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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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FXR agonist
WAY-362450 is a highly potent, selective, and orally bioavailable farnesoid X receptor (FXR) agonist (EC50: 4 nM, eff=149%).
- Dong-Hyun Kim, .et al. , Cell Death Dis, 2021, Apr; 12(4): 320 PMID: 33767132
- Dong-Hyun Kim, .et al. , FASEB J, 2019, Jul 12:fj201900325R PMID: 31298930
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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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LXR-like receptors agonist
GW3965 HCl is a selective and orally active liver X receptor (LXR) full agonist.- Mohácsik P, .et al. , Endocrinology, 2018, Feb 1;159(2):1159-1171 PMID: 29253128
- Pencheva N, .et al. , Cell., 2014, 156(5):986-1001 PMID: 24581497
- Bin Dong, .et al. , J Lipid Res., 2013, May; 54(5): 1241-1254 PMID: 23427282
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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). -
CYP3A Inhibitor
Cobicistat is a potent inhibitor of cytochrome P450 3A enzymes, including the important CYP3A4 subtype. It also inhibits intestinal transport proteins, increasing the overall absorption of several HIV medications, including atazanavir, darunavir and tenofovir alafenamide fumarate. -
PDE4 Inhibitor
Apremilast, a novel PDE4 inhibitor, inhibits spontaneous production of tumour necrosis factor-alpha from human rheumatoid synovial cells and ameliorates experimental arthritis.- Higuchi T, .et al. , Research Square, 2023, Mar 02
- Adarotene belongs to the so-called class of atypical retinoids. The presence of the phenolic hydroxyl group on Adarotene structure allows a rapid O-glucuronidation as a major mechanism of elimination of the drug, favoring a fast excretion of its glucuronide metabolite in the urines.
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ACE inhibitor/Beta blocker
Moxonidine is a new-generation centrally-acting antihypertensive drug. It may have a role when thiazides, beta-blockers, ACE inhibitors and calcium channel blockers are not appropriate or have failed to control blood pressure. In addition, it demonstrates favourable effects on parameters of the insulin resistance syndrome, apparently independent of blood pressure reduction. -
PDE-2 Inhibitor
BAY 60-7550 is a potent PDE2 inhibitor with IC50 values of 2.0 nM (bovine) and 4.7 nM (human). - Calcifediol is a major circulating metabolite of vitamin D3 and acts as a competitive inhibitor with an apparent Ki of 3.9 μM. It also suppresses PTH secretion and mRNA (ED50=2 nM)
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Collagen proline hydroxylase inhibitor
Collagen proline hydroxylase inhibitor is a collagen proline hydroxylase inhibitor. -
CETP inhibitor
Evacetrapib (LY2484595) is a potent and selective inhibitor of CETP with IC50 of 5.5 nM, elevates HDL cholesterol without increases in aldosterone or blood pressure. Phase 3.- Phenix J, .et al. , bioRxiv, 2023, Feb 22
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SGK1 inhibitor
EMD638683 R-Form is the R-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM. -
SGK1 inhibitor
EMD638683 S-Form is the S-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM. -
Hsp90 inhibitor
Ganetespib is a potent, synthetic, small molecule inhibitor of Hsp90, a chaperone protein that is essential to the function of certain other proteins that drive the growth, proliferation, and survival of many different types of cancer.- Dilay Karademir, .et al. , Med Oncol, 2023, Jul 11;40(8):234 PMID: 37432531
- Tung-Yun Wu, .et al. , J Adv Res, 2022, Jun 22;S2090-1232(22)00148-5 PMID: 35752438
- Aykut Ozgur, .et al. , J Chemother, 2021, Apr 2;1-10 PMID: 33794753
- Michael Heider, .et al. , Mol Cell, 2021, Mar 18;81(6):1170-1186 PMID: 33571422
- Kosinsky RL, .et al. , Cell Death Dis, 2019, Dec 4;10(12):911 PMID: 31801945
- Yamada-Kanazawa S, .et al. , Br J Dermatol, 2017, Aug;177(2):456-469 PMID: 28078663
- Hiroki Murano, .et al. , Plant Biotechnol Rep, 2017, 11:107-113
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SCD inhibitor
MK-8245 is a Liver-Targeted Stearoyl-CoA Desaturase (SCD) Inhibitor. MK-8245 is useful for the Treatment of Diabetes and Dyslipidemia.- Miyayama Y, .et al. , Microbiol Immunol, 2019, Dec 19 PMID: 31854467
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Androgen Receptor antagonist
Cyproterone acetate is a synthetic derivative of 17-hydroxyprogesterone, and acts as an androgen receptor antagonist as well as a weak progesterone receptor agonist with weak progestational and glucocorticoid activity. - Ercalcitriol (1α,25-Dihydroxy Vitamin D2) is an active metabolite of vitamin D2.
- Luliconazole is an azole antifungal indicated for the topical treatment of interdigital tinea pedis.
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Vitamin D Analog
Lexacalcitol (KH1060) is over 100 times more active than 1alpha,25-dihydroxyvitamin D3 [1alpha,25-(OH)2D3], as judged by in vitro antiproliferative and cell differentiating assays. -
factor Xa inhibitor
Otamixaban(FXV 673) is an intravenous direct factor Xa inhibitor.- Tim Hempel, .et al. , Chemical Science, 2021, 12, 12600-12609
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DHFR inhibitor
Pralatrexate is an antifolate (a folate analogue metabolic inhibitor) designed to accumulate preferentially in cancer cells. -
DGAT1 Inhibitor
PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM. - Paricalcitol is a drug used for the prevention and treatment of secondary hyperparathyroidism (excessive secretion of parathyroid hormone) associated with chronic renal failure.
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Adenosine deaminase inhibitor
Pentostatin is an irreversible inhibitor of adenosine deaminase (Ki = 2.5 pM).- Lifang Han, .et al. , Cell Rep, 2022, May 31;39(9) PMID: 35649375
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PPAR-γ antagonist
T0070907 was identified as a potent and selective PPARgamma antagonist. With an apparent binding affinity (concentration at 50% inhibition of [(3)H]rosiglitazone binding or IC(50)) of 1 nm, T0070907 covalently modifies PPARgamma on cysteine 313 in helix 3 of human PPARgamma2. -
RARα agonist
Tamibarotene is a retinoic acid receptor α (RARα) agonist that induces differentiation (ED50 = 0.79 nM) and apoptosis of HL-60 cells in vitro. -
PDE1 inhibitor
Vinpocetine is a Ca2+-calmodulin-dependent phosphodiesterase I (PDE1) inhibitor. -
anticancer and radioprotection agent
Geniposidic acid is an effective anticancer and radioprotection agent. -
antitumor agent
Lonidamine (AF-1890), an antitumor agent, is a hexokinase, mitochondrial pyruvate carrier (Ki 2.5 μM in isolated rat liver mitochondria) and plasma membrane monocarboxylate transporters inhibitor, which also inhibits mitochondrial complex II. - Levothyroxine, also L-thyroxine or T4, is a synthetic form of the thyroid hormone thyroxine, which is normally secreted by the follicular cells of the thyroid gland.