a non-selective AMYR/CTR agonist and long-acting acylated amylase analogue. Cagrilintide acetate causes a reduction in food intake and significant weight loss in a dose-dependent manner. Cagrilintide acetate can be used in obesity studies .
|
-
- HY-P1235A
-
|
Atrial Natriuretic Peptide (ANP) (1-28), human, porcine acetate
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Carperitide acetate (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine acetate) is a 28-amino acid hormone, that is normally produced and secreted by the human heart in response to cardiac injury and mechanical stretch. Carperitide acetate inhibits endothelin-1 secretion in a dose-dependent way.
|
-
- HY-P3730
-
|
|
CDK
|
Cancer
|
|
Cdk2/Cyclin Inhibitory Peptide I (Tat-LFG), a CDK2 inhibitor, kills U2OS osteosarcoma cells in a dose-dependent manner .
|
-
- HY-P5921
-
|
TsTx-Kα
|
Peptides
|
Neurological Disease
|
|
Tityustoxin-Kα (TsTx-Kα) is an inhibitor of potassium voltage-gated channels. Tityustoxin-Kα shows a dose-dependent block of the sustained outward current in cultured hippocampal neurons .
|
-
- HY-P1086
-
|
|
Peptides
|
Others
|
|
Cadherin Peptide, avian is a calcium-dependent glycoprotein. Cadherin Peptide, avian takes part in homophilic cell-cell adhesion and dose-dependently inhibits bovine brain microvessel endothelial cells (BBMECs) adhesion .
|
-
- HY-P4663
-
|
NSC 350591
|
Peptides
|
Cancer
|
|
Val-Gly-Ser-Glu (NSC 350591) is an ECF-A tetrapeptide. Val-Gly-Ser-Glu dose-dependently increases the number of human eosinophils, but not neutrophils, rosetting with complement-coated sheep erythrocytes (EAC3b) .
|
-
- HY-P10032
-
-
- HY-P2005
-
|
|
Peptides
|
Others
|
|
Malformin C is an algicidal peptide can be isolated from Aspergillus and exhibits dose-dependent algicidal activity. Malformin C induces a significant increase in ROS levels in algal cells, resulting in impaired SOD activity and high production of MDA content .
|
-
- HY-P1329
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity .
|
-
- HY-P5859
-
|
α-PMTX
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
α-Pompilidotoxin (α-PMTX) is a neurotoxin that can be obtained from the venom of Anoplius safnariensis. α-Pompilidotoxin reversibly and dose-dependently enhances excitatory postsynaptic currents (EPSCs). α-Pompilidotoxin is a useful tool in the field of neuroscience research .
|
-
- HY-P3100
-
|
|
Parasite
|
Infection
|
|
Orfamide A is a major metabolite of insecticidal biosurfactant in Pseudomonas sp. F6 and has aphidicidal activity. Orfamide A can be used for aphid control in organic agriculture. Orfamide A exhibits dose-dependent mortality against aphids with an LC50 value of 34.5 μg/mL .
|
-
- HY-P1329A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity .
|
-
- HY-P0262A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
Metabolic Disease
|
|
Galantide TFA is a reversible and non-specific galanin (GAL) receptor antagonist. Galantide TFA dose-dependently shows antagonism to galanin-induced K + conductance with an IC50 value of 4 nM. Galantide TFA can be used for the research of neurological disease and hormone metabolism research .
|
-
- HY-P10032A
-
-
- HY-P2082
-
|
|
Peptides
|
Others
|
|
[D-pGlu1,D-Phe2,D-NaI3,6]-Gn-RH is a gonadotropin-releasing hormone (Gn-RH) agonist that has a dose-dependent inhibitory activity on progesterone secretion from cultured human granulosa cells.
|
-
- HY-P1257
-
|
|
Peptides
|
Metabolic Disease
|
|
Xenin-8, a C-terminal octapeptide, is a biologically active fragment of Xenin. Xenin is a 25-amino acid peptide of the neurotensin/xenopsin family. Xenin-8 stimulates basal insulin secretion and potentiates the insulin response to glucose in a dose-dependent manner (EC50=0.16 nM) .
|
-
- HY-P10517
-
|
SFT
|
HIV
|
Infection
|
|
Sifuvirtide (SFT) is a potent HIV fusion inhibitor. Sifuvirtide inhibits HIV-1 mediated cell fusion in a dose-dependent manner and is highly potent against infection by primary and laboratory-adapted HIV-1 isolates of multiple genotypes. Sifuvirtide can be used in the research of anti-HIV drugs .
|
-
- HY-P2080
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
GIP (1-30) amide,human is a glucose-dependent insulinotropic polypeptide (GIP) fragment. GIP is an incretin hormone that stimulates insulin secretion and reduces postprandial glycaemic excursions. GIP (1-30) amide,human dose-dependently promotes insulin secretion over the range 10 -9-10 -6 M .
|
-
- HY-P2080B
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
GIP (1-30) amide,human acetate is a glucose-dependent insulinotropic polypeptide (GIP) fragment. GIP is an incretin hormone that stimulates insulin secretion and reduces postprandial glycaemic excursions. GIP (1-30) amide,human acetate dose-dependently promotes insulin secretion over the range 10 -9-10 -6 M .
|
-
- HY-P1440A
-
|
|
Potassium Channel
|
Neurological Disease
|
|
BeKm-1 TFA is a potent and selective KV11.1 (hERG) channel blocker. BeKm-1 TFA is selective for KV11.1 over a panel of 14 other potassium channels. BeKm-1 TFA dose-dependently prolongs QTc interval in isolated rabbit heart.
|
-
- HY-P1235
-
|
Atrial Natriuretic Peptide (ANP) (1-28), human, porcine
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Carperitide (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine) is a 28-amino acid hormone, that is normally produced and secreted by the human heart in response to cardiac injury and mechanical stretch. Carperitide (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine) inhibits endothelin-1 secretion in a dose-dependent way.
|
-
- HY-P1257A
-
|
|
Peptides
|
Metabolic Disease
|
|
Xenin-8 TFA, a C-terminal octapeptide, is a biologically active fragment of Xenin. Xenin is a 25-amino acid peptide of the neurotensin/xenopsin family. Xenin-8 TFA stimulates basal insulin secretion and potentiates the insulin response to glucose in a dose-dependent manner (EC50=0.16 nM) .
|
-
- HY-P10571
-
|
|
Melanocortin Receptor
|
Endocrinology
|
|
GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC50=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R .
|
-
- HY-P2080C
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
GIP (1-30)-Myr is the Myr-modified GIP (1-30), which is a glucose-dependent insulinotropic polypeptide (GIP) fragment. GIP is an incretin hormone that stimulates insulin secretion and reduces postprandial glycaemic excursions. GIP (1-30) dose-dependently promotes insulin secretion over the range 10 -9-10 -6 M .
|
-
- HY-P10710
-
|
|
IFNAR
Interleukin Related
COX
|
Inflammation/Immunology
|
|
BMP-4 is a penetrating heparin-binding peptide with anti-inflammatory and anti-chondrogenic functions. In murine chondrocytes and macrophages, BMP-4 regulates the iNOS-IFN-IL6 signaling pathway to inhibit the expression of inflammatory proteins such as iNOS, COX2, IFN, and IL6 in a dose-dependent manner, effectively suppressing inflammation and alleviating various arthritis symptoms .
|
-
- HY-P10228
-
|
|
Fungal
Bacterial
|
Infection
|
|
S-Thanatin is an insect antimicrobial peptide with potent broad-spectrum antibacterial activity. S-Thanatin can inhibit the activity of Gram-negative bacteria, Gram-positive bacteria, and fungi, without cytotoxicity. The antibacterial activity of S-Thanatin is not affected by PH value, but monovalent cations (Na +/K +) can reduce its antibacterial activity against Gram-negative bacteria in a dose-dependent manner .
|
-
- HY-P4641
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
H-Trp-Phe-OH is a dipeptide consisting of tryptophan and phenylalanine (Trp-Phe). H-Trp-Phe-OH is also an antihypertensive peptide with inhibitory activity on angiotensin-converting enzyme (ACE), dose-dependently increases NO levels, and decreases endothelin-1 (ET-1) levels. H-Trp-Phe-OH (2 mg/kg; subcutaneous injection; 6 injections over 3 days) causes an increase in ovarian weight in female mice .
|
-
- HY-P4984
-
|
|
Biochemical Assay Reagents
|
Inflammation/Immunology
Cancer
|
|
Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) is a T cell proliferation activator. Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) promotes the in vitro proliferation of human peripheral blood mononuclear cells (PBMC) in a dose-dependent manner. Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78) can be used in research on inflammatory and immunity, as well as cancer .
|
-
- HY-P10711
-
|
|
Autophagy
|
Cancer
|
|
ALA-A2 is an anticancer peptide discovered in alpha-lactalbumin that selectively kills cancer cells by inducing Autophagy. ALA-A2 has cell-penetrating capabilities, allowing it to effectively enter cells without relying on membranolytic effects. In A549 lung cancer cells, ALA-A2 demonstrates significant dose-dependent anticancer activity. ALA-A2 holds promise for research in cancer therapy and autophagy regulation .
|
-
- HY-P0249
-
-
- HY-P0249B
-
-
- HY-P4121
-
|
|
Peptides
|
Metabolic Disease
|
|
L17E, an endosomolytic peptide, is a cationic amphiphilic peptide with specific membrane lytic activity for late endosomes (LEs). L17E diminishes the TS5-p45 induced apoptosis in a dose-dependent manner. L17E is endocytosed into cells and trafficked to LEs. Within the acidic environment of LEs, L17E perturbs and lyses the LE membrane, leading to disruption of LE membrane and release of LE content to the cytosol. L17E is used to investigate the role of the endosomal protein trafficking pathway .
|
-
- HY-W007223
-
|
D-5-HTP; 5-Hydroxy-D-tryptophan
|
5-HT Receptor
|
Neurological Disease
|
|
D-5-Hydroxytryptophan (D-5-HTP) is the D-isomer of 5-HTP and can be isolated from DL-5-hydroxytryptophan by continuous separation. Compared with intraperitoneal administration of L-5-Hydroxytryptophan, which can induce dose-dependent backward walking behavior in mice, D-5-Hydroxytryptophan has no significant effect on mouse behavior and is a negative control. D-5-Hydroxytryptophan is also a 5-HT ligand, capable of binding to the 5-HT site with affinity in the micromolar range .
|
-
- HY-P5900
-
|
m3-HwTx-IV
|
Sodium Channel
|
Neurological Disease
|
|
m3-Huwentoxin IV (m3-HwTx-IV) is a potent NaV inhibitor with IC50s of 3.3, 6.8, 7.2, 8.4, 11.9 and 369 nM against hNaV1.7, hNaV1.6, hNaV1.3, hNaV1.1, hNaV1.2 and hNaV1.4, respectively in QPatch assay. m3-Huwentoxin IV dose-dependently suppresses spontaneous pain induced by the NaV1.7 activator OD1 in a rodent pain model .
|
-
- 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-P0262
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Galantide, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide appears to bind to a single population of SP receptors (KD~40 nM) .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N5099
-
-
-
- HY-N0775
-
-
-
- HY-N11922
-
-
-
- HY-N8816
-
-
-
- HY-B0163
-
-
-
- HY-N6621
-
-
-
- HY-N1159
-
-
-
- HY-N11950
-
-
-
- HY-N2383
-
|
(1R,2S,3S,4S,6R)-4-Amino-6-(hydroxymethyl)cyclohexane-1,2,3-triol
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
|
Glycosidase
|
|
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-107164
-
-
-
- HY-12956B
-
-
-
- HY-N6621A
-
-
-
- HY-N6681
-
-
-
- HY-N5060
-
-
-
- HY-121377
-
-
-
- HY-W042191
-
-
-
- HY-P2005
-
-
-
- HY-N4209
-
-
-
- HY-N0775R
-
-
-
- HY-116498
-
|
|
Microorganisms
Source classification
|
Others
|
|
Penigequinolone A is an alkaloid isolated from Penicillium. It is lethal to P. penetrans (LD50=100 mg/L) but has no effect on C. elegans at concentrations up to 1000 mg/L.1 Penigequinolone A also accelerates the root growth of rice seedlings in a dose-dependent manner.
|
-
-
- HY-N11911
-
-
-
- HY-N5054
-
-
-
- HY-B0094
-
-
-
- HY-N5060R
-
-
-
- HY-N0262
-
-
-
- HY-N7934
-
-
-
- HY-N6745
-
-
-
- HY-N0092R
-
|
|
Structural Classification
Natural Products
Human Gut Microbiota Metabolites
Microorganisms
Source classification
Endogenous metabolite
|
Adenosine Receptor
Endogenous Metabolite
|
Inosine (Standard) is the analytical standard of Inosine. This product is intended for research and analytical applications. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors . In Vitro:Inosine dose-dependently stimulates cAMP production mediated through the A2AR .
Inosine dose-dependently induces hA2AR-mediated ERK1/2 phosphorylation .
Inosine (100 μM; 24 hours) reduces oxidative stress in MES 23.5 cells cultured with astrocytes .
In Vivo:Inosine (10-100 mg/kg; i.p.) exhibits antinociceptive effect in mice .
|
-
-
- HY-N3734
-
-
-
- HY-142088
-
-
-
- HY-125396
-
-
-
- HY-N12481
-
-
-
- HY-W008820R
-
|
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Disease markers
Endocrine diseases
Nervous System Disorder
Endogenous metabolite
|
Endogenous Metabolite
|
|
Glutaric acid (Standard) is the analytical standard of Glutaric acid. This product is intended for research and analytical applications. Glutaric acid, C5 dicarboxylic acid, is an intermediate during the catabolic pathways of lysine and tryptophan. Glutaric acid affects pericyte contractility and migration. Glutaric acid is an indicator of glutaric aciduria type I .
In Vitro: Glutaric acid (GA) at concentrations of 1 and 2 mM is able to reduce TRAP measurement by up to 28% in a dose-dependent manner (β=0.77; P<0.001). Furthermore, a significantly inverse correlation is also verified between chemiluminescence and TRAP (β=0.81; P<0.001). Glutaric acid does not alter the activities of Cat and SOD, but strongly inhibits (up to 46%) the activity of GPx even at the lower concentration used (0.5 mM). It is observed that the metabolite inhibits this activity in a dose-dependent manner at concentrations as low as 0.05 mM .
|
-
-
- HY-N2252
-
-
-
- HY-B0094R
-
-
-
- HY-N0262R
-
-
-
- HY-N3504
-
-
-
- HY-N0407
-
-
-
- HY-N0241
-
-
-
- HY-N13739
-
|
|
Structural Classification
Terpenoids
Sesquiterpenes
Source classification
Asteraceae
Taraxacum coreanum Nakai
Plants
|
Tyrosinase
|
|
Taraxinic acid can be found in the roots of Taraxacum flavostylum and Taraxacum lucidum. It is a Tyrosinase inhibitor that dose-dependently inhibits Tyrosinase activity, showing approximately 54.5% inhibition at a concentration of 50 μg/mL. Taraxinic acid has an IC50 of 83.2 μM against melanoma cells A375 and HTB140, and an IC50 of 60.4 μM against melanoma cells WM793, with activity being both dose- and time-dependent. Taraxinic acid holds promise for research in the field of anticancer therapy .
|
-
-
- HY-N9182
-
-
-
- HY-N11910
-
-
-
- HY-N0528
-
-
-
- HY-N0407R
-
|
|
Structural Classification
Iridoids
Terpenoids
Source classification
Scrophulariaceae
Plants
Picrorhiza scrophulariiflora Pennell
|
STAT
|
|
Picroside I (Standard) is the analytical standard of Picroside I. This product is intended for research and analytical applications. Picroside I is the major ingredient of Picrorhiza scrophulariiflora. Picrorhiza scrophulariiflora is a high value medicinal herb due to rich source of hepatoprotective metabolites, Picroside-I and Picroside-II . Picroside I is a promising agent for the management of asthma. Picroside I reduces the inflammation significantly at its higher dose. Picroside I also downregulates pSTAT6 and GATA3 expressions. Picroside I dose-dependently increases the serum levels of IFN-γ .
|
-
-
- HY-N10439
-
-
-
- HY-112650
-
-
-
- HY-N6954
-
|
|
Structural Classification
other families
Xanthones
Classification of Application Fields
Garcinia oblongifolia Champ. ex Benth.
Guttiferae
Source classification
Phenols
Polyphenols
Plants
Disease Research Fields
Cancer
|
ATM/ATR
STAT
CDK
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Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia that is used as an anti-inflammatory, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, while efficiently inhibiting the expression levels of cyclin B1, cyclin D1, cyclin E2, cdc2, Stat3 and CDK7. Garcinone C significantly inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner .
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- HY-N7210
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Structural Classification
Natural Products
Source classification
Rubiaceae
Plants
Coffea arabica L.
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Apoptosis
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Kahweol acetate, a bioactive compound found in coffee, has been identified for its potent anti-cancer properties, particularly in inhibiting the proliferation and migration of prostate cancer cells. Alongside cafestol, it shows dose-dependent effects in suppressing tumor growth and metastasis in both in vitro and in vivo studies. Mechanistically, kahweol acetate and cafestol induce apoptosis, inhibit epithelial-mesenchymal transition, and reduce androgen receptor activity, especially in androgen receptor-positive cells. They also downregulate chemokine receptors CCR2 and CCR5, crucial for cancer progression, without altering their ligand levels. These findings suggest that kahweol acetate, in combination with cafestol, may serve as promising therapeutic agents against prostate cancer .
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- HY-N0528R
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- HY-126638
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NSC 324645
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Human Gut Microbiota Metabolites
Microorganisms
Source classification
Endogenous metabolite
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Parasite
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Marcfortine A is an indole alkaloid originally isolated from P. roqueforti. It has nematocidal activity against the parasitic nematode H. contortus (LD99=0.06 μg/mL) and inhibits motility of adult worms (EC50=2 μM). Marcfortine A eliminates H. contortus, T. colubriformis, and O. ostertagi from experimentally infected jirds (ED95s=0.33, 0.11, and 2.5 mg/animal, respectively). It dose-dependently inhibits nicotine-induced calcium mobilization in SH-SY5Y and TE-671 cells expressing α3 subunit-containing human nicotinic acetylcholine receptors (nAChRs) and muscle-type nAChRs, respectively.
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- HY-N6954R
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Structural Classification
other families
Xanthones
Garcinia oblongifolia Champ. ex Benth.
Guttiferae
Source classification
Phenols
Polyphenols
Plants
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ATM/ATR
STAT
CDK
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Garcinone C (Standard) is the analytical standard of Garcinone C. This product is intended for research and analytical applications. Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia that is used as an anti-inflammatory, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, while efficiently inhibiting the expression levels of cyclin B1, cyclin D1, cyclin E2, cdc2, Stat3 and CDK7. Garcinone C significantly inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time? and dose?dependent manner .
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- HY-N5045
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- HY-N9541
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Structural Classification
Alkaloids
Microorganisms
Pyrrole Alkaloids
Source classification
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Others
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Chaetoglobosin Vb is a novel cytotoxic alkaloid with anti-inflammatory and antioxidant activities. Chaetoglobosin Vb can inhibit oxidative stress induced by LPS stimulation, reduce the production of reactive oxygen species and increase the expression of the antioxidant enzyme superoxide dismutase (SOD). Chaetoglobosin Vb significantly reduced the gene and protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) induced by LPS, and alleviated the production of proinflammatory cytokines such as TNF-α, IL-6 and IL-1β. Chaetoglobosin Vb exerts its biological activity through the TLR4-mediated MyD88-dependent signaling pathway and the TRIF-dependent signaling pathway, which is specifically manifested by inhibiting the phosphorylation of p38, ERK, and JNK MAPK and the translocation of NF-κB p65 subunit to the nucleus. Chaetoglobosin Vb showed no cytotoxic effect in the concentration range of 25-100 μM and promoted SOD enzyme activity and phosphorylation of p38, ERK1/2 and JNK in a dose-dependent manner .
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Product Name |
Chemical Structure |
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- HY-157029S
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KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-157031S
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KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-B0006S1
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Carvedilol-d4 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker[1]. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome[3].
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- HY-121356S1
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Carebastine-d5 Methyl Ester is the deuterium labeled Carebastine. Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner[1]. Carebastine suppresses the expression of macrophage migration inhibitory factor[2].
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- HY-121356S
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Carebastine-d5 is the deuterium labeled Carebastine. Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner[1]. Carebastine suppresses the expression of macrophage migration inhibitory factor[2].
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- HY-W013576S
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Methyl 2-Octynoate-d5 is deuterated labeled Estragole (HY-N5060). Estragole (4-Allylanisole), a relatively nontoxic volatile terpenoid ether, is a major component of the essential oil of many plants. Estragole dose-dependently blocks nerve excitability . Estragole displays anti-toxoplasma activity .
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- HY-B0094S
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Artemisinin-d3 is the deuterium labeled Artemisinin. Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants[1]. Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects[2].
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- HY-B0162S
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Ivabradine-d6 is the deuterium labeled Ivabradine[1]. Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity[2][3][4][5].
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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-B0006S
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Carvedilol-d3 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker[1]. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome[3].
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- HY-B0006S2
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Carvedilol-d5 is deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker[1]. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome[3].
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- HY-B0094S3
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Artemisinin- 13C,d4 is 13C and deuterated labeled Artemisinin (HY-B0094). Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .
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- HY-W015912S
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2-Acetylfuran-d3 is deuterated labeled Citreoviridin (HY-N6745). Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na +/K +-ATPase whereas in microsomes, both Na +/K +-ATPase and Mg 2+-ATPase activities are significantly stimulated in a dose-dependent manner . Citreoviridin inhibits cell proliferation and enhances apoptosis of human umbilical vein endothelial cells .
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- HY-113439S
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12-HETE-d8 is the deuterium labeled 12-HETE. 12-HETE, a major metabolic product of arachidonic acid using 12-LOX catalysis, inhibits cell apoptosis in a dose-dependent manner. 12-HETE promotes the activation and nuclear translocation of NF-κB through the integrin-linked kinase (ILK) pathway[1].12-HETE has both anti-thrombotic and pro-thrombotic effects[2]. 12-HETE is a neuromodulator[3].
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| Cat. No. |
Product Name |
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Classification |
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- HY-157029S
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Alkynes
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KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-157031S
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Alkynes
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KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-129737
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Azide
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A-62198 is a potent and selective renin inhibitor with antihypertensive activity. A-62198 reduces mean arterial pressure (MAP) in anesthetized, salt-deprived monkeys in a dose-dependent manner. A-62198 induced MAP reduction in normal monkeys that reached statistical significance at the highest dose and significantly inhibited plasma renin activity (PRA) at all doses .
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| Cat. No. |
Product Name |
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Classification |
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- HY-137131
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DC-Cholesterol hydrochloride
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Cholesterol
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DC-Chol hydrochloride could inhibit Aβ40 fibril formation under appropriate experimental conditions. DC-Chol hydrochloride strongly inhibits amyloidogenesis of oxidized hCT in a dose-dependent manner .
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- HY-130345
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Phospholipids
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C18-PAF, octadecane PAF, is the ligand of platelet-activating factor and PAF G protein-coupled receptor (PAFR). C18-PAF has renovasodilator properties and antihypertensive lipid properties. C18-PAF increases renal blood flow and causes dose-dependent systemic hypotension .
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- HY-150739A
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CpG ODNs
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ODN 21158 sodium is a potent G-modified TLR3 and TLR9 inhibitor. ODN 21158 sodium inhibits IFN-α secretion in a dose dependent manner .
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- HY-150739
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CpG ODNs
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ODN 21158 is a potent G-modified TLR3 and TLR9 inhibitor. ODN 21158 shows no cytotoxic. ODN 21158 inhibits IFN-α secretion in a dose dependent manner .
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