“Ligand-gated Ion Channels”的搜索结果
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CYP2C9 inhibitor
Sulfaphenazole is a specific inhibitor of CYP2C9 which blocks atherogenic and pro-inflammatory effects of linoleic acid (increase in oxidative stress and activation of AP-1) mediated by CYP2C9.
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MAO inhibitor
Pargyline hydrochloride is an irreversible inhibitor of monoamine oxidase (MAO) that is used clinically to treat moderate hypertension.
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PDE4B inhibitor
Ademetionine, also known as AdoMet; MSI-195; SAMe, S-adenosylmethionine, is a PDE4B inhibitor potentially for treatment of primary biliary cirrhosis and major depressive disorder.
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MAO-A inhibitor
Minaprine is a reversible inhibitor of MAO-A; weakly inhibit acetylcholinesterase; an antidepressant for treatment of depression.
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PDE5 inhibitor
Lodenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED).
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CETP inhibitor
CKD-519 is a selective and potent cholesteryl ester transfer protein (CETP) inhibitor being developed for the treatment of dyslipidemia to raise high-density lipoprotein cholesterol. Single doses of CKD-519 up to 400 mg were well tolerated and showed potent inhibition of CETP activity.
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FASN inhibitor
TVB-3166 is an orally-available, reversible, potent, and selective FASN inhibitor, inducing apoptosis, inhibiting anchorage-independent cell growth under lipid-rich conditions, and inhibiting in-vivo xenograft tumor growth.
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Hsp70 inhibitor
JG-98, an allosteric heat shock protein 70 (Hsp70) inhibitor, which binds tightly to a conserved site on Hsp70 and disrupts the Hsp70-Bag3 interaction. JG-98 shows anti-cancer activities affecting both cancer cells and tumor-associated macrophages.
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- Shivani Patel, .et al. Cytoplasmic proteotoxicity regulates HRI-dependent phosphorylation of eIF2α via the Hsp70-Bag3 module, iScience, 2022, Apr 22;25(5):104282 PMID: 35573186
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Hsp47 inhibitor
Col003 is a potent inhibitor of Hsp47, competitively binds to the collagen binding site on Hsp47 (IC50, 1.8 μM), and inhibits collagen secretion by destabilizing the collagen triple helix.
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CETP inhibitor
CETP-IN-3 (Compound 13) is an small molecule inhibitor of the plasma glycoprotein cholesterol ester transfer protein (CETP), elevating HDL-C through inhibition of CETP.
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HSP27 inhibitor
HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof.
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- Haruka Wakasa, .et al. Adverse Effects of High Temperature On Mammary Alveolar Development In Vitro, J Mammary Gland Biol Neoplasia, 2022, Jun;27(2):155-170 PMID: 35581442
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FASN inhibitor
TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC50 values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression.
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IDH1 inhibitor
DH1 Inhibitor 2 is a potent IDH1 inhibitor via a direct covalent modification of His315, with an IC50 of 110 nM.
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HSP90-calcineurin-NFAT inhibitor
YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathway against glioblastoma, directly binding to heat shock protein 90 (HSP90) with an IC50 of 820 nM on NFAT nuclear translocation.
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CYP3A4 enzyme inhibitor
Bergaptol is a hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM. Recent studies suggest that it may have antiproliferative and anticancer properties.
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factor Xa (FXa) inhibitor
Edoxaban(DU-176) is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention.
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PDE-5 inhibitor
Mirodenafil dihydrochloride (SK3530 dihydrochloride) is a phosphodiesterase type 5 (PDE-5) inhibitor developed for the treatment of erectile dysfunction.
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PDE-5 inhibitor
Mirodenafil(SK3530) is a phosphodiesterase type 5 (PDE-5) inhibitor developed for the treatment of erectile dysfunction.
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FAAH inhibitor
PF 750 is a selective and covalent fatty acid amide hydrolase (FAAH) inhibitor, with IC50s varied from 16.2-595 nM in different pre-incubation times. Covalently modifies the enzyme??s active site serine nucleophile.
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Hsp90 inhibitor
SNX-5422 Mesylate (PF-04929113 Mesylate), a prodrug of SNX-2112, is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37?nM.
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FASN inhibitor
HS-80 is an enantiomer of Fasnall, which is a selective fatty acid synthase (FASN) inhibitor. HS-80 is able to inhibit the incorporation of tritiated acetate into lipids with an IC50 of 7.13 μM.
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CYP450 dependent inhibitor
Liarozole dihydrochloride (R75251; R85246) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).
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nuclear export receptor CRM1 inhibitor
Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle.
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CYP17 lyase inhibitor
Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) that demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.
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PDE1 inhibitor
ITI-214 is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).
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picomolar PDE1 inhibitor
ITI-214 (free base) is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).
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