Search Result
Results for "
Is Inhibitors
" in MedChemExpress (MCE) Product Catalog:
9965
Inhibitors & Agonists
20
Biochemical Assay Reagents
136
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-132595A
-
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QPI-1002 sodium
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MDM-2/p53
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Cancer
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Teprasiran sodium is a small interfering RNA that temporarily inhibits p53-mediated cell death that underlies acute kidney injury (AKI) .
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-
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- HY-B1890
-
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rel-Cianidanol; rel-Catechuic acid
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COX
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Infection
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
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(±)-Catechin (rel-Cianidanol) This is a green tea polyester. Catechin possesses anti-cancer activity, which has led to its demise. (±)-Catechin 具有两种forms (+)-Catechin and its reflection body (-)-Catechin. (+)-Catechin inhibitory environment-1 (COX-1) IC50 为 1.4 μM. (-)-Catechin has the effect of promoting hBM-MSC adipose cell differentiation, increasing adipose tissue, and PPARγ horizontal. (±)-Catechin has anti-diabetic, anti-hypertrophic, anti-diabetic, anti-cardiovascular, anti-infective, and liver-protecting effects.
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-
-
- HY-132595
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-
-
- HY-120944
-
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MMP
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Inflammation/Immunology
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BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively .
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-
-
- HY-155376
-
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mTOR
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Cancer
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mTOR inhibitor-14 (compound 14c) is a potent mTOR inhibitor. mTOR inhibitor-14 also shows minimal CYP2C8 inhibition. mTOR inhibitor-14 can inhibit tumor growth .
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-
-
- HY-162023
-
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mTOR
PI3K
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Cancer
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mTOR inhibitor-10 (Compound 9c) is a selective inhibitor for mTOR. mTOR inhibitor-10 inhibits mTOR and PI3K-α, with IC50 of 0.7 and 825 nM. mTOR inhibitor-10 inhibits proliferation of LNCaP with IC50 of 87 nM .
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-
-
- HY-162025
-
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mTOR
PI3K
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Cancer
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mTOR inhibitor-17 (Compound 9e) is a selective inhibitor for mTOR. mTOR inhibitor-10 inhibits mTOR and PI3K-α, with IC50 of 0.68 and 1359 nM. mTOR inhibitor-10 inhibits proliferation of LNCaP with IC50 of 40 nM .
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-
-
- HY-162024
-
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mTOR
PI3K
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Cancer
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mTOR inhibitor-16 (Compound 9f) is a selective inhibitor for mTOR. mTOR inhibitor-10 inhibits mTOR and PI3K-α, with IC50 of 1.25 and 82 nM. mTOR inhibitor-10 inhibits proliferation of LNCaP with IC50 of 140 nM .
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- HY-152191
-
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Apoptosis
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Cancer
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ChoKα inhibitor-3 is a sulphur-containing choline kinase inhibitor. ChoKα inhibitor-3 can inhibit HChoK α1 with an IC50 value of 0.66 μM. ChoKα inhibitor-3 also can induce apoptosis. ChoKα inhibitor-3 can be used for the research of cancer .
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-
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- HY-152195
-
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Apoptosis
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Cancer
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ChoKα inhibitor-5 is a sulphur-containing choline kinase inhibitor. ChoKα inhibitor-5 can inhibit HChoK α1 with an IC50 value of 0.64 μM. ChoKα inhibitor-5 also can induce apoptosis. ChoKα inhibitor-5 can be used for the research of cancer .
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-
-
- HY-132243
-
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Nuclear Factor of activated T Cells (NFAT)
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Inflammation/Immunology
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NFAT Inhibitor-3 (Compound 10) is a factor nuclear factor of activated T cells (NFAT) inhibitor. NFAT Inhibitor-3 inhibits IL-2 production. NFAT Inhibitor-3 binds in a sequence-selective manner directly to DNA. NFAT Inhibitor-3 can be used for the research of transcription factor dysregulation .
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-
-
- HY-164632
-
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Ras
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Cancer
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KRAS inhibitor-32 (compound 139A) is a KRAS inhibitor. KRAS inhibitor-32 can be used in anti-cancer research .
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-
-
- HY-156019
-
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FGFR
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Cancer
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FGFR1 inhibitor-10 (Compound 4i) is an FGFR1 inhibitor (IC50: 28 nM). FGFR1 inhibitor-10 inhibits the phosphorylation of FGFR1. FGFR1 inhibitor-10 has anti-angiogenic, anti-invasion activity, and anti-tumor effect .
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-
-
- HY-169310
-
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ATM/ATR
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Cancer
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ATM Inhibitor-11 (Compound 1) is an inhibitor for ATM with an IC50 of 0.32 nM. ATM Inhibitor-11 inhibits the KAP1 phosphorylation with an IC50 of 0.97 nM. ATM Inhibitor-11 exhibits high exposure in the brain, heart and plasma of ICR mouse. ATM Inhibitor-11 exhibits anti-tumor efficacy in NCI-H441 xenograft mouse model .
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- HY-144687
-
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ATM/ATR
PI3K
mTOR
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Cancer
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ATM Inhibitor-4 (compound 39) is a potent and selective ATM inhibitor, with an IC50 of 0.32 nM. ATM Inhibitor-4 shows stronger inhibition of PI3K kinases family. ATM Inhibitor-4 shows a full inhibition of mTOR at 1 μM. ATM Inhibitor-4 exhibits favorable metabolic stability .
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-
-
- HY-162976
-
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Ras
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Cancer
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KRAS inhibitor-35 (compound 72) is a KRAS inhibitor, with IC50 of 2 nM. KRAS inhibitor-35 can be used in tumor research .
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-
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- HY-148367A
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- HY-151287
-
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Ras
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Cancer
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KRAS inhibitor-20 is a small molecular inhibitor of KRas G12C, the oncogenic mutant. KRAS inhibitor-20 inhibits KRas G12C with the IC50 value <10 nM .
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- HY-163177
-
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HIV
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Infection
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HIV-1 inhibitor-63 (compound S17) is a potent HIV-1 inhibitor. HIV-1 inhibitor-63 inhibits integrase-Ku70 complex formation with an IC50 value of 12 µM. HIV-1 inhibitor-63 inhibits HIV-1 post-integration DNA repair .
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-
-
- HY-147322
-
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YAP
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Cancer
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YAP/TAZ inhibitor-2 is a potent and orally active TEAD-YAP/TAZ inhibitor with an EC50 value of 3 nM. YAP/TAZ inhibitor-2 shows anti-proliferative activity. YAP/TAZ inhibitor-2 shows antitumor activity .
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- HY-118911
-
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ATM/ATR
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Cancer
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ATM Inhibitor-10 (compound 74), a 3-quinoline carboxamide, is a highly selective and orally active ATM inhibitor (IC50: 0.6 nM). ATM Inhibitor-10 has anti-tumor activity in SW620 xenograft models. ATM Inhibitor-10 is synergistic with Top I inhibitors .
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- HY-153787
-
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ATM/ATR
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Cancer
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ATM inhibitor-6 (A-193) is a selective ATM kinase inhibitor. ATM inhibitor-6 can be used in cancer research .
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-
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- HY-167871
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-
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- HY-162974
-
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Ras
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Cancer
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KRAS inhibitor-34 (compound 27) is a KRAS inhibitor, with IC50 of 6.4 nM. KRAS inhibitor-34 can be used in tumor research .
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- HY-137471
-
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RIN1
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Notch
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Cancer
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RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation .
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-
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- HY-131344
-
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mTOR
Autophagy
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Cancer
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mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells .
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-
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- HY-144686
-
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ATM/ATR
PI3K
mTOR
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Cancer
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ATM Inhibitor-3 (compound 34) is a potent and selective ATM inhibitor, with an IC50 of 0.71 nM. ATM Inhibitor-3 shows inhibition of PI3K kinases family. ATM Inhibitor-3 exhibits favorable metabolic stability .
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-
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- HY-122158
-
-
-
- HY-119937
-
-
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- HY-136121
-
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Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 6 (Compound 14b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 6 inhibits tubulin polymerization with an IC50 of 0.87 μM. Tubulin inhibitor 6 inhibits K562 cell growth with an IC50 of 840 nM .
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- HY-136123
-
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Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM .
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-
- HY-136122
-
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Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 7 (Compound 33c) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 7 inhibits tubulin polymerization with an IC50 of 0.52 μM. Tubulin inhibitor 7 inhibits K562 cell growth with an IC50 of 11 nM .
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-
- HY-149487
-
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FGFR
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Cancer
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FGFR1 inhibitor-8 (Compound 9) is a FGFR1 inhibitor (IC50s: 0.5 nM). FGFR1 inhibitor-8 binds to the ATP-binding pocket of FGFR1. FGFR1 inhibitor-8 has anticancer activity .
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- HY-149488
-
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FGFR
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Cancer
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FGFR1 inhibitor-9 (Compound 7) is an FGFR1 inhibitor (IC50s: 0.85 nM). FGFR1 inhibitor-9 binds to the ATP-binding pocket of FGFR1. FGFR1 inhibitor-9 has anticancer activity .
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-
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- HY-151619
-
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Epoxide Hydrolase
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Inflammation/Immunology
|
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sEH inhibitor-12 (compound 34) is a sEH inhibitor with an IC50 value of 0.7 μM. sEH inhibitor-12 inhibits the 5-lipoxygenase-activating protein (FLAP)-mediated leukotriene (LT) biosynthesis with an IC50 value of 2.9 μM. sEH inhibitor-12 can be used for the research of inflammation .
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- HY-154957
-
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mTOR
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Neurological Disease
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mTOR inhibitor-11 (Compound 9) is a brain-penetrant mTOR inhibitor (IC50: 21 nM for pS6). mTOR inhibitor-11 also inhibits pCHK1 and PDE4D with IC50s of 17.2 and 17.0 μM. mTOR inhibitor-11 can be used for research of CNS disease .
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- HY-136704
-
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Glutaminase
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Cancer
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GLS1 Inhibitor-1 (Compound 27) is an orally active inhibitor for glutaminase 1 (GLS1) with an IC50 of 0.021 μM. GLS1 Inhibitor-1 inhibits the proliferation of PC-3 with an IC50 of 0.3 nM. GLS1 Inhibitor-1 exhibits antitumor efficacy against NCI-H1703 with GI50 of 0.011 μM. GLS1 Inhibitor-1 exhibits moderate pharmacokinetic characteristics .
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- HY-151617
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- HY-152536
-
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NO Synthase
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Cancer
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iNOS inhibitor-10 is an iNOS inhibitor (IC50: 65 nM). iNOS inhibitor-10 has antiproliferative effect against triple negative breast cancer cells .
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- HY-101998
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-
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- HY-146617
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Glutaminase
Apoptosis
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Cancer
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GLS1 Inhibitor-4 (compound 41e) is a potent GLS1 inhibitor with an IC50 of 11.86 nM. GLS1 Inhibitor-4 shows antiproliferative activity, good metabolic stability, robust GLS1 binding affinity. GLS1 Inhibitor-4 blocks the glutamine metabolism and induce the production of ROS. GLS1 Inhibitor-4 induces apoptosis and shows antitumor activity .
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- HY-139624
-
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JNK
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Others
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JNK3 inhibitor-1 is a potent and selective JNK3 inhibitor (IC50 = 0.005 μM). JNK3 inhibitor-1 is orally bioavailable and brain penetrant.
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-
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- HY-149693
-
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Aurora Kinase
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Cancer
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Aurora kinase inhibitor-11 (compound 25) is an inhibitor of Aurora Kinase with an IC50 of 0.14 μM. Aurora kinase inhibitor-11 has anticancer activity .
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- HY-159476
-
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Ras
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Cancer
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KRAS inhibitor-26 (compound 194a) is a potent KRAS G12V inhibitor (IC50: ≤100 nM). KRAS inhibitor-26 can be used for cancer research .
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- HY-145436
-
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Ras
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Cancer
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KRAS inhibitor-11 (compound 12) is a KRAS inhibitor .
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- HY-139607
-
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Monoamine Oxidase
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Inflammation/Immunology
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SSAO inhibitor-1 is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor. SSAO inhibitor-1 has anti-inflammatory activity and can be used for liver diseases research .
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- HY-146616
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Glutaminase
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Cancer
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GLS1 Inhibitor-3 (compound C147) is a potent GLS1 inhibitor with an IC50 of 27.98 nM. GLS1 Inhibitor-3 shows antiproliferative activity .
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-
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- HY-146088
-
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HIV
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Infection
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HIV-1 inhibitor-31 (compound 4) is a potent HIV-1 inhibitor. HIV-1 inhibitor-31 can be used for researching AIDS .
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-
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- HY-147993
-
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Aurora Kinase
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Cancer
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Aurora kinase inhibitor-10 (Compound 6c) is an orally active Aurora B inhibitor with an IC50 of 8 nM. Aurora kinase inhibitor-10 shows antitumor activity .
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- HY-151996
-
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Microtubule/Tubulin
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Cardiovascular Disease
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Tubulin inhibitor 31 is a potent tubulin inhibitor with an IC50 value of 4 µM. Tubulin inhibitor 31 shows anti-proliferative activity. Tubulin inhibitor 31 inhibits the HUVEC migration .
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- HY-153433
-
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Others
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Neurological Disease
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Serine Hydrolase inhibitor-21 (compound 8), a pyridine, is a serine hydrolase inhibitor with a Ki of 429 nM for BuChE. Serine Hydrolase inhibitor-21 has the potential for Alzheimer's disease research .
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- HY-154958
-
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mTOR
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Neurological Disease
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mTOR inhibitor-12 (Compound 11) is a selective brain penetrant mTOR inhibitor without genotoxicity risk. mTOR inhibitor-12 can be used for the research of CNS diseases .
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- HY-162091
-
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Topoisomerase
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Cancer
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Topoisomerase I inhibitor 13 (Compound G11) is a Topo I inhibitor that inhibits cancer cell proliferation. Topoisomerase I inhibitor 13 significantly inhibits tumor growth in vivo .
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- HY-157814
-
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Apoptosis
Epigenetic Reader Domain
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Cancer
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Menin-MLL inhibitor-25 (compound A6) is a potent Menin-MLL interaction inhibitor with an IC50 value of 0.38 µM. Menin-MLL inhibitor-25 shows anti-proliferative activity. Menin-MLL inhibitor-25 induces apoptosis and cell cycle arrest at G0/G1 phase. Menin-MLL inhibitor-25 reverses the differentiation arrest .
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- HY-149866
-
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Cytochrome P450
HIV
Reverse Transcriptase
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Infection
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HIV-1 inhibitor-58 (Compound 10c) is a broad-spectrum antiviral agent. HIV-1 inhibitor-58 is a non-nucleoside reverse transcriptase inhibitor. HIV-1 inhibitor-58 inhibits WT strain IIIB, NNRTI-resistant strains (such as K103N and E138K) in MT-4 cells, with EC50 less than 50 nM. HIV-1 inhibitor-58 also inhibits CYP2C9 and CYP2C19 (IC50: 2.06 μM, 1.91 μM). HIV-1 inhibitor-58 can be used for HIV infection reserch .
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- HY-145909
-
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-17 (Compound 5i) is a potent inhibitor of BRD4 with an IC50 of 0.33 μM. BRD4 Inhibitor-17 plays crucial role in regulating transcription of inflammatory, proliferation and cell cycle genes. BRD4 Inhibitor-17 serves as potential antidotes for arsenicals .
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- HY-150963
-
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Renin
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Cardiovascular Disease
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Renin inhibitor-1 (compound 26) is a potent and orally active renin inhibitor with IC50s of 0.9, 1.8 nM for rh-renin and hPRA, respectively. Renin inhibitor-1 shows antihypertensive efficacy. Renin inhibitor-1 has the potential for the research of hypertension and cardiovascular/renal diseases .
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- HY-148838
-
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c-Myc
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Cancer
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c-Myc inhibitor 8 (compound 56) is a c-Myc inhibitor. c-Myc inhibitor 8 effectively inhibits cell viability of a variety of cancer cells. c-Myc inhibitor 8 inhibits human prostate and lung cancer growth in mouse models. c-Myc inhibitor 8 can be used for cancer research .
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- HY-152209
-
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-26 is a bromodomain protein 4 (BRD4) inhibitor/nitric oxide-donator. BRD4 Inhibitor-26 inhibits BRD4 (BD1) and BRD4 (BD2) with IC50 values of 0.82 μM and 1.94 μM, respectively. BRD4 Inhibitor-26 can be used for the research of ovarian cancer .
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- HY-141525
-
-
- HY-151288
-
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Ras
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Cancer
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KRAS inhibitor-21 (22b) is a KRAS G12C inhibitor with an IC50 value of <0.01 μM. KRAS inhibitor-21 can be used in cancer research .
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- HY-400902
-
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YAP
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Cancer
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YAP/TAZ inhibitor-3 (Compound 24) is a YAP/TAZ inhibitor. YAP/TAZ inhibitor-3 shows firefly luciferase inhibitory activity, with an IC50 < 0.1 μM .
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- HY-163190
-
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Bacterial
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Infection
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NDM-1 inhibitor-4 (compound 27) is a NDM-1 inhibitor with Ki of 1.7 μM. NDM-1 inhibitor-4 has antimicrobial effect .
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- HY-147375
-
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Epigenetic Reader Domain
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Cancer
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Bromodomain inhibitor-10 (compound 128) is a potent bromodomain inhibitor with Kds of 15.0, 2500 nM for BRD4-1 and BRD4-2, respectively. Bromodomain inhibitor-10 inhibits the production of IL12p40 .
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-
- HY-147374
-
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Epigenetic Reader Domain
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Metabolic Disease
Inflammation/Immunology
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Bromodomain inhibitor-9 is a Bromodomains inhibitor that selectively inhibits BRD4-1 (Kd: 12 nM). Bromodomain inhibitor-9 can be used in the research of diseases or conditions associated with systemic or tissue inflammation, lipid metabolism, fibrosis or chronic autoimmune diseases .
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- HY-161986
-
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HIV
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Infection
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HIV-1 inhibitor-74 (compound 10c) is a potent HIV-1 inhibitor with an EC50 value of 0.0047 µM for HIV-1 IIIB. HIV-1 inhibitor-74 shows cytotoxicity. HIV-1 inhibitor-74 inhibits WT HIV-1 RT activity with an IC50 value of 0.134 µM. HIV-1 inhibitor-74 shows broad-spectrum anti HIV-1 activity .
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- HY-112851
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-
- HY-144991
-
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Aurora Kinase
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Cancer
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Aurora kinase inhibitor-8 is a highly selective inhibitor of the Aurora kinases.
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- HY-18353
-
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mTOR
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Cancer
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mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
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- HY-155090
-
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ATM/ATR
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Cancer
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ATM Inhibitor-8 (Compound 10r) is a highly potent, selective and orally active ATM inhibitor,with an IC50 of 1.15 nM. ATM Inhibitor-8 exhibits anti-tumor activity .
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- HY-157460
-
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-29 (SQ-17) is a BRD4 inhibitor, with an IC50 of <100 nM. BRD4 Inhibitor-29 shows antiproliferative effect against prostate cancer cells .
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- HY-159121
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-
- HY-142468
-
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HIV
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Infection
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HIV-1 inhibitor-12 is potent HIV-1 inhibitor. HIV-1 inhibitor-12 inhibits HIV-1 capsid protein polymerization with an IC50 of 9 nM (WO2021104413A1, compound 1-1a) .
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-
- HY-155211
-
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mTOR
PI3K
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Cancer
|
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mTOR inhibitor-13 (compound 9g), an aryl ureido compound, is a potent and selective mTOR inhibitor with an IC50 of 0.29 nM. mTOR inhibitor-13 also inhibits PI3K-α with an IC50 of 119 nM .
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- HY-143272
-
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FGFR
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Cancer
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FGFR1 inhibitor-6 is a potent FGFR1 inhibitor with an IC50 value of 16.31 nM. FGFR1 inhibitor-6 shows cytotoxic activities. FGFR1 inhibitor-6 induces apoptosis and cell cycle arrest at pre-G1 and G2/M phase .
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- HY-148373
-
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Epigenetic Reader Domain
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Cancer
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BRM/BRG1 ATP Inhibitor-3 is a BRG1/BRM inhibitor. BRM/BRG1 ATP Inhibitor-3 inhibits BRM and BRG1 with IC50 values of 10.4 nM and 19.3 nM, respectively. BRM/BRG1 ATP Inhibitor-3 can be used for the research of cancers and BAF complex-related disorders .
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- HY-118933
-
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SJA6017
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Proteasome
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Others
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Calpain Inhibitor VI (SJA6017) is a synthesized peptide aldehyde inhibitor of calpain. Calpain Inhibitor VI inhibits purified m-calpain with the IC50 of 80 nM. Calpain Inhibitor VI can be used for the research of cataract .
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- HY-157397A
-
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Others
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Neurological Disease
|
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ANAT inhibitor-4 tetralithium (compound BA2) is potent N-acetyltransferase (ANAT) inhibitor with a Ki value of 48 nM. ANAT inhibitor-4 tetralithium has the potential for canavan disease (CD) research .
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- HY-169153
-
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Others
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Inflammation/Immunology
|
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Cot inhibitor-3 (Compound 33) is a potent and selective cancer osaka thyroid (COT) kinase inhibitor, with an IC50 of 4 nM. Cot inhibitor-3 can be used to prevent inflammation-driven lameness .
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-
- HY-153745
-
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Trk Receptor
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Cancer
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Protein kinase inhibitor 5 is a potent TRK-A inhibitor with an IC50 value of 1.8 nM. Protein kinase inhibitor 5 inhibits cell viability .
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-
- HY-153692A
-
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Biochemical Assay Reagents
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Others
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(R)-WRN inhibitor 1 is the R-isomer of WRN inhibitor 1 (example 7). WRN inhibitor 1 is a WRN inhibitor with anticancer activity .
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-
- HY-149519
-
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Epigenetic Reader Domain
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Cancer
|
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BRD4 Inhibitor-28 (Compound 18) is an orally active BRD4 Inhibitor. BRD4 Inhibitor-28 inhibits BRD40-BD1, BRD40-BD2 with IC50s of 15, 55 nM. BRD4 Inhibitor-28 also inhibits BRD2-BD1, BRD3-BD1, BRDT-BD1 with IC50s of 19, 25, 68 nM. BRD4 Inhibitor-28 has anti-melanoma activity .
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-
- HY-112911
-
-
- HY-137497
-
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Ras
Apoptosis
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Cancer
|
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KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells .
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- HY-146660
-
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c-Myc
Epigenetic Reader Domain
Apoptosis
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Cancer
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BRD4 Inhibitor-18 is a highly potent BRD4 inhibitor with an IC50 value of 110 nM. BRD4 Inhibitor-18 has a hydrophobic acetylcyclopentanyl side chain. BRD4 Inhibitor-18 can significantly suppress the proliferation of MV-4-11 cells with high BRD4 level. BRD4 Inhibitor-18 has apoptosis-promoting and G0/G1 cycle-arresting activity .
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-
- HY-143235
-
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Epigenetic Reader Domain
Apoptosis
Bcl-2 Family
Caspase
c-Myc
|
Cancer
|
|
BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research .
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- HY-146208
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer .
|
-
- HY-147891
-
|
|
Apoptosis
|
Cancer
|
|
Angiogenesis inhibitor 3 (compound 8) is a potent angiogenesis inhibitor. Angiogenesis inhibitor 3 inhibits the proliferation of HUVEC and HCT-15 cells, with IC50 values of 1.00 and 0.71 μM. Angiogenesis inhibitor 3 induces the apoptosis of HUVEC and HCT-15 cells. Angiogenesis inhibitor 3 shows anticancer activity, and suppresses the invasion of cancer cells. Angiogenesis inhibitor 3 inhibits the angiogenesis in zebrafish embryos .
|
-
- HY-147890
-
|
|
Apoptosis
|
Cancer
|
|
Angiogenesis inhibitor 2 (compound 72) is a potent angiogenesis inhibitor. Angiogenesis inhibitor 2 inhibits the proliferation of HUVEC and HCT-15 cells, with IC50 values of 1.93 and 0.21 μM. Angiogenesis inhibitor 2 induces the apoptosis of HUVEC and HCT-15 cells. Angiogenesis inhibitor 2 shows anticancer activity, and suppresses the invasion of cancer cells. Angiogenesis inhibitor 2 inhibits the angiogenesis in zebrafish embryos .
|
-
- HY-152200
-
|
|
HIV Protease
Reverse Transcriptase
|
Infection
Inflammation/Immunology
|
|
HIV-1 inhibitor-53 is a dual HIV-1 protease and reverse transcriptase inhibitor. HIV-1 inhibitor-53 inhibits HIV-1 protease (PR) and reverse transcriptase (RT) activity with IC50 values of 1.93 nM and 2.35 μM, respectively. HIV-1 inhibitor-53 can be used for the research of acquired immune deficiency syndrome (AIDS) .
|
-
- HY-151962
-
|
|
JNK
Apoptosis
GSK-3
p38 MAPK
|
Neurological Disease
|
|
JNK3 inhibitor-5 (Compound 22b) is a potent and selective JNK3 inhibitor with an IC50 of 0.379 nM. JNK3 inhibitor-5 effectively protects the neuronal cells against amyloid beta-induced apoptosis. JNK3 inhibitor-5 has a high cell permeability and is predicted as BBB permeable .
|
-
- HY-163362
-
|
|
Reverse Transcriptase
PKC
HIV
|
Infection
|
|
HIV-1 inhibitor-65 (compound 3c) is an inhibitor of HIV-1 (EC50: 2.9 nM) and an activator of protein kinase C (PKC). HIV-1 inhibitor-65 inhibits syncytium formation (EC50: 7.0 nM) and inhibits HIV-1 entry and HIV-1 reverse transcriptase .
|
-
- HY-124639
-
|
|
CDK
|
Cancer
|
|
CDK9 inhibitor HH1 is a potent and selectively CDK9 inhibitor. CDK9 inhibitor HH1 inhibits the transcription of CDK. CDK9 inhibitor HH1 can be used in research of cancer .
|
-
- HY-148573
-
-
- HY-47597
-
|
|
Bacterial
|
Infection
|
|
Protein kinase G inhibitor-2 (Compound 266) is a mycobacterial protein kinase G inhibitor, with an IC50 of 3 μM. Protein kinase G inhibitor-2 can be used for mycobacterial infection research .
|
-
- HY-156554
-
|
|
Raf
|
Cancer
|
|
Raf inhibitor 3 (Example 30) is a Raf inhibitor. Raf inhibitor 3 inhibits B-Raf and C-Raf with IC50 values less than 15 nM. Raf inhibitor 3 can be used for research of cancers .
|
-
- HY-112373
-
|
|
Aurora Kinase
|
Others
|
|
Aurora kinase inhibitor-3 is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50 of >10 μM. Aurora kinase inhibitor-3 has a binding mode with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket .
|
-
- HY-146711
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 24 is a potent tubulin inhibitor. Tubulin inhibitor 24 inhibits tubulin polymerization. Tubulin inhibitor 24 induces cell cycle arrest at the G2/M phase in a concentration-dependent manner. Tubulin inhibitor 24 shows antitumor activity with no obvious toxicity .
|
-
- HY-147750
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
Cancer
|
|
TDP1 Inhibitor-2 (compound 5) is a potent inhibitor for TDP1 (tyrosyl-DNA phosphodiesterase 1), with an IC50 of 99 nM. TDP1 Inhibitor-2 also can inhibit SCAN1 (spinocerebellar ataxia syndrome with axonal neuropathy), with an IC50 of 3.5 μM .
|
-
- HY-148043
-
|
|
β-catenin
|
Others
|
|
Schnurri-3 inhibitor-1 is a potent schnurri-3 inhibitor which is an essential regulator of adult bone formation. Schnurri-3 inhibitor-1 can inhibit Shn3 with EF1alpha promoter in osteoblast cell line Shn3FFL with an AC50 value of 2.09 μM. Schnurri-3 inhibitor-1 can be used to research osteoporosis .
|
-
- HY-151616
-
|
|
Epoxide Hydrolase
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
sEH inhibitor-10 (Compound 37) is a selective soluble epoxide hydrolase (sEH) inhibitor (IC50=0.5 μM). sEH inhibitor-10 maintains high cycloeicosatrienoic acid (EETs) levels by inhibiting sEH, thereby reducing inflammation, regulating endothelial tone, improving mitochondrial function, and reducing oxidative stress. sEH inhibitor-10 has good research potential in metabolic, renal and cardiovascular diseases .
|
-
- HY-122914
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-3 is an inhibitor of KRAS inhibitor. KRAS inhibitor-3 binds to WT and oncogenic KRAS mutants with high affinity (KD: 0.28 μM for KRAS WT, 0.63 μM for KRAS G12C, 0.37 μM for KRAS G12D, 0.74 μM for KRAS Q61H). KRAS inhibitor-3 also disrupts interaction of KRAS with Raf .
|
-
- HY-139629
-
-
- HY-142253
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-10 is a nanomolar HIV-1 maturation inhibitor.
|
-
- HY-162971
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-33 (compound 115a) is an inhibitor of pyridopyrimidine kras (IC50 ≤ 100nM) .
|
-
- HY-149260
-
-
- HY-48958
-
|
|
Bacterial
|
Infection
|
|
Protein kinase G inhibitor-1 (Compound 270) is a mycobacterial protein kinase G inhibitor, with an IC50 of 0.9 μM. Protein kinase G inhibitor-1 can be used for mycobacterial infection research .
|
-
- HY-146308
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-26 (compound 9a) is a potent HIV-1 reverse transcriptase (RT) inhibitor with an IC50 value of 1.4 μM. HIV-1 inhibitor-26 has low cytotoxicity with a CC50 of 1486 μM in PBMCs. HIV-1 inhibitor-26 can be used for researching AIDS .
|
-
- HY-143294
-
|
|
Epoxide Hydrolase
|
Cardiovascular Disease
|
|
sEH inhibitor-2 (compound 5l) is an orally active (predicted percentage absorption: 71.2-88.4%) soluble epoxide hydrolase (sEH) inhibitor, with an IC50 of 0.9 nM. sEH inhibitor-2 can maintain epoxyeicosatrienoic acids (EETs) serum level in high concentrations. sEH inhibitor-2 can be used in study of cardiovascular protection .
|
-
- HY-152560
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-55 (compound 4d) inhibits WT HIV-1 with an EC50 value of 8.6 nM. HIV-1 inhibitor-55 also shows inhibitory potency against single and double HIV-1 mutants. HIV-1 inhibitor-55 can be used for the research of virus infection .
|
-
- HY-111370
-
|
|
mTOR
|
Cancer
|
|
mTOR inhibitor-2 is a highlt potent, selective and oral mTOR inhibitor with an IC50 of 7 nM. mTOR inhibitor-2 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates .
|
-
- HY-145821
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 15 is a potent tubulin inhibitor. Tubulin inhibitor 15 shows antiproliferative activity. Tubulin inhibitor 15 shows cytotoxicity in HepG2 cells .
|
-
- HY-145822
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 16 is a potent tubulin inhibitor. Tubulin inhibitor 16 shows antiproliferative activity. Tubulin inhibitor 16 shows cytotoxicity in HepG2 cells .
|
-
- HY-153745A
-
|
|
Trk Receptor
|
Cancer
|
|
Protein kinase inhibitor 5 sulfate hydrate is a potent TRK-A inhibitor with an IC50 value of 1.8 nM. Protein kinase inhibitor 5 sulfate hydrate inhibits cell viability .
|
-
- HY-128403
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK inhibitor 8 (Compound 27) is a Btk inhibitor with an IC50 of 0.11 nM. BTK inhibitor 8 inhibits B cell activation in hWB with an IC50 of 2 nM .
|
-
- HY-103271
-
|
|
Bcl-2 Family
|
Cancer
|
|
Bax inhibitor peptide, negative control is a inhibitor of Bax. Bax inhibitor peptide, negative control inhibits Bax translocation to mitochondria and Bax-mediated apoptosis in vitro .
|
-
- HY-155054
-
|
|
Parasite
|
Infection
|
|
Cysteine protease inhibitor-3 (Compound 15) is a Cysteine protease inhibitor. Cysteine protease inhibitor-3 inhibits Pf3D7, PfW2, PfFP2 and PfFP3 with IC50s of 0.74 μM, 1.05 μM, 3.5 μM, and 4.9 μM, respectively. Cysteine protease inhibitor-3 has anti-plasmodial efficacy against both drug-sensitive and drug-resistant parasites .
|
-
- HY-146739
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD4 Inhibitor-19 is a BET inhibitor with an IC50 of 55 nM for BRD4-BD1. BRD4 Inhibitor-19 can be used for multiple myeloma research .
|
-
- HY-147388
-
|
|
Cholinesterase (ChE)
|
Metabolic Disease
|
|
hiCE inhibitor-1, a sulfonamide derivative, is a selective human intestinal enzyme (hiCE) inhibitor with a Ki value of 53.3 nM. hiCE inhibitor-1 can be used to improve Irinotecan (HY-16562)-induced diarrhoea .
|
-
- HY-148395
-
|
|
Dihydroorotate Dehydrogenase
|
Cancer
|
|
UCK2 Inhibitor-2 is a non-competitive uridine-cytidine kinase 2 (UCK2) inhibitor with an IC50 value of 3.8 µM. UCK2 Inhibitor-2 can suppress uridine salvage in cells .
|
-
- HY-149268
-
|
|
JNK
|
Neurological Disease
|
|
JNK3 inhibitor-6 (Compound A53) is a selective JNK3 Inhibitor (IC50=78 nM). JNK3 inhibitor-6 has neuroprotective effect, and can used for research of neurodegenerative diseases .
|
-
- HY-153754
-
|
|
Others
|
Metabolic Disease
|
|
Phosphatidylcholine transfer protein inhibitor-1 (Answer 37 in Patent) is a phosphatidylcholine transfer protein (PC-TP) inhibitor. Phosphatidylcholine transfer protein inhibitor-1 can be used for research of PC-TP related disease such as obesity .
|
-
- HY-156876
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
20-HETE inhibitor-2 is an inhibitor of 20-HETE, preventing 20-HETE production. 20-HETE inhibitor-2 can used in study 20-HETE related diseases .
|
-
- HY-138284
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Avenanthramide-C methyl ester is an anti-inflammatory agent and NF-κB inhibitor that inhibits the secretion of pro-inflammatory factors. Avenanthramide-C methyl ester inhibits NF-κB activation by inhibiting IKK and IκB phosphorylation and inhibiting proteasome activity .
|
-
- HY-112722
-
-
- HY-149991
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-56 (compound 12126065) is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor. HIV-1 inhibitor-56 has antiviral activity against wild-type HIV-1 in TZM cells with an EC50 value of 0.24 nM. HIV-1 inhibitor-56 penetrates the blood-brain barrier .
|
-
- HY-18953
-
|
|
mTOR
|
Cancer
|
|
mTOR inhibitor-23 (compound DHM25) is a selective, competitive, irreversible and covalent inhibitor of mTOR. mTOR inhibitor-23 has the mechanism of inhibition occurs mainly through its capacity to covalently interact with a nucleophilic amino acid inside the ATP pocket. mTOR inhibitor-23 exerts potent antitumor activity against triple-negative breast tumor cell lines .
|
-
- HY-152539
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-54 is a potent HIV-1 inhibitor. HIV-1 inhibitor-54 has anti-HIV activity in MT-4 cells against WT HIV-1 (strain IIIB) with an EC50 value of 0.032 μM. HIV-1 inhibitor-54 can be used for the research of virus infection .
|
-
- HY-149279
-
|
|
JNK
|
Neurological Disease
|
|
JNK3 inhibitor-7 is a potent, orally active and cross the blood-brain barrier JNK3 inhibitor with IC50 values of 53, 973, 1039 nM for JNK3, JNK2, JNK1, respectively. JNK3 inhibitor-7 shows significant neuroprotective effects. JNK3 inhibitor-7 has the potential for the research of Alzheimer’s disease (AD) .
|
-
- HY-155032
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 15 (compound 7a) is a nonsubstrate inhibitor of P-glycoprotein (Pgp). P-gp inhibitor 15 inhibits Pgp-ATPase activity，and interfers Pgp-mediated Rhodamine123 efflux. P-gp inhibitor 15 also enhances the inhibitory efficacy of Paclitaxel (HY-B0015)，inhibits tumor progress in nude mice KBV xenograft tumors model .
|
-
- HY-101275
-
-
- HY-119369
-
|
|
Bacterial
|
Infection
|
|
FadD32 Inhibitor-1 is a potent FadD32 inhibitor with anti-tubercular activity .
|
-
- HY-144685
-
|
|
ATM/ATR
|
Cancer
|
|
ATM Inhibitor-2 (compound 7) is a potent and selective ATM inhibitor, with an IC50 of <1 nM .
|
-
- HY-155473
-
-
- HY-13278A
-
|
|
IRAK
|
Inflammation/Immunology
|
|
IRAK inhibitor 4 (trans) is the trans form of IRAK inhibitor 4. IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor.
|
-
- HY-P4028
-
|
|
Virus Protease
|
Infection
|
|
Herpes virus inhibitor 1 is a herpes virus inhibitor and disrupts herpes virus ribonucleotide reductase quaternary structure. Herpes virus inhibitor 1 inhibits viral replication .
|
-
- HY-P4030
-
|
|
HIV Protease
|
Infection
|
|
Herpes virus inhibitor 2 is a herpes virus inhibitor and disrupts herpes virus ribonucleotide reductase quaternary structure. Herpes virus inhibitor 2 inhibits viral replication .
|
-
- HY-139376
-
|
|
FGFR
|
Cancer
|
|
FGFR1 inhibitor-2 is a FGFR1 inhibitor (IC50 is 4.55 μM in MDA-MB-231 cells). FGFR1 inhibitor-2 can be used for the research of metastatic triple-negative breast cancer .
|
-
- HY-148374
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRM/BRG1 ATP Inhibitor-4 is a BRG1/BRM inhibitor. BRM/BRG1 ATP Inhibitor-4 can be used for the research of cancers and BAF complex-related disorders .
|
-
- HY-148839
-
|
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 9 (compound 332) is a c-Myc inhibitor with an logEC50 of ≥6. c-Myc inhibitor 9 inhibits tumor growth in nude mouse models. c-Myc inhibitor 9 can be used for cancer research .
|
-
- HY-149252
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 32 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 32 shows anti-proliferative activity and inhibits microtubule polymerization. Tubulin inhibitor 32 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin inhibitor 32 shows anti-tumor activity .
|
-
- HY-151928
-
|
|
JNK
|
Neurological Disease
|
|
JNK3 inhibitor-3 (compound 15g) is a selective, BBB permeable and orally active c-Jun N-terminal kinase 3 (JNK3) inhibitor. JNK3 inhibitor-3 has inhibitory activities to JNK1, JNK2 and JNK3 with IC50 values of 147.8, 44.0 and 4.1 nM, respectively. JNK3 inhibitor-3 significantly improves the memory in mouse dementia model. JNK3 inhibitor-3 can be used for the research of Alzheimer’s disease .
|
-
- HY-151933
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
HIV-1 inhibitor-49 is an orally active HIV-1 inhibitor, is a HEPT analog. HIV-1 inhibitor-49 possesses great pharmacokinetics profiles and potent non-nucleoside reverse transcriptase inhibitory activity (IC50=30 nM). HIV-1 inhibitor-49 exerts potential safety without acute toxicity in mouse model .
|
-
- HY-151972
-
|
|
Epigenetic Reader Domain
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
BRD4 Inhibitor-25 is a BRD4 inhibitor with IC50s of 0.82 μM, 1.94 μM for BD1 and BD2 domains of BRD4. BRD4 Inhibitor-25 induces apoptotic and autophagy cell death in ovarian cancer cells. BRD4 Inhibitor-25 can be used in the research of cancers, cardiovascular, neuromuscular and inflammatory disorders.
|
-
- HY-149280
-
|
|
JNK
|
Neurological Disease
|
|
JNK3 inhibitor-8 is a potent, delective, orally active and cross the blood-brain barrier JNK3 inhibitor with IC50 values of 21, 2203, >10000 nM for JNK3, JNK2, JNK1, respectively. JNK3 inhibitor-8 shows significant neuroprotective effects. JNK3 inhibitor-8 has the potential for the research of Alzheimer’s disease (AD) .
|
-
- HY-149291
-
|
|
ATM/ATR
Apoptosis
|
Cancer
|
|
ATM Inhibitor-7 is a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor with an IC50 value of 1.0 nM. ATM Inhibitor-7 induces Apoptosis and cell cycle arrest at G2/M phase when combinanted with CPT-11 (HY-16562). ATM Inhibitor-7 combines with CPT-11 shows antitumor activity .
|
-
- HY-122573
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
Bromodomain inhibitor-13 (Compound 1) is an analog of PFI-3 (HY-12409). Bromodomain inhibitor-13 is a bromodomain-containing protein (BCP) inhibitor. Bromodomain inhibitor-13 targets SMARCA2, SMARCA4, PB1(5), and second bromodomain of PB1 (PB1(2)) with KD values of 37, 53, 30, and 190 nM, respectively .
|
-
- HY-112412
-
|
PDGF Receptor Tyrosine Kinase Inhibitor III
|
PDGFR
|
Neurological Disease
|
|
PDGFR Tyrosine Kinase Inhibitor III (PDGF Receptor Tyrosine Kinase Inhibitor III), a multikinase inhibitor, inhibits PDGFR, EGFR, FGFR, PKA, and PKC, respectively. PDGFR Tyrosine Kinase Inhibitor III can be used for the research of amyotrophic lateral sclerosis .
|
-
- HY-146089
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-32 (compound 3c) is a potent HIV-1 inhibitor with an IC50 value of 34 nM for WT HIV-1. HIV-1 inhibitor-32 can be used for researching AIDS .
|
-
- HY-150759
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-45 (compound IA-6) is a potent HIV-1 RNase H inhibitor with an IC50 value of 0.067 μM. HIV-1 inhibitor-45 shows an antiviral activity .
|
-
- HY-153017
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-1 inhibitor-4 is a HIF-1 inhibitor (IC50: 560 nM). HIF-1 inhibitor-4 reduces the HIF-1α protein level without affecting its mRNA level .
|
-
- HY-163191
-
|
|
Beta-lactamase
Bacterial
|
Infection
|
|
NDM-1 inhibitor-5 (compound 57) is a potent NDM-1 inhibitor, with a Ki of 2.5 μM. NDM-1 inhibitor-5 also shows antibacterial synergistic activity with meropenem (HY-13678) .
|
-
- HY-160548
-
-
- HY-163852
-
-
- HY-155209
-
|
|
Stearoyl-CoA Desaturase (SCD)
|
Cancer
|
|
SCD1 inhibitor-5 (compound 51) is a SCD1 inhibitor,with the IC50 values of 0.13 μM and 31 μM for H2122 and H1819, respectively. SCD1 inhibitor-5 can be used in cancer research .
|
-
- HY-168189
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-76 (compound 9t-2) is a non-nucleoside reverse transcriptase inhibitor of HIV-1. HIV-1 inhibitor-76 can be used in anti-HIV research .
|
-
- HY-115956
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 18 (compound 5j) is a potent inhibitor of tubulin. Tubulin inhibitor 18 is a chalcone compound. Tubulin inhibitor 18 has the potential for the research of cancer diseases .
|
-
- HY-P34013
-
|
|
Ser/Thr Protease
|
Cancer
|
|
Urinary Trypsin Inhibitor Fragment is a fragment derived from urinary trypsin inhibitor by proteolysis. Urinary Trypsin Inhibitor Fragment can inhibit tumor cell invasion by limited proteolysis .
|
-
- HY-168187
-
|
|
Src
|
Cancer
|
|
Src Inhibitor 3 (Compound 7d) is a Src inhibitor with an IC50 of 285 nM. Src Inhibitor 3 inhibits HepG2 cells proliferative with an IC50 of 1.55 μM .
|
-
- HY-118371
-
|
|
Arginase
|
Cancer
|
|
Arginase inhibitor 2 is an Arginase inhibitor (Page 130 in reference patent). Arginase inhibitor 2 synergizes with adoptively transferred antigen- specific T cells to inhibit tumor growth .
|
-
- HY-70005
-
|
Carboxypeptidase inhibitor
|
Carboxypeptidase
|
Metabolic Disease
|
|
CPA inhibitor (Carboxypeptidase inhibitor; compound 5) is a potent carboxypeptidase A (CPA) inhibitor with a Ki of 0.32 μM .
|
-
- HY-130260
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-4 (compound F12) is a potent KRAS inhibitor and developed as anticancer agents .
|
-
- HY-111412
-
-
- HY-128703
-
-
- HY-139648
-
-
- HY-153159
-
|
|
Others
|
Cancer
|
|
Angiogenesis inhibitor 4 is a potent angiogenesis inhibitor. Angiogenesis inhibitor 4 can be used in research of cancer .
|
-
- HY-156875
-
-
- HY-160499
-
-
- HY-W192171
-
-
- HY-162983
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-36 (compund Abd2) directly inhibits KRAS Q61H .
|
-
- HY-156130
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
Menin-MLL inhibitor 29 (Compound C1) is a Menin-MLL PPI inhibitor. Menin-MLL inhibitor 29 binds to Menin with a KD value of 138 nM, and inhibits the binding of Menin to MBM1 (Menin-binding motif 1) with an IC50 value of 46 nM. Menin-MLL inhibitor 29 inhibits HepG2 and Hep3B hepatoma cell proliferation (IC50s: 0.31 μM and 0.71 μM). Menin-MLL inhibitor 29 inhibits tumor growth .
|
-
- HY-118013
-
|
|
Bacterial
|
Infection
|
|
NDM-1 inhibitor-2 is an inhibitor of New Delhi metallo-β-lactamase-1 (NDM-1) and has the ability to inhibit NDM-1 activity. NDM-1 inhibitor-2 exhibits a good inhibitory effect on drug-resistant bacterial strains that overexpress NDM-1. When NDM-1 inhibitor-2 is used in combination with the carbapenem antibiotic meropenem, a favorable synergistic effect can be produced .
|
-
- HY-154987
-
|
|
MARK
|
Cancer
|
|
MAPK4 inhibitor 3 (compound 23b) is an inhibitor of MAPK4 with an IC50 value of 1.01 μM. MAPK4 inhibitor 3 inhibits cancer cells growth. MAPK4 inhibitor 3 can be used for research on cancer and tauopathies .
|
-
- HY-139077
-
|
|
Stearoyl-CoA Desaturase (SCD)
|
Metabolic Disease
Cancer
|
|
SCD1 inhibitor-3 is a safe, potent and orally active SCD1 inhibitor. SCD1 inhibitor-3 can be used for the research of metabolic diseases such as obesity, type II diabetes and dyslipidemia, as well as skin diseases, acne and cancer .
|
-
- HY-139605
-
|
|
GLUT
|
Inflammation/Immunology
Cancer
|
|
GLUT inhibitor-1 is a potent and orally active inhibitor of glucose transporters, targeting both GLUT1 and GLUT3, with IC50s of 242 nM and 179 nM, respectively. GLUT inhibitor-1 has the potential for the reaesrch of cancers and autoimmune diseases .
|
-
- HY-144818
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
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 .
|
-
- HY-138295
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-10 (compound 11) selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1 .
|
-
- HY-146543
-
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Ras
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Cancer
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KRAS inhibitor-13 (compound 5-6) is a potent KRAS G12C inhibitor with an IC50 of 0.883 µM. KRAS inhibitor-13 shows p-ERK inhibition activities with IC50s of 5.9, >100 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-13 has the potential for the research of pancreatic, colorectal, and lung cancers .
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- HY-112807
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SGLT
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Metabolic Disease
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SGLT inhibitor-1 is a potent dual inhibitor of sodium glucose co-transporter proteins (SGLTs), inhibits hSGLT1 and hSGLT2 with IC50s of 43 nM and 9 nM, respectively .
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- HY-145828
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Microtubule/Tubulin
Ferroptosis
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Cancer
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Microtubule inhibitor 2 is a potent and selective, orally active microtubule inhibitor. Microtubule inhibitor 2 triggers cell death through ferroptosis . Microtubule inhibitor 2 shows antitumor activity .
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- HY-115957
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Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 19 (compound 9b) is a potent inhibitor of tubulin. Tubulin inhibitor 19 is an indole chalcone compound. Tubulin inhibitor 19 has the potential for the research of cancer diseases .
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- HY-152156
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis .
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- HY-122714
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PAI-1
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Cancer
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SK-216 is a plasminogen activator inhibitor-1 (PAI-1) inhibitor that acts as an anti-metastatic agent for human osteosarcoma and inhibits lung metastasis of human osteosarcoma .
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- HY-160549
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c-Myc
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Cancer
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c-Myc inhibitor 14 (Compound 13A) is a c-Myc protein inhibitor. The IC50 value of HL60 inhibitor is <100 nM. c-Myc inhibitor 14 shows antitumor activity .
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- HY-128722
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HIV
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Infection
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HIV-1 inhibitor-3 is a HIV infection inhibitor extracted from patent US2018360927 .
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- HY-139638
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MEK
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Cancer
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MEK4 inhibitor-1 is a novel MEK4 inhibitor against pancreatic adenocarcinoma with an IC50 value of 61 nM.
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- HY-139639
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MEK
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Cancer
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MEK4 inhibitor-2 is a novel MEK4 inhibitor against pancreatic adenocarcinoma with an IC50 value of 83 nM.
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- HY-151983
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Thrombin
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Cardiovascular Disease
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Thrombin inhibitor 6 is a potent thrombin inhibitor (IC50: 1 nM). Thrombin inhibitor 6 has the function as an anticoagulant .
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- HY-114199
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- HY-153668
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- HY-108255
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HIV
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Infection
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HIV-1 inhibitor-60 (compound 45) is an HIV inhibitor with the potential for the research of infection diseases .
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- HY-162461
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Reverse Transcriptase
HIV
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Infection
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HIV-1 inhibitor-66 is an orally active non-nucleoside reverse transcription inhibitor (NNRTI). HIV-1 inhibitor-66 shows inhibitory activity against wild-type HIV-1 reverse transcriptase with an IC50 of 40 nM .
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- HY-32015
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MAP3K
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Inflammation/Immunology
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Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC50 of 28 nM. Cot inhibitor-1 shows an inhibition of TNF-alpha production in human whole blood with an IC50 of 5.7 nM .
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- HY-147370
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HIV
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Infection
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HIV-1 inhibitor-46 (compound 13d) is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor with an EC50 value of 1.425 μM. HIV-1 inhibitor-46 can be used for the research of AIDS .
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- HY-115514A
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BRK
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Cancer
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BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models .
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- HY-147903
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HIV
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Infection
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HIV-1 inhibitor-42 (compound 5b) is a potent HIV-1 inhibitor, with an IC50 of 0.06 μM. HIV-1 inhibitor-42 inhibits HIV-1 RT RNA-dependent DNA polymerase and DNA-dependent DNA polymerase, with IC50 values of 0.518 and 0.072 μM .
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- HY-162341
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Topoisomerase
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Cancer
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Topoisomerase I inhibitor 15 (compound 4b) is an inhibitor of topoisomerase I with anticancer activity. Topoisomerase I inhibitor 15 inhibits A549 cells with an IC50 of 7.34 μM .
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- HY-111079
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HIV
Reverse Transcriptase
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Others
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HIV-1 inhibitor-70 (compound 20) is a bifunctional inhibitor that inhibits both wild-type (WT) and K103N mutant reverse transcriptases (RTs) of HIV-1.
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- HY-146533
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Ras
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Cancer
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KRAS inhibitor-12 (compound 6-1) is a potent KRAS G12C inhibitor with an IC50 of 0.537 µM. KRAS inhibitor-12 shows p-ERK inhibition activities with IC50s of 1.3, 3.7 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-12 has the potential for the research of pancreatic, colorectal, and lung cancers .
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- HY-146544
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Ras
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Cancer
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KRAS inhibitor-14 (compound 3-22) is a potent KRAS G12C inhibitor with an IC50 of 0.249 µM. KRAS inhibitor-14 shows p-ERK inhibition activities with IC50s of 1.12, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-14 has the potential for the research of pancreatic, colorectal, and lung cancers .
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- HY-146545
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Ras
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Cancer
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KRAS inhibitor-15 (compound 3-19) is a potent KRAS G12C inhibitor with an IC50 of 0.954 µM. KRAS inhibitor-15 shows p-ERK inhibition activities with IC50s of 2.03, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-15 has the potential for the research of pancreatic, colorectal, and lung cancers .
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- HY-146546
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Ras
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Cancer
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KRAS inhibitor-16 (compound 3-11) is a potent KRAS G12C inhibitor with an IC50 of 0.457 µM. KRAS inhibitor-16 shows p-ERK inhibition activities with IC50s of 3.06, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-16 has the potential for the research of pancreatic, colorectal, and lung cancers .
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- HY-146475
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Ras
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Cancer
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KRAS inhibitor-17 (compound 3-9) is a potent KRAS G12C inhibitor with an IC50 of 3.37 µM. KRAS inhibitor-17 shows p-ERK inhibition activities with IC50s of 9.25, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-17 has the potential for the research of pancreatic, colorectal, and lung cancers .
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- HY-146476
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Ras
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Cancer
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KRAS inhibitor-18 (compound 3-10) is a potent KRAS G12C inhibitor with an IC50 of 4.74 µM. KRAS inhibitor-18 shows p-ERK inhibition activities with IC50s of 66.4, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-18 has the potential for the research of pancreatic, colorectal, and lung cancers .
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- HY-147723
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HIV
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Infection
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HIV-1 inhibitor-39 (compound 3c) is a potent HIV-1 inhibitor with an EC50 of >112.88 µM. HIV-1 inhibitor-39 shows anti-RT (HIV-1 reverse transcriptase) activities with an IC50 of 15.75 µM. HIV-1 inhibitor-39 shows cytotoxicity for MT-4 cells with an CC50 of 112.9 µM .
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- HY-138131
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Others
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Neurological Disease
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SOD1-Derlin-1 inhibitor-1 (compound 56-20) is an inhibitor of SOD1-Derlin-1 interaction. SOD1-Derlin-1 inhibitor-1 inhibits SOD1 G93A-Derlin-1 complex with an IC50 value of 7.11 μM. SOD1-Derlin-1 inhibitor-1 can be used for the research of amyotrophic lateral sclerosis .
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- HY-155029
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Epoxide Hydrolase
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Inflammation/Immunology
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sEH inhibitor-16 is a soluble epoxide hydrolase (sEH) inhibitors with an IC50 of 2 nM. sEH inhibitor-16 reduces the inflammatory damage in Cerulein (HY-A0190)-induced acute pancreatitis (AP) in mice and can be used for inflammation/immunology research .
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- HY-155078
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-27 (compound 6) is a BRD4 inhibitor with IC50 of 9.6 and 11.3 μM for BRD4 BD1 and BRD4 BD2, respectively. BRD4 Inhibitor-27 has the potential to study cancer .
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- HY-17541
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Cathepsin
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Others
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Cysteine Protease inhibitor is an inhibitor of cysteine protease.
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- HY-17541A
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Cathepsin
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Others
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Cysteine Protease inhibitor hydrochloride is an inhibitor of cysteine protease.
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- HY-49066
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- HY-148000
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- HY-153668A
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- HY-156639
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EGFR
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Cancer
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EGFR/ErbB-2 inhibitor-1 is a ErbB2/HER2 inhibitor .
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- HY-156969
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Topoisomerase
Btk
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Cancer
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Topoisomerase I inhibitor 11 is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 11 can bind to BTK .
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- HY-164201
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HIV
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Infection
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HIV-1 inhibitor-69 (compound Test set 1) is a HIV-1 RT inhibitor .
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- HY-136279
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Apoptosis
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Cancer
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TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC50 of 2.8 nM. TrxR inhibitor D9 has the capability to inhibit tumor proliferation both in vitro and in vivo .
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- HY-112335
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Src
Interleukin Related
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Cancer
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Lck Inhibitor III (compound 12h) is a potent Lck inhibitor, with an IC50 of 867 nM. Lck Inhibitor III inhibits IL-2 synthesis in Jurkat cells, with an IC50 of 1.270 μM .
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- HY-153692
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DNA/RNA Synthesis
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Cancer
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WRN inhibitor 1 (example 7) is a Wemer Syndrome ATP dependent helicase enzyme (WRN) inhibitor that inhibits WRN helicase domain activity. WRN inhibitor 1 has the potential to study cancer .
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- HY-160854
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin inhibitor 43 (Compound 29) has significant antitumor activity. Tubulin inhibitor 43 inhibits the proliferation and growth of cancer cells by inhibiting the activity of β-microtubulin, and finally induces apoptosis .
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- HY-146387
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Sirtuin
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Neurological Disease
Cancer
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SIRT5 inhibitor 3 (compound 46) is a potent and competitive SIRT5 inhibitor with an IC50 value of 5.9 μM. SIRT5 inhibitor 3 can inhibit SIRT5 desuccinylation. SIRT5 inhibitor 3 can be used for researching cancer and neurodegenerative diseases .
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- HY-150697
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HIV
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Others
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HIV-1 inhibitor-44 (compound 11l) is a HIV-1 reverse transcriptase inhibitor. HIV-1 inhibitor-44 shows inhibitory activity against wild-type HIV-1 strain with an EC50 value of 0.209 μM .
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- HY-125218
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ITK7
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PARP
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Cancer
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PARP11 inhibitor ITK7 (ITK7) is a potent and selective PARP11 inhibitor. PARP11 inhibitor ITK7 can potently inhibit PARP11 with an IC50 value of 14 nM. PARP11 inhibitor ITK7 can be used for the research of cellular localization .
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- HY-149989
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Ack1
Akt
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Cancer
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Ack1 inhibitor 1 is a potent, selective, and orally active inhibitor of ACK1 kinase with an IC50 value of 2.1 nM. Ack1 inhibitor 1 inhibits the phosphorylation of ACK1 and activation of downstream AKT. Ack1 inhibitor 1 has anti-tumor activity .
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- HY-156552
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- HY-161386
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DNA/RNA Synthesis
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Cancer
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WRN inhibitor 7 (Compound h6) is a WRN inhibitor. WRN inhibitor 7 effectively inhibits WRN's helicase and ATPase activity (IC50: 9.8 μM and 15.8 μM respectively). WRN inhibitor 7 can be used for research of microsatellite instable (MSI) cancers .
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- HY-164662
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mTOR
PI3K
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Cancer
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mTOR inhibitor-24 (comounp 9d) is a mTOR inhibitor, with IC50s of 0.34 nM (mTOR) and 324 nM (PI3K-α) respectively. mTOR inhibitor-24 inhibtis LNCaP cell proliferation (IC50: 180 nM) .
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- HY-159984
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HIV
|
Infection
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HIV-1 inhibitor-78 (compound 15f) is a potent and broad-spectrum non-nucleoside reverse transcriptase inhibitor, with an EC50 of 3 nM for wild-type HIV-1. HIV-1 inhibitor-78 can be used for the research of HIV infection .
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- HY-128859
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Cytochrome P450
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Metabolic Disease
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EMT inhibitor-2 (Compound 1) inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively .
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- HY-148042
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HIV
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Infection
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HIV-1 inhibitor-47 is an inhibitor of HIV-1, and inhibits vif-dependent degradation of human APOBEC3G, with an IC50 value of 14.33 μM. HIV-1 inhibitor-47 also involves in derivatives of 1-(2-pyrimidinyl)piperazine synthesis, with potential antianxiety, antidepressant, and antipsychotic effect .
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- HY-153970
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URAT1
|
Inflammation/Immunology
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URAT1 inhibitor 7 (compound 10f) is a potent URAT1 inhibitor, with an IC50 of 12 nM. URAT1 inhibitor 7 exhibits microsomal stability (HLM <13 µL/min/mg). URAT1 inhibitor 7 also inhibits CYP2C9, with an IC50 of 4.2 μM. URAT1 inhibitor 7 can be used for gout research .
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- HY-163797
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DNA/RNA Synthesis
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Cancer
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WRN inhibitor 10 (Compound P24) is an inhibitor for the Werner helicase WRN with an IC50 of 1.1 nM. WRN inhibitor 10 inhibits the proliferation of cancer cell SW48 with IC50 of 39 nM. WRN inhibitor 10 exhibits good liver microsomal stability and film permeability. WRN inhibitor 10 exhibits good pharmacokinetic characteristics in CD-1 mice .
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- HY-147552
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HIV
|
Infection
|
|
HIV-1 inhibitor-35 (compound 74) is a potent HIV-1 inhibitor with EC50s of 80 nM and 70 nM for LTR and CMV in HEK293 cells, respectively. HIV-1 inhibitor-35 has inhibitory activity against liver cancer cell HepG2 with a CC50 of 40 nM. HIV-1 inhibitor-35 can be used as HIV-1 latency reversing agent .
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- HY-123982
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|
|
Others
|
Neurological Disease
|
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SOD1-Derlin-1 inhibitor-2 (compound 56-59) is an inhibitor of SOD1-Derlin-1 interaction. SOD1-Derlin-1 inhibitor-2 attenuates the interactions between Derlin-1 and SOD1 mut. SOD1-Derlin-1 inhibitor-2 can be used for the research of amyotrophic lateral sclerosis (ALS) .
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-
- HY-149350
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|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-57 (Compound 12g) is a HIV inhibitor. HIV-1 inhibitor-57 is active against wild-type and five prevalent NNRTI-resistant HIV-1 strains with EC50 values ranging from 0.024 to 0.0010 μM. HIV-1 inhibitor-57 forms additional interactions with residues around the binding site in HIV-1 RT .
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- HY-122912
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ALDH1Ai 673A
|
Aldehyde Dehydrogenase (ALDH)
Necroptosis
|
Cancer
|
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ALDH1A inhibitor 673A is an ALDH1A inhibitor. ALDH1A inhibitor 673A inhibits all three ALDH1A family members (IC50: 246 nM, 230 nM, 348 nM for ALDH1A1, ALDH1A2, ALDH1A3 respectively. ALDH1A inhibitor 673A induces necroptotic cell death preferentially in CD133+ ovarian CSCs. ALDH1A inhibitor 673A also inhibits chemotherapy-resistant tumor growth .
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