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CYP3A4 inhibitor
Posaconazole is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14?? demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours. -
MAO-B inhibitor
Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C. -
MAO-B inhibitor
Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C. -
Factor Xa inhibitor
Rivaroxaban is an oxazolidinone derivative optimized for inhibiting both free Factor Xa and Factor Xa bound in the prothrombinase complex.- Stefan Bittmann, .et al. , J Regen Biol Med, 2020, 2(2):1-3
- Daniël Verhoef, .et al. , Nat Commun, 2017, 8: 528 PMID: 28904343
- Mizuki Yamamoto, .et al. , Antimicrob Agents Chemother, 2016, Nov; 60(11): 6532-6539 PMID: 27550352
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PDE inhibitor
Roflumilast acts as a selective, long-acting inhibitor of the enzyme PDE-4.- Bo Liao, .et al. , Exp Ther Med, 2023, May 9;25(6):302 PMID: 37229319
- Zhongyuan Zhang, .et al. , Exp Ther Med, 2021, Dec;22(6):1398 PMID: 34650646
- Bing Zhong, .et al. , ACS Omega, 2021, Jan 26; 6(3): 2149-2155 PMID: 33521454
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HMG-CoA reductase inhibitor
Rosuvastatin (Crestor) is a member of the drug class of statins, used to treat high cholesterol and related conditions, and to prevent cardiovascular disease. Rosuvastatin is a competitive inhibitor of the enzyme HMG-CoA reductase, having a mechanism of action similar to that of other statins. -
PDE4 inhibitor
(S)-(+)-Rolipram ((+)-Rolipram) is a cyclic AMP(cAMP)-specific phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 1100 nM. (S)-(+)-Rolipram can suppresse tumor necrosis factor-alpha (TNFα) production by human mononuclear cells. -
MAO Inhibitor
Safinamide Mesylate is mesylate salt of Safinamide, which selectively and reversibly inhibits MAO-B with IC50 of 0.45 μM. -
PDE5 inhibitor
Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM. -
HMG-CoA reductase inhibitor
Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM. -
HDAC inhibitor
Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. -
Phospholipase inhibitor
Tanshinones are the major bioactive compounds of Salvia miltiorrhiza Bunge (Danshen) roots, which are used in many therapeutic remedies in Chinese traditional medicine.- Kumar R, .et al. , Mol Biol Rep, 2018, Oct 11 PMID: 30311125
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Hydroxylase inhibitor
Tetrahydropapaverine, one of the TIQs and an analogue of salsolinol and tetrahydropapaveroline, has been reported to have neurotoxic effects on dopamine neurons. -
FTase inhibitor
Tipifarnib (Zarnestra) is a farnesyltransferase inhibitor that inhibits the Ras kinase in a post translational modification step before the kinase pathway becomes hyperactive.- Xiaoming Liu, .et al. , J Immunother Cancer, 2022, Apr;10(4):e004399 PMID: 35483745
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PDE-5 Inhibitor
Vardenafil is a PDE5 inhibitor used for treating erectile dysfunction. -
CYP17 inhibitor
Voriconazole (Vfend) is a triazole antifungal agent that is available as a lyophilized powder for solution for intravenous infusion. -
PDE Inhibitor
Ibudilast, a pharmacologic phosphodiesterase inhibitor, prevents human immunodeficiency Virus-1 Tat-Mediated activation of microglial cells. -
Hsp90 inhibitor
Geldanamycin binds to the ATP site of Hsp90 (Kd = 1.2 μM) and inhibits its chaperone activity.- Michael Heider, .et al. , Mol Cell, 2021, Mar 18;81(6):1170-1186 PMID: 33571422
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CYP17A1 inhibitor
TAK-700 (Orteronel) is an oral, non-steroidal androgen synthesis inhibitor that selectively inhibits the 17,20 lyase enzyme. -
FAAH inhibitor
URB597 is a relatively selective inhibitor of the enzyme fatty acid amide hydrolase (FAAH).- Lakhan S Khara, .et al. , J Exp Biol, 2022, May 1;225(9):jeb244146 PMID: 35438163
- Md Shah Sufian, .et al. , J Exp Biol, 2021, 21 JUNE
- Toshihiko Tsutsumi, .et al. , Biochim Biophys Acta Mol Cell Biol Lipids, 2020, Sep;1865(9):158761 PMID: 32629025
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CYP17 inhibitor
Abiraterone acetate (CB7630) is an orally active acetate ester of the steroidal compound Abiraterone with antiandrogen activity. Abiraterone inhibits 17 α-hydroxylase/C17,20 lyase (CYP17A1). -
HSP90 Inhibitor
AT13387 is a targeted inhibitor of Hsp90,inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival.- Boucherat O, .et al. , Am J Respir Crit Care Med, 2018, Jul 1;198(1):90-103 PMID: 29394093
- Olivier Boucherat, .et al. , Sci Rep, 2017, 7: 4546 PMID: 28674407
- Hiroki Murano, .et al. , Plant Biotechnol Rep, 2017, 11:107-113
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Hsp90 inhibitor
PF-04929113 (SNX-5422) is orally bioavailable heat shock protein 90 (Hsp90) inhibitor.- Henry Aceros, .et al. , Life Sci, 2019, 2019 PMID: 30986447
- Hiroki Murano, .et al. , Plant Biotechnol Rep, 2017, 11:107-113
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CETP inhibitor
Anacetrapib (MK-0859) is a CETP inhibitor being developed to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease. -
MAO B inhibitor
Rasagiline is a selective irreversible inhibitor of MAO-B (monoamine oxidase-B). -
HMG-CoA reductase inhibitor
Rosuvastatin is a member of the drug class of statins, used to treat high cholesterol and related conditions, and to prevent cardiovascular disease. -
Hsp90 Inhibitor
PU-H71 is a potent Hsp90 inhibitor (IC50 = 50 nM).- Michael Heider, .et al. , Mol Cell, 2021, Mar 18;81(6):1170-1186 PMID: 33571422
- Kale S, .et al. , Naunyn Schmiedebergs Arch Pharmacol, 2019, Sep 14 PMID: 31522240
- Hiroki Murano, .et al. , Plant Biotechnol Rep, 2017, 11:107-113
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CYP17 inhibitor
TOK-001 (Galeterone) is both an androgen receptor antagonist and CYP17A1 inhibitor. -
DBH inhibitor
Nepicastat hydrochloride is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine.
- Melina C Acosta, .et al. , Horm Behav, 2022, Jan;137:105086 PMID: 34808463
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HMG-CoA Reductase inhibitor
Clinofibrate is a lipid clearing agent that appears to modify lipid metabolism, diminishing the steroid induced accumulation of lipids within osteocytes. It also can effectively reduce the plasma fibrinogen level.
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Hsp90 inhibitor
SNX-2112 is a heat shock protein 90 (Hsp90) inhibitor with anticancer properties currently in clinical trials. SNX-2112 induced autophagy in a time- and dose-dependent manner via Akt/mTOR/p70S6K inhibition. SNX-2112 induces significant apoptosis and autophagy in human melanoma A-375 cells, and may be an effective targeted therapy agent
- Michael Heider, .et al. , Mol Cell, 2021, Mar 18;81(6):1170-1186 PMID: 33571422
- Hiroki Murano, .et al. , Plant Biotechnol Rep, 2017, 11:107-113
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PDE10A inhibitor
PF-2545920 is a phosphodiesterase inhibitor selective for the PDE10A subtype.
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DGAT-1 inhibitor
A 922500 is a diacylglycerol acyltransferase 1 (DGAT-1) inhibitor (IC50 values are 7 and 24 nM at human and mouse DGAT-1 respectively).
- SIFEI HAN, .et al. , J Pharm Sci, 2016, Feb;105(2):786-796 PMID: 6540595
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CETP inhibitor
JTT-705 (Dalcetrapib) is a CETP inhibitor.Inhibition of CETP is a target to increase HDL-cholesterol and potentially reduce atherosclerosis. -
SREBP inhibitor
PF 429242 is a reversible, competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease.- Kai Xue, .et al. , Oxid Med Cell Longev, 2021, Nov 26;2021:5710440 PMID: 34873430
- Tong-bing Wang, .et al. , Cell Death Dis, 2021, Aug; 12(8): 717 PMID: 34285190
- Shiying Xie, .et al. , Am J Physiol Renal Physiol, 2020, Aug 31 PMID: 32865015
- Yang PM, .et al. , Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
- Hui Fang, .et al. , Am J Physiol Cell Physiol, 2017, Dec 1; 313(6): C632-C643 PMID: 28903918
- Tsutomu Nakagawa, .et al. , J Biochem, 2016, Apr 1;161(4):369-379 PMID: 28013223
- Shimada S, .et al. , Virology, 2015, Aug;482:19-27 PMID: 25817401
- Jan H. Reiling, .et al. , Nat Cell Biol., 2013, 15(12): 1473-1485 PMID: 24185178
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CETP inhibitor
Torcetrapib (CP-529414) is a CETP inhibitor with IC50 of 37 nM. -
Hsp90 inhibitor
IPI-504 is a novel, water-soluble, potent inhibitor of heat-shock protein 90 (Hsp90).