Metabolism

CH-223191 is a ligand-selective antagonist of the Ah (Dioxin) receptor.

Gemfibrozil (Lopid) is a compound used to lower lipid levels.

PF 429242 is a reversible, competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease.

Elafibranor is an agonist of the peroxisome proliferator-activated Receptor-α and -δ, induces resolution of nonalcoholic steatohepatitis without fibrosis worsening.

Monoammoniumglycyrrhizinate is a constituent of the licorice root that has vital anti-viral activities that have been shown to inhibit the expression of 11_?HSD2 (11_?hydroxysteroid dehydrogenase type 2) via an indirect mechanism.

AS1842856 is a cell-permeable inhibitor that blocks the transcription activity of Foxo1 with IC50 of 33 nM. It could directly bind to the active Foxo1, but not the Ser256-phosphorylated form.

Tanshinones are the major bioactive compounds of Salvia miltiorrhiza Bunge (Danshen) roots, which are used in many therapeutic remedies in Chinese traditional medicine.

JZL195 is a selective and efficacious dual FAAH/MAGL inhibitor with IC50 of 13 nM and 19 nM for mouse brain FAAH and MAGL respectively.

URB597 is a relatively selective inhibitor of the enzyme fatty acid amide hydrolase (FAAH).

JZL184 is a potent and selective monoacylglycerol lipase (MAGL) inhibitor. Blocks hydrolysis of the endocannabinoid 2-arachidonyl glycerol (2-AG) in vivo in the mouse brain (IC50 = 8 nM).

VBY-825 is a novel, reversible cathepsin inhibitor with high potency against cathepsins B, L, S and V.

Abiraterone (CB-7598) inhibits 17 α-hydroxylase/C17,20 lyase (CYP17A1), an enzyme which is expressed in testicular, adrenal, and prostatic tumor tissues.

Trilostane is an inhibitor of 3??-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome.

Pentostatin is an irreversible inhibitor of adenosine deaminase (Ki = 2.5 pM).

AUY922 (NVP-AUY922) is highly potent and oral inhibitor of Hsp90 with IC50=21 nM in Hsp90 FP binding assay and inhibits proliferation of various human cancer cell lines in vitro, with GI50 average 9 nM.

VER 155008 is a small molecule, ATP-derivative inhibitor of HSP70 (IC50 = 500 nM).

Moclobemide is a reversible and selective inhibitor of monoamine oxidase A (MAO-A).

WNK463 is an orally bioavailable pan-WNK-kinase inhibitor.

Orlistat is a general lipase inhibitor with IC50 of 122 ng/ml for PL from human duodenal juice.  Orlistat is also an inhibitor of fatty acid synthase (FASN), is used orally for long-term research of obesity. Anti-atherosclerotic effect. 

Edoxaban(DU-176) is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention.

Capecitabine is a prodrug, that is enzymatically converted to 5-fluorouracil in the tumor, where it inhibits DNA synthesis and slows growth of tumor tissue. The activation of capecitabine follows a pathway with three enzymatic steps and two intermediary metabolites, 5'-deoxy-5-fluorocytidine (5'-DFCR) and 5'-deoxy-5-fluorouridine (5'-DFUR), to form 5-fluorouracil.

17-DMAG is a water-soluble analog of 17-AAG and geldanamycin that binds the ATP binding site of Hsp90 and inhibits its chaperone activity. Displays more potent antitumor activity than 17-AAG.

Erastin is a cell-permeable piperazinyl-quinazolinone compound that exhibits oncogene-selective lethality in cells with H-Ras mutations.

CA-074 methyl ester is a cell-permeable analog of CA-074 that acts as an irreversible cathepsin B inhibitor. CA-074 methyl ester is reported to inhibit bone resorption in rodent models and shown to inhibit B16 melanoma cell invasion in vitro.

HSP990 is an orally bioavailable inhibitor of human heat-shock protein 90 (Hsp90) with potential antineoplastic activity.

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

PU-H71 is a potent Hsp90 inhibitor (IC50 = 50 nM).

MK-8245 is a Liver-Targeted Stearoyl-CoA Desaturase (SCD) Inhibitor. MK-8245 is useful for the Treatment of Diabetes and Dyslipidemia.

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.

Enasidenib is a potent and selective IDH2 inhibitor with potential anticancer activity (IDH2 = Isocitrate dehydrogenase 2).

GW3965 is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM, respectively.

MPC-3100 is an orally bioavailable, synthetic, second-generation small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.

BIIB021 is an oral fully synthetic Hsp90 inhibitor that selectively and potently inhibits the molecular chaperone Hsp90 thereby inhibiting the proper assembly of multiple oncogenic proteins involved in tumor growth and survival.

ML-210??the most potent compound in the nitroisoxazole series?? is a selective covalent inhibitor of glutathione peroxidase 4 (GPX4) by binding the selenocysteine residue.

Aminopterin is an antineoplastic drug. It works as an enzyme inhibitor by competing for the folate binding site of the enzyme dihydrofolate reductase.

P7C3-A20 is a potent neuroprotective agent.

Mito-TEMPO is a mitochondria-targeted superoxide dismutase mimetic with superoxide and alkyl radical scavenging properties.

Disulfiram blocks the processing of alcohol in the body by inhibiting acetaldehyde dehydrogenase thus causing an unpleasant reaction when alcohol is consumed.

Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent.

MC-976 is an Vitamin D3 derivative.

CPI-613 is a racemic mixture of the enantiomers of a synthetic alpha-lipoic lipoic acid analogue with potential chemopreventive and antineoplastic activities.

Clofazimine is a rhimophenazine dye, originally developed for the treatment of tuberculosis, it has both antimicrobial and antiinflammatory activity, postulated mechanisms of action include intercalation of clofazimine with bacterial DNA and increasing levels of cellular phospholipase A2.

Tanshinone IIA (TIIA) is one of the major extracts obtained from Salvia miltiorrhiza BUNGE, which has anti-inflammatory and anti-apoptotic effects on many diseases.

Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects.

ENOblock (AP-III-a4) is a novel small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 uM); inhibit cancer cell metastasis in vivo.

L-Citrulline is an amino acid derived from ornithine in the catabolism of proline or glutamine and glutamate, or from l-arginine via arginine-citrulline pathway.

Hydroxyflutamide (Hydroxyniphtholide) is a metabolite of flutamide found to inhibit the proliferation of estradiol-induced growth of MCF-7 breast cancer cells.

BAY-876 is a potent and Selective GLUT1 Inhibitor. BAY-876 showed good metabolic stability in vitro and high oral bioavailability in vivo.

Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM.

Rolipram is a PDE4-inhibitor with IC50 = 2.0 μM.