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Other Inhibitors groups bioactive small molecules whose targets fall outside the pathway categories of this catalogue. The compounds have not yet been assigned to target categories, so the range is broad and uneven. Streptozotocin, a glucosamine-nitrosourea compound used to induce experimental diabetes in rodents, sits beside the O-GlcNAcase inhibitor Thiamet G. Exherin is an N-cadherin antagonist, and AdipoRon is an agonist of adiponectin receptors 1 and 2 (AdipoR1 and AdipoR2). Plant compounds such as the isoflavone daidzein are also included. Despite the category name, not every compound is an inhibitor, as the AdipoRon example shows. Compounds with a well-defined target are usually listed in the matching pathway or target category.
Synonyms: Org-9426
Rocuronium (Org-9426) is an aminosteroid non-depolarizing neuromuscular blocker or muscle relaxant used in modern anaesthesia.
TOK-8801 is a synthesized dihydroimidazothiazole carboxamide and is under development as an immunomodulator.
UK-157147 is a substrate for UDP-glucuronosyltransferases (UGT1A1) with a Km value of 105 μM.
Synonyms: LYC30937
Parimifasor (LYC30937) is an immunomodulator, with anti-inflammatory activity.
Synonyms: Firefly Luciferin
D-Luciferin is a popular bioluminescent substrate of luciferase in the presence of ATP, used in luciferase-based bioluminescence imaging and cell-based high-throughput screening applications.
Plumbagin, exhibits cytotoxicity in rodent models of carcinogenesis and carcinoma; has antifungal, antiviral, and antibacterial action.
Synonyms: Tretazicar
CB1954 is a anticancer prodrug that is converted in the presence of the enzyme NQO2 and co-substrate caricotamide ( EP-0152R) (EP) into a potent cytotoxic bifunctional alkylating agent.It can be activated by NAD(P)H quinone oxidoreductase 2.
Synonyms: CLZN
Coelenterazine is a luminescent enzyme substrate, used for monitoring reporter genes in BRET, ELISA and HTS techniques.
RETF-4NA is a chymase substrate peptide that is cleaved more avidly by α2-macroglobulin-bound chymase than the free, unbound form.
Synonyms: p-Aminohippuric acid
4-Aminohippuric acid is a typical substrate of organic anion transport systems.
PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively.
DMT1 blocker 1 is a blocker of divalent metal transporter 1 (DMT1) with an IC50 of 0.64 μM, is expected to block iron uptake by enterocytes in vivo.
L-Lysine thioctate is a substrate of lipoamidase.
Synonyms: 2'-Deoxy-2'-fluoro-5-Methyluridine
2'-Fluorothymidine (2'-Fluoro-2'-deoxythymidine), a bioisostere of both thymidine (TdR) and methyluridine, is a putative highly selective substrate for thymidine kinase type 2 (TK2).
Velaresol, also known as BW12C or BW12C79, is a oxyhaemoglobin stabilizer.
