Metabolism

17-AAG is an ansamycin antibiotic which acts as an anti-tumor agent. Specifically, 17-AAG binds and inhibits Hsp90.

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.

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

Methotrexate is a cytotoxic agent that inhibits thymidylate synthetase and de novo purine synthesis.

Acarbose is an anti-diabetic drug used to treat type 2 diabetes mellitus and, in some countries, prediabetes.

Acitretin is a second generation retinoid and is typically used for psoriasis.

Adapalene is a third-generation topical retinoid primarily used in the treatment of mild-moderate acne and is also used (off-label) to treat keratosis pilaris as well as other skin conditions.

Alizarin is novelly used as a staining agent in biological research because it stains free calcium and certain calcium compounds a red or light purple color.

Allopurinol is a purine analog; it is a structural isomer of hypoxanthine (a naturally occurring purine in the body) and is an inhibitor of the enzyme xanthine oxidase.

Aminophylline is a nonselective adenosine receptor antagonist and phosphodiesterase inhibitor capable of reversing ischemia-induced bradyasystole.

Mono-ammonium glycyrrhizinate(AMGZ) is a unique product derived from Licorice root and has an extremely sweet taste.

Apigenin, found in many plants, is a natural product belonging to the flavone class that is the aglycone of several naturally-occurring glycosides. Apigenin acts as a monoamine transporter activator, one of the few chemicals demonstrated to possess this property. Apigenin is a ligand for central benzodiazepine receptors that competitively inhibited the binding of flunitrazepam with a Ki of 4μM, exerting anxiolytic and slight sedative effects.

Apixaban is an anticoagulant for the prevention of venous thromboembolism and venous thromboembolic events.

Avasimibe (CI-1011) is an orally bioavailable Acyl-CoA:Cholesterol O-Acyltransferase (ACAT) inhibitor.

Baicalein is a flavonoid originally isolated from the roots of Scutellaria baicalensis Georgi. Baicalein inhibits lipid peroxidation, as assessed by production of TBARS, with an IC50 value of 5 µM.

Benserazid hydrochloride is an inhibitor of L-aromatic amino acid decarboxylase.

Berberine hydrochloride was novelly found that it has various beneficial effects on the cardiovascular system and significant anti-inflammatory activities. Berberine can effectively reduce intracellular superoxide levels in LPS-stimulated macrophages. Such a restoration of cellular redox by berberine is mediated by its selective inhibition of gp91phox expression and enhancement of SOD 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.

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.

Carbidopa inhibits aromatic-L-amino-acid decarboxylase, an enzyme important in the biosynthesis of L-tryptophan to serotonin and in the biosynthesis of L-DOPA to Dopamine (DA).

Carmofur is a pyrimidine analogue used as an antineoplastic agent. It is a derivative of fluorouracil.

Celastrol is a triterpenoid antioxidant compound isolated from the Chinese Thunder of God vine (T. wilfordii). In an isolated rat liver assay of lipid peroxidation, celastrol had an IC50 value of 7 µM, equivalent to about 15 times the antioxidant potency of α-tocopherol.

Chloramphenicol is a bacteriostatic antimicrobial.

Chlorpromazine is a dopamine antagonist of the typical antipsychotic class of medications possessing additional antiadrenergic, antiserotonergic, anticholinergic and antihistaminergic properties used to treat schizophrenia.

Cilomilast is orally active and acts as a selective Phosphodiesterase-4 inhibitor with antiinflammatory effects that target bronchoconstriction, mucus hypersecretion, and airway remodeling associated with COPD.

Cilostazol is a selective inhibitor of 3-type phosphodiesterase (PDE3) with therapeutic focus on cAMP.

Cladribine is a synthetic anti-cancer agent that mimics the nucleoside adenosine and thus inhibits the enzyme adenosine deaminase, which interferes with the cell's ability to process DNA.

Clarithromycin is a macrolide antibiotic. It prevents bacteria from growing by interfering with their protein synthesis.

Clofibrate increases the activity of extrahepatic lipoprotein lipase (LL), thereby increasing lipoprotein triglyceride lipolysis. Chylomicrons are degraded, VLDLs are converted to LDLs, and LDLs are converted to HDL.

Action of clotrimazole is against the division and growing of fungi.Clotrimazole alters the permeability of the fungal cell wall and inhibits the activity of enzymes within the cell. It specifically inhibits the biosynthesis of ergosterol and other sterols required for cell membrane production.

Non-opioid analgesic with muscle relaxant properties.

Daphnetin is a coumarin analog that acts as an inhibitor of several protein kinases. It inhibits EGFR kinase (IC50 = 7.67 μM), PKA (IC50 = 9.33 μM), and PKC (IC50 = 25 μM), in vitro. The inhibition of EGFR kinase by daphnetin was competitive to ATP and non-competitive to the peptide substrate. Also acts as a potent antioxidant and anti-malarial agent.

Decitabine is a hypomethylating agent.It hypomethylates DNA by inhibiting DNA methyltransferase.

Deferasirox is a rationally-designed oral iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor.

Diclofenamide (or dichlorphenamide) is a sulfonamide and a carbonic anhydrase inhibitor of the meta-Disulfamoylbenzene class.

Dipyridamole (Persantine) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.

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

Dorzolamide HCl is a carbonic anhydrase inhibitor. It is an anti-glaucoma agent and topically applied in the form of eye drops. Dorzolamide HCl is used to lower increased intraocular pressure in open-angle glaucoma and ocular hypertension.

Dyphylline is a xanthine derivative with bronchodilator and vasodilator effects. It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor.

Elesclomol induces oxidative stress by provoking a buildup of reactive oxygen species within cancer cells.

Enalapril is an angiotensin converting enzyme (ACE) inhibitor used in the treatment of hypertension and some types of chronic heart failure.

Enalaprilat is the active metabolite of enalapril. It is the first dicarboxylate-containing ACE inhibitor and was developed partly to overcome these limitations of captopril.

Glycyrrhetinic acid inhibits the enzymes (15-hydroxyprostaglandin dehydrogenase and delta-13-prostaglandin) that metabolize the prostaglandins PGE-2 and PGF-2α to their respective 15-keto-13,14-dihydro metabolites which are inactive.

Ezetimibe is a compound that lowers cholesterol. It acts by decreasing cholesterol absorption in the intestine. Ezetimibe localises at the brush border of the small intestine, where ezetimibe inhibits the absorption of cholesterol from the intestine.

Febuxostat is a non-purine inhibitor of xanthine oxidase (Ki = 1.2 nM).

Fenofibrate is a drug of the fibrate class. It is mainly used to reduce cholesterol levels in patients at risk of cardiovascular disease.

Fludarabine or fludarabine phosphate (Fludara) is a chemotherapy drug used in the treatment of hematological malignancies (cancers of blood cells such as leukemias and lymphomas) .Fludarabine inhibits DNA synthesis by interfering with ribonucleotide reductase and DNA polymerase. It is active against both dividing and resting cells.

Fludarabine or fludarabine phosphate (Fludara) is a chemotherapy drug used in the treatment of hematological malignancies (cancers of blood cells such as leukemias and lymphomas) .Fludarabine inhibits DNA synthesis by interfering with ribonucleotide reductase and DNA polymerase. It is active against both dividing and resting cells.

Fluvastatin sodium (XU 62320) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM.

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