Search Result
Results for "
versus
" in MedChemExpress (MCE) Product Catalog:
4
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P99452
-
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SNDX-6352
|
c-Fms
|
Inflammation/Immunology
Cancer
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Axatilimab (SNDX-6352) is a humanized IgG4 antibody with high affinity to CSF-1R. Axatilimab can be used for the research of chronic graft versus host disease (cGVHD) and neoplastic diseases .
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-
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- HY-14873
-
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BG 9928
|
Adenosine Receptor
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Cardiovascular Disease
Metabolic Disease
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Tonapofylline (BG 9928) is an orally active and selective adenosine A1 receptor antagonist with a Ki of 7.4 nM for human adenosine A1 receptor (hA1), which displays 915-fold selectivity versus human adenosine A2A receptor and 12-fold selectivity versus human adenosine A2B receptor and is used in development for the treatment of heart failure .
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-
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- HY-18172
-
-
-
- HY-10401
-
-
-
- HY-119996A
-
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Monocarboxylate Transporter
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Inflammation/Immunology
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AR-C141990 hydrochloride is a potent lactate transporters (monocarboxylate transporters; MCTs) inhibitor with pKi values of 7.6, 6.6 for MCT-1 and MCT-2, respectively . AR-C141990 hydrochloride has immunosuppressive properties and inhibits graft versus host response .
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-
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- HY-144648
-
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SARS-CoV
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Infection
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Mpro/PLpro-IN-1 (Compound 29) is a potent inhibitor of M pro/PL pro. Mpro/PLpro-IN-1 is a dual acting SARS-CoV-2 proteases inhibitor featuring micromolar inhibitory potency versus M pro (IC50 = 1.72 μM) and submicromolar potency versus PL pro (IC50 = 0.67 μM) .
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- HY-106851
-
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FG 10571; PNU 78875
|
GABA Receptor
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Neurological Disease
|
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Panadiplon (FG 10571; PNU 78875), a benzodiazepine receptor, is a 5GABAA partial agonist. Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors .
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-
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- HY-156414
-
-
-
- HY-145995
-
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Others
|
Others
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CS12192 is a compound improving survival and weight gain. CS12192 has the potential for the research of graft-versus-host disease (GVHD) (extracted from the patent CN112773802A) .
|
-
-
- HY-18172A
-
|
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Potassium Channel
|
Neurological Disease
|
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(+)-KCC2 blocker 1 is a selective K +-Cl - cotransporter KCC2 blocker with an IC50 of 0.4 μM. (+)-KCC2 blocker 1 is a benzyl prolinate and a enantiomer of KCC2 blocker 1 .
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-
-
- HY-10302
-
|
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CGRP Receptor
|
Neurological Disease
|
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MK-3207 (Hydrochloride) is a potent and orally bioavailable CGRP receptor antagonist with IC50 of 0.12 nM and Ki of 0.024 nM, and is highly selective versus human AM1, AM2, CTR, and AMY3.
|
-
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- HY-10963
-
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CYT387 mesylate
|
JAK
Autophagy
|
Cancer
|
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Momelotinib mesylate (CYT387 mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.
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-
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- HY-12019
-
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c-Met/HGFR
|
Cancer
|
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SGX523 is a exquisitely selective and ATP-competitive MET inhibitor. SGX523 potently inhibits MET with an IC50 of 4 nM and is >1,000-fold selective versus other protein kinases. Antitumor activity .
|
-
-
- HY-116097
-
|
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Monoamine Oxidase
|
Neurological Disease
|
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PSB-1491 is a selective and competitive monoamine oxidase B (MAO-B) inhibitor with an IC50 of 0.386 nM for hMAO-B. PSB-1491 shows >25000-fold selective versus MAO-A .
|
-
-
- HY-116770
-
PFM01
1 Publications Verification
|
Endonuclease
|
Cancer
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PFM01, N-alkylated Mirin derivative, is a MRE11 endonuclease inhibitor. PFM01 can regulate double-strand break repair (DSBR) by nonhomologous end-joining (NHEJ) versus homologous recombination (HR) .
|
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- HY-100397
-
|
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Elastase
|
Inflammation/Immunology
|
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Elastatinal is a potent and competitive inhibitor of elastase, with a Ki of 0.21 μM. Elastatinal more potently inhibits pancreatic elastase versus leucocyte elastase. Elastatinal shows no activity on human leucocyte chymotrypsin-like protease .
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- HY-P99664
-
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Interleukin Related
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Inflammation/Immunology
|
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Inolimomab is an anti-interleukin-2 receptor (IL-2R) α chain monoclonal antibody. Inolimomab improves the survival rate in the early research of treating acute graft-versus-host disease (aGVHD) .
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- HY-10962
-
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CYT387 sulfate salt
|
JAK
Autophagy
Apoptosis
|
Cancer
|
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Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM).
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- HY-117554
-
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HDAC
|
Cancer
|
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BRD9757 is a potent, capless and selective HDAC6 inhibitor with an IC50 of 30 nM. BRD9757 shows excellent selectivity toward HDAC6 versus the class I (>20-fold) and class II (>400-fold) HDACs .
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- HY-106278
-
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PPAR
|
Metabolic Disease
|
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GW 590735 is a potent and selective PPARα agonist. GW 590735 showsEC50=4 nM on PPARα and at least 500-fold selectivity versus PPARδ and PPARγ. GW 590735 can be used for the research of dyslipidemia .
|
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- HY-19414
-
|
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Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
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MLN-4760 is a potent and selective human ACE2 inhibitor (IC50, 0.44 nM), with excellent selectivity (>5000-fold) versus related enzymes including human testicular ACE (IC50, >100 μM) and bovine carboxypeptidase A (CPDA; IC50, 27 μM).
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-
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- HY-119934
-
|
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Sodium Channel
|
Neurological Disease
|
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NaV1.7 inhibitor-1 is an efficacious voltage-gated sodium channel (NaV) 1.7 inhibitor with an IC50 of 0.6 nM for hNaV1.7, exhibits 80-fold selectivity versus hNaV1.5 .
|
-
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- HY-50859
-
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INCB018424 sulfate
|
JAK
Autophagy
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Cancer
|
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Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3.
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-
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- HY-153398
-
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Phosphodiesterase (PDE)
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Infection
Cancer
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Enpp-1-IN-17 (example 274) is a potent ENPP1 inhibitor, with the inhibition constants (Ki values) toward cGAMP and ATP hydrolysis of 100 nM-1 μM and > 1 μM, respectively. The selectivity ratio for inhibition of cGAMP hydrolysis versus ATP hydrolysis is >6.4 .
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-
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- HY-W027631
-
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Others
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Infection
|
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cis-2-Butene-1,4-diol, an industrial product, can be used for the synthesis of antiviral product oxetanocin A. cis-2-Butene-1,4-diol is a probe for studying isomerization versus hydrogenation and hydrogenolysis reactions .
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-
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- HY-111372A
-
|
(Rac)-BAY 94-8862
|
Mineralocorticoid Receptor
|
Cardiovascular Disease
|
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(Rac)-Finerenone ((Rac)-BAY 94-8862) is the racemate of Finerenone. Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold) .
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-
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- HY-P99378
-
|
ALTB-168; Anti-PSGL1/CD162 Reference Antibody (neihulizumab)
|
Apoptosis
|
Inflammation/Immunology
|
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Neihulizumab (ALTB-168) is an immune checkpoint agonistic antibody that binds to human CD162 (PSGL-1), leading to downregulation of activated T-cells. Neihulizumab can be uesd for steroid-refractory acute graft-versus-host-disease (SR-aGVHD), psoriasis, psoriatic arthritis and ulcerative colitis research .
|
-
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- HY-162618
-
|
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Cannabinoid Receptor
|
Neurological Disease
|
|
PSB-KK1445 is a potent and selective GPR18 agonist with EC50s of 45.4 nM and 124 nM for human and mouse GPR18, respectively. PSB-KK1445 displays >200-fold selectivity versus both CB receptor subtypes, GPR55, and GPR183 .
|
-
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- HY-P99837
-
|
SPV-T3a
|
CD3
|
Infection
|
|
Dafsolimab (SPV-T3a) is an IgG2a murine monoclonal antibody (anti-CD3). Dafsolimab can induce cell death through modulation and activation of the CD3/T cell receptor complex. Dafsolimab can be used for the research of graft-versus-host disease (GVHD) .
|
-
-
- HY-10044
-
|
WYE-125132
|
mTOR
Apoptosis
|
Cancer
|
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WYE-132 (WYE-125132) is a highly potent, ATP-competitive, and specific mTOR kinase inhibitor (IC50: 0.19±0.07 nM; >5,000-fold selective versus PI3Ks). WYE-132 (WYE-125132) inhibits mTORC1 and mTORC2.
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-
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- HY-N2554
-
|
Ostenol
|
Monoamine Oxidase
|
Neurological Disease
|
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Osthenol (Ostenol), a prenylated coumarin isolated from the dried roots of Angelica pubescens, is selective, reversible, and competitive human monoamine oxidase-A (hMAO-A) inhibitor (Ki=0.26 µM). Osthenol potently inhibits recombinant hMAO-A with an IC50 of 0.74 µM and shows a high selectivity index for hMAO-A versus hMAO-B .
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- HY-103407A
-
|
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Dopamine Receptor
|
Neurological Disease
Cancer
|
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PD 168568 dihydrochloride is a orally active and potent dopamine receptor D4 (DRD4) antagonist. PD 168568 dihydrochloride contains an isoindolinone and is selective for the D4 receptor versus D2 and D3, with Ki values of 8.8, 1842, and 2682 nM, respectively. PD 168568 dihydrochloride can be used for glioblastoma (GBM) research .
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- HY-132932
-
|
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Calcium Channel
|
Others
|
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Cavα2δ-IN-1 shows high selectivity for voltage-gated calcium channels Cavα2δ-1 (Ki 6 nM) versus Cavα2δ-2 (Ki ＞ 10000 nM).
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-
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- HY-103407
-
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Dopamine Receptor
|
Neurological Disease
Cancer
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PD 168568 is a orally active and potent dopamine receptor D4 (DRD4) antagonist. PD 168568 contains an isoindolinone and is selective for the D4 receptor versus D2 and D3, with Ki values of 8.8, 1842, and 2682 nM, respectively. PD 168568 can be used for glioblastoma (GBM) research .
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-
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- HY-124037
-
|
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Sirtuin
|
Cancer
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SRT 1460, a potent Sirtuin-1 (SIRT1) activator with an EC1.5 value of 2.9 μM, shows good selectivity for activation of SIRT1 versus SIRT2 and SIRT3 (EC1.5>300 μM), and is more potent than Resveratrol and the closest sirtuin homologues .
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-
- HY-116830
-
BRD0705
1 Publications Verification
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GSK-3
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Cancer
|
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BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) research .
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- HY-110092A
-
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P2Y Receptor
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Cancer
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PSB-1114 triethylamine is a potent, enzymatically stable, and subtype-selective P2Y2 receptor agonist with an EC50 of 134 nM. PSB-1114 triethylamine displays >50-fold selectivity versus the P2Y4 (EC50 of 9.3 μM) and P2Y6 (EC50 of 7.0 μM) receptors .
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- HY-15610
-
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RG 7421; MEK inhibitor 1
|
MEK
Apoptosis
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Cancer
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GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAF V600E, EC50=7 nM).
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- HY-111925
-
|
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TRP Channel
|
Cardiovascular Disease
|
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BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7 .
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-
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- HY-110092
-
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P2Y Receptor
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Metabolic Disease
|
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PSB-1114 tetrasodium is a potent, enzymatically stable, and subtype-selective P2Y2 receptor agonist with an EC50 of 134 nM. PSB-1114 tetrasodium displays >50-fold selectivity versus the P2Y4 (EC50 of 9.3 μM) and P2Y6 (EC50 of 7.0 μM) receptors .
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-
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- HY-W484263
-
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NO Synthase
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Neurological Disease
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hnNOS-IN-3 (compound 39) is a selective nNOS inhibitor, with a Ki of 0.32 μM. The nNOS binding of hnNOS-IN-3 is competitive with L-arginine. The selectivity of hnNOS-IN-3 for nNOS versus iNOS (Ki=37 μM) and eNOS (Ki=9.4 μM) is 115-fold and 29-fold, respectively .
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-
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- HY-10260
-
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ZD6474
|
VEGFR
Autophagy
Apoptosis
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Cancer
|
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Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
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- HY-10260B
-
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ZD6474 hydrochloride
|
VEGFR
Autophagy
Apoptosis
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Cancer
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Vandetanib hydrochloride (D6474 hydrochloride) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib hydrochloride also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
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- HY-10260A
-
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ZD6474 trifluoroacetate
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VEGFR
Autophagy
Apoptosis
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Cancer
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Vandetanib trifluoroacetate (D6474 trifluoroacetate) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib trifluoroacetate also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
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- HY-124179
-
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NF-κB
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Cancer
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IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor with an IC50 of 0.1 μM, 3 μM for NF-κB DNA binding and c-Rel DNA binding, respectively. IT-901, a bioactive naphthalenethiobarbiturate derivative, has the potential for human lymphoid tumors and ameliorate graft-versus-host disease (GVHD) .
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-
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- HY-W007524
-
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2-Quinolinamine
|
NO Synthase
Orthopoxvirus
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Infection
Neurological Disease
|
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2-Aminoquinoline (2-Quinolinamine) is a promising compound as bioavailable nNOS inhibitor but suffers from low human nNOS inhibition, low selectivity versus human eNOS, and significant binding to other CNS targets. 2-Aminoquinoline exhibits antiviral activity against the vaccinia virus. 2-Aminoquinoline has the potential for the research of antineurodegenerative agents .
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-
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- HY-13643
-
|
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Histone Demethylase
|
Cancer
|
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Daminozide, a plant growth regulator, is a selective inhibitor of the human KDM2/7 histone demethylases, with IC50s of 0.55, 1.5 and 2.1 μM for PHF8, KDM2A, and KIAA1718, respectively. Daminozide has >100-fold selectivity for KDM2/7 subfamily versus other demethylase subfamily members tested .
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-
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- HY-101588
-
|
MK-7264; AF-219
|
P2X Receptor
|
Inflammation/Immunology
|
|
Gefapixant is an orally active and potent purinergic P2X3 receptor (P2X3R) antagonist, with IC50 values of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. Gefapixant can be used for the research of chronic cough and knee osteoarthritis .
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-
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- HY-101517
-
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PI3K
|
Cancer
|
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PI3K-IN-2 (compound 10) is a potent and orally active PI3Kβ/δ (IC50=7.1/8.6 nM) inhibitor with excellent selectivity versus PI3Kσ and PI3Kγ (IC50=13/190 nM, respectively) .
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-
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- HY-18173
-
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11β-HSD
|
Metabolic Disease
|
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AZD8329 is a potent 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 9 nM for human 11β-HSD1, displays excellent selectivity versus 11β-HSD2, 17β-HSD1 and 17β-HSD3 .
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-
- HY-111372
-
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BAY 94-8862
|
Mineralocorticoid Receptor
|
Cardiovascular Disease
|
|
Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
|
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- HY-12439
-
ML380
1 Publications Verification
|
mAChR
|
Neurological Disease
|
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ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR .
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- HY-106345
-
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FKBP
Calcium Channel
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Neurological Disease
Inflammation/Immunology
|
|
ILS-920 is a nonimmunosuppressive Rapamycin analog with reduced immunosuppressive activity and potent neuroprotective activity. ILS-920 binds selectively to the immunophilin FKBP52 and to the β1-subunit of L-type voltage-gated calcium channels (VGCC). ILS-920 shows 200-fold selectivity for FKBP52 versus FKBP12 .
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- HY-121508
-
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NF-κB
|
Inflammation/Immunology
Cancer
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(E/Z)-IT-603 is a mixture of E-IT-603 and Z-IT-603 (IT-603). IT-603 is a c-Rel inhibitor with an IC50 of 3 μM. IT-603 has anti-tumor activity. (E/Z)-IT-603 is a promising modulator of T-cell responses in the context of graft-versus-host disease (GVHD) and malignant diseases .
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-
- HY-P99445
-
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APG101; CAN008
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TNF Receptor
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Inflammation/Immunology
Cancer
|
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Asunercept (APG101; CAN008) is a soluble CD95-Fc fusion protein targeting CD95L. Asunercept disrupts CD95/CD95L signaling by selectively binding to CD95L. Asunercept can be used in the research of glioblastoma multiforme (GBM), myelodysplastic syndrome (MDS), and graft-versus-host disease (GvHD) .
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- HY-16689
-
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Potassium Channel
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Others
|
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VU 0240551 is a potent neuronal K-Cl cotransporter KCC2 inhibitor (IC50=560 nM) and is selective versus NKCC1. VU 0240551 also inhibits hERG and L-type Ca 2+ channels. VU 0240551 attenuates GABA-induced hyperpolarization of P cells, produces a positive shift in the P cell GABA reversal potential and enhances P cell synaptic transmission .
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- HY-116830A
-
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GSK-3
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Cancer
|
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(Rac)-BRD0705 is a less active racemate of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) .
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- HY-100971
-
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AMI-193
|
5-HT Receptor
Dopamine Receptor
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Neurological Disease
|
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Spiramide (AMI-193) is a potent and selective antagonist of 5-HT2 and dopamine D2 receptor, with Kis of 2 nM and 3 nM, respectively. Spiramide has >2000-fold selectivity for 5-HT2 versus 5-HT1C (Ki=4300 nM) receptors. Spiramide exhibits antipsychotic activity .
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- HY-114015
-
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Ser/Thr Protease
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Cancer
|
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APC-6860 is a trypsin-like serine proteases inhibitor with ki values of 0.21 and 0.44 μM for uPA and trypsin, respectively. APC-6860 has a selectivity ratio for tPA versus uPA of 80. APC-6860 has ki values of 0.1 and 0.082 μM for human and murine urokinases, respectively. APC-6860 can be used for the research of cancer .
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- HY-101588A
-
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MK-7264 citrate; AF-219 citrate
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P2X Receptor
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Inflammation/Immunology
|
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Gefapixant citrate is an orally active and potent purinergic P2X3 receptor (P2X3R) antagonist, with IC50 values of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. Gefapixant citrate can be used for the research of chronic cough and knee osteoarthritis .
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- HY-155193
-
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Others
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Inflammation/Immunology
|
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XY-52 (Compound 32) is a Stimulation-2 (ST2) inhibitor, with an IC50 value of 5.68 μM in AlphaLISA assay, and 4.59 μM in HEK-Blue assay. XY-52 increases proinflammatory T-cell proliferation. XY-52 reduces the plasma sST2 and IFNγ biomarkers in the graft versus host disease (GVHD) mice model .
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-
- HY-105064D
-
|
CP-597396 hydrochloride hydrate
|
Na+/H+ Exchanger (NHE)
|
Cardiovascular Disease
|
|
Zoniporide (CP-597396) hydrochloride hydrate is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride hydrate inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride hydrate potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM) .
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-
- HY-116830B
-
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(R)-BRD0705
|
GSK-3
|
Cancer
|
|
BRD5648 ((R)-BRD0705) is a negative control of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) .
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-
- HY-105064B
-
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CP-597396 hydrochloride
|
Na+/H+ Exchanger (NHE)
|
Cardiovascular Disease
|
|
Zoniporide (CP-597396) hydrochloride is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM) .
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-
- HY-131328
-
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LOXO-305
|
Btk
|
Cancer
|
|
Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM .
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- HY-158014
-
|
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Dopamine Transporter
|
Neurological Disease
|
|
JJC8-089 is a dopamine transporter (DAT) inhibitor that may improve motivational dysfunction and increase effortful behavior in goal-directed activities. JJC8-089 significantly reversed the low-effort effects induced by the VMAT-2 inhibitor Tetrabenazine (HY-B0590) in rats and increased the choice of high-effort fixed-ratio 5-bar presses versus food intake. .
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-
- HY-12076
-
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BMS 817378
|
c-Met/HGFR
TAM Receptor
|
Cancer
|
|
BMS 777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively, and 40-fold more selective for Met-related targets than Lck, VEGFR-2, and TrkA/B, with more than 500-fold greater selectivity versus all other receptor and non receptor kinases .
|
-
- HY-122001
-
|
|
Sodium Channel
|
Neurological Disease
|
|
PF-05186462 is a potent and selective inhibitor of human Nav1.7 voltage-dependent sodium channel, with an IC50 of 21 nM. PF-05186462 shows significant selectivity for Nav1.7 versus other sodium channels (Nav 1.1, 1.2, 1.3, 1.4, 1.5, 1.6, and 1.8). PF-05186462 can be used for the research of acute or chronic pain .
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-
- HY-101588R
-
|
|
P2X Receptor
|
Inflammation/Immunology
|
|
Gefapixant (Standard) is the analytical standard of Gefapixant. This product is intended for research and analytical applications. Gefapixant is an orally active and potent purinergic P2X3 receptor (P2X3R) antagonist, with IC50 values of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. Gefapixant can be used for the research of chronic cough and knee osteoarthritis .
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- HY-10260R
-
|
|
VEGFR
Autophagy
Apoptosis
|
Cancer
|
|
Vandetanib (Standard) is the analytical standard of Vandetanib. This product is intended for research and analytical applications. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
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- HY-111372R
-
|
|
Mineralocorticoid Receptor
|
Cardiovascular Disease
|
|
Finerenone (Standard) is the analytical standard of Finerenone. This product is intended for research and analytical applications. Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
|
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- HY-101562
-
|
GDC-0077; RG6114
|
PI3K
Apoptosis
|
Cancer
|
|
Inavolisib (GDC-0077) is a potent, orally active, and selective PI3Kα inhibitor (IC50=0.038 nM). Inavolisib exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. Inavolisib is more selective for mutant versus wild-type PI3Kα. Inavolisib can be used for the study of breast cancer .
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- HY-10260S1
-
|
|
Isotope-Labeled Compounds
VEGFR
Autophagy
Apoptosis
|
Cancer
|
|
Vandetanib-d4 is the deuterium labeled Vandetanib. Vandetanib (ZD6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1][2].
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- HY-10260S
-
|
ZD6474-d6
|
Isotope-Labeled Compounds
VEGFR
Autophagy
Apoptosis
|
Cancer
|
|
Vandetanib-d6 is the deuterium labeled Vandetanib. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1].
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-
- HY-107732
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
JNJ-5207787 is a nonpeptidic, selective and penetrate the blood-brain barrier neuropeptide Y Y2 receptor (Y2) antagonist. JNJ-5207787 inhibits the binding of peptide YY (PYY) with pIC50s of 7.0 and 7.1 for human Y2 receptor and rat Y2 receptor, respectively. JNJ-5207787 is >100-fold selective versus human Y1, Y4, and Y5 receptors .
|
-
- HY-107479
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
(R)-JNJ-31020028 is a high affinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC50 values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively. (R)-JNJ-31020028 shows >100-fold selective versus human Y1, Y4, and Y5 receptors. (R)-JNJ-31020028 has antidepressant like effects .
|
-
- HY-18642
-
|
PF-4981517
|
Cytochrome P450
|
Others
|
|
CYP3cide (PF-4981517) is a potent, selective and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC50 values for Midazolam 1’-hydroxylase activity are 0.03 μM, 17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. CYP3cide can be used to distinguish the contributions of CYP3A4 versus CYP3A5 on agent metabolism .
|
-
- HY-111372S
-
|
BAY 94-8862-d3
|
Mineralocorticoid Receptor
|
Others
|
|
Finerenone-d3 is the deuterium labeled finerenone (HY-111372). Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
|
-
- HY-10260S2
-
|
ZD6474-13C6
|
Isotope-Labeled Compounds
VEGFR
Autophagy
Apoptosis
|
Cancer
|
|
Vandetanib-13C6 is a deuterated labeled Vandetanib . Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
|
-
- HY-13643R
-
|
|
Histone Demethylase
|
Cancer
|
|
Daminozide (Standard) is the analytical standard of Daminozide. This product is intended for research and analytical applications. Daminozide, a plant growth regulator, is a selective inhibitor of the human KDM2/7 histone demethylases, with IC50s of 0.55, 1.5 and 2.1 μM for PHF8, KDM2A, and KIAA1718, respectively. Daminozide has >100-fold selectivity for KDM2/7 subfamily versus other demethylase subfamily members tested .
|
-
- HY-164455
-
|
|
Aurora Kinase
JAK
STAT
|
Inflammation/Immunology
|
|
AJI-214 is a dual-target inhibitor of Aurora kinase A and JAK2. AJI-214 directly blocks Aurora kinase A to inhibit T cell mitotic progression and cell polarity, and inhibits JAK2 activation to inhibit STAT3 phosphorylation, thereby reducing the differentiation of TH1 and TH17 cells. AJI-214 can be used in studies on regulating immune responses and preventing graft-versus-host disease (GVHD) .
|
-
- HY-161305
-
|
|
HDAC
|
Metabolic Disease
Cancer
|
|
SE-7552, a 2-(difluoromethyl)-1,3,4-oxadiazole (DFMO) derivative, is an orally active, highly selective, non-hydroxamate HDAC6 inhibitor with an IC50 of 33 nM. SE-7552 is greater than 850-fold selectivity versus all other known HDAC isozymes. SE-7552 is capable of blocking multiple myeloma growth in vivo. SE-7552 acts as an anti-obesity agent in diet-induced obese mice .
|
-
- HY-164454
-
|
|
Aurora Kinase
JAK
STAT
|
Inflammation/Immunology
|
|
AJI-100 is a dual-target inhibitor of Aurora kinase A and JAK2 with IC50 values ??of 12.7 nM and 18.5 nM, respectively. AJI-100 directly blocks Aurora kinase A to inhibit T cell mitosis and cell polarity, and inhibits JAK2 activation to inhibit STAT3 phosphorylation, thereby reducing the differentiation of TH1 and TH17 cells. AJI-100 can be used in studies on regulating immune responses and preventing graft-versus-host disease (GVHD) .
|
-
- HY-126247
-
|
|
Ras
|
Cancer
|
|
BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
|
-
- HY-103637
-
|
VTP-43742
|
ROR
|
Inflammation/Immunology
|
|
Vimirogant (VTP-43742) is a potent, selective, and orally active RORγt inhibitor (Ki=3.5 nM; IC50=17 nM). Vimirogant exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant has the potential for autoimmune disorders research .
|
-
- HY-103637A
-
|
VTP-43742 hydrochloride
|
ROR
|
Inflammation/Immunology
|
|
Vimirogant (VTP-43742) hydrochloride is a potent, selective, and orally active RORγt inhibitor (Ki=3.5 nM; IC50=17 nM). Vimirogant hydrochloride exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant hydrochloride inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant hydrochloride has the potential for autoimmune disorders research .
|
-
- HY-111310
-
|
|
Lipoxygenase
|
Neurological Disease
Metabolic Disease
|
|
ML351 is a potent and highly specific 15-LOX-1 inhibitor with an IC50 of 200 nM. ML351 shows excellent selectivity (>250-fold) versus the related isozymes, 5-LOX, platelet 12-LOX, 15-LOX-2, ovine COX-1, and human COX-2 . ML351 prevents dysglycemia and reduces β-cell oxidative stress in nonobese diabetic mouse model of T1D .
|
-
- HY-126077
-
MTI-31
1 Publications Verification
LXI-15029
|
mTOR
|
Inflammation/Immunology
Cancer
|
|
MTI-31 (LXI-15029) is a potent, orally active and highly selective inhibitor of mTORC1 and mTORC2. MTI-31 is selective for mTOR (Kd: 0.20 nM) versus PIK3CA, PIK3CB and PIK3G with >5,000 fold selectivity in mTOR binding assays. MTI-31 shows an IC50 of 39 nM for mTOR in LANCE assay of mTOR substrate phosphorylation with 100 μM ATP. MTI-31 can be used for the research of breast cancer .
|
-
- HY-150298
-
|
CPI-818
|
Itk
|
Inflammation/Immunology
Cancer
|
|
Soquelitinib (CPI-818) is an orally active and highly selective covalent interleukin-2-inducible kinase (ITK) inhibitor. Soquelitinib is active in six different models of T cell-mediated inflammatory and immune disease, including acute and chronic asthma, pulmonary fibrosis, systemic sclerosis (scleroderma), psoriasis, and acute graft versus host disease with Th2 cytokine product inhibition. Soquelitinib increases tumor infiltration of normal CD8 + cells that possess enhanced T effector function .
|
-
- HY-13775
-
XL019
5 Publications Verification
|
JAK
Apoptosis
|
Cancer
|
|
XL019?is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2 .
|
-
- HY-124750
-
-
- HY-109041
-
|
AKB-9778
|
Phosphatase
Tie
|
Inflammation/Immunology
|
|
Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM) .
|
-
- HY-P99116
-
|
RG7716
|
VEGFR
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
Faricimab, an overall good safety and tolerability profile, is a bispecific antibody targeting Angiopoietin-2 (Ang-2) and vascular endothelial growth factor-A (VEGF-A). Faricimab prevents retinal vascular leakage, cell death and inflammation in retinal ischemia/reperfusion (I/R) injury and sCNV mouse models. Faricimab demonstrates statistically superior visual acuity gains versus Ranibizumab (HY-P9951). Faricimab can be used for retinal diseases, such as age-related macular degeneration (w-AMD), diabetic macular edema (DME) and macular edema following retinal vein occlusion (RVO) .
|
-
- HY-112825
-
|
|
Others
|
Inflammation/Immunology
|
|
Platelet-activating factor (PAF) is a pro-inflammatory phospholipid mediator that is rapidly synthesized by lyso-PAF acetyltransferase (lyso-PAFAT) in response to extracellular stimuli. Two types of lyso-PAFAT have been identified: lysophosphatidylcholine acyltransferase (LPCAT)1, which is mostly expressed in the lungs, and LPCAT2, which is expressed in inflammatory cells. TSI-01 is a selective inhibitor of LPCAT2 (IC50s=0.47 versus 3.02 μM for human LPCAT2 and LPCAT1, respectively). 60 μM it is shown to suppress PAF biosynthesis in mouse peritoneal macrophages stimulated with a calcium ionophore.
|
-
- HY-126247B
-
|
|
Others
|
Cancer
|
|
(R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P4667
-
|
|
Peptides
|
Metabolic Disease
|
|
VLHDDLLEA is a peptide that can be isolated from the MHC complex HLA-A*0201 molecule. VLHDDLLEA can be recognized by HLA-A*0201-restricted cytotoxic T cells (CTLs). VLHDDLLEA can be used for research on graft versus host disease (GvHD) .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99452
-
|
SNDX-6352
|
c-Fms
|
Inflammation/Immunology
Cancer
|
|
Axatilimab (SNDX-6352) is a humanized IgG4 antibody with high affinity to CSF-1R. Axatilimab can be used for the research of chronic graft versus host disease (cGVHD) and neoplastic diseases .
|
-
- HY-P99664
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
Inolimomab is an anti-interleukin-2 receptor (IL-2R) α chain monoclonal antibody. Inolimomab improves the survival rate in the early research of treating acute graft-versus-host disease (aGVHD) .
|
-
- HY-P99378
-
|
ALTB-168; Anti-PSGL1/CD162 Reference Antibody (neihulizumab)
|
Apoptosis
|
Inflammation/Immunology
|
|
Neihulizumab (ALTB-168) is an immune checkpoint agonistic antibody that binds to human CD162 (PSGL-1), leading to downregulation of activated T-cells. Neihulizumab can be uesd for steroid-refractory acute graft-versus-host-disease (SR-aGVHD), psoriasis, psoriatic arthritis and ulcerative colitis research .
|
-
- HY-P99445
-
|
APG101; CAN008
|
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
Asunercept (APG101; CAN008) is a soluble CD95-Fc fusion protein targeting CD95L. Asunercept disrupts CD95/CD95L signaling by selectively binding to CD95L. Asunercept can be used in the research of glioblastoma multiforme (GBM), myelodysplastic syndrome (MDS), and graft-versus-host disease (GvHD) .
|
-
- HY-P99116
-
|
RG7716
|
VEGFR
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
Faricimab, an overall good safety and tolerability profile, is a bispecific antibody targeting Angiopoietin-2 (Ang-2) and vascular endothelial growth factor-A (VEGF-A). Faricimab prevents retinal vascular leakage, cell death and inflammation in retinal ischemia/reperfusion (I/R) injury and sCNV mouse models. Faricimab demonstrates statistically superior visual acuity gains versus Ranibizumab (HY-P9951). Faricimab can be used for retinal diseases, such as age-related macular degeneration (w-AMD), diabetic macular edema (DME) and macular edema following retinal vein occlusion (RVO) .
|
-
- HY-P99636
-
|
ABX-CBL
|
Inhibitory Antibodies
|
Inflammation/Immunology
|
|
Gavilimomab (ABX-CBL) is an IgM murine monoclonal antibody that recognizes CD147 on the cell surface and initiates cell killing through complement-mediated lysis. Gavilimomab can be used for the research of graft-versus-host disease (GVHD) .
|
-
- HY-P99837
-
|
SPV-T3a
|
CD3
|
Infection
|
|
Dafsolimab (SPV-T3a) is an IgG2a murine monoclonal antibody (anti-CD3). Dafsolimab can induce cell death through modulation and activation of the CD3/T cell receptor complex. Dafsolimab can be used for the research of graft-versus-host disease (GVHD) .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-10260S1
-
|
|
|
Vandetanib-d4 is the deuterium labeled Vandetanib. Vandetanib (ZD6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1][2].
|
-
-
- HY-10260S
-
|
|
|
Vandetanib-d6 is the deuterium labeled Vandetanib. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1].
|
-
-
- HY-111372S
-
|
|
|
Finerenone-d3 is the deuterium labeled finerenone (HY-111372). Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
|
-
-
- HY-10260S2
-
|
|
|
Vandetanib-13C6 is a deuterated labeled Vandetanib . Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
|
-
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