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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: Levophed
Noradrenaline bitartrate monohydrate (Levophed) is a direct alpha-adrenergic receptors stimulator.
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: CK-2017357
Tirasemtiv amplifies skeletal muscle response to nerve activation in humans.
Synonyms: LYC30937
Parimifasor (LYC30937) is an immunomodulator, with anti-inflammatory activity.
Bioymifi is a potent and selective small molecule agonist of DR5 that directly targets DR5, specifically binds the ECD of DR5 (Kd ~1.2 μM), and induces the formation of DR5 aggregates and DR5 activation.
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.
TRX-818 is a new, potent and multi-targeted anti-cancer agent in numerous human cancer cell lines.
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.
Synonyms: OE312; AJ 266447; AJ-26647; Carglumic Acid.
Carglumic acid (N-Carbamyl-L-glutamic acid), a functional analogue of N-acetylglutamate (NAG) and a carbamoyl phosphate synthetase 1 (CPS1) activator, is used to treat acute and chronic hyperammonemia associated with NAG synthase (NAGS) deficiency.
Synonyms: Benfluorex HCl; Lipophoral; Mediator; JP 992; EINECS 245-801-8; Mediaxal; Balans
Benfluorex hydrochloride (JP-992 hydrochloride) is a hepatic nuclear factor 4 alpha (HNF4α) activator.
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.
L-Lysine thioctate is a substrate of lipoamidase.
G6PD activator AG1 is a glucose-6-phosphate dehydrogenase (G6PD) activator with an EC50 of 3 μ, extracted from patent WO2019023264A1, compound AG1.
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).
Synonyms: Hydroxypropyl tetrahydropyrantriol
Pro-xylane (Hydroxypropyl tetrahydropyrantriol) is a biologically active C-glycoside in aqueous media, acts as an activator of glycosaminoglycans (GAGs) biosynthesis.
N6-Methyladenosine 5'-monophosphate disodium salt is an activator of glycogen phosphorylase b, with a Ka value of 22 µM. N6-Methyladenosine 5'-monophosphate disodium salt is a non-competitive rat adenylate kinase II inhibitor.
TM-25659 is a transcriptional co-activator with PDZ-binding motif (TAZ) modulator. Anti-osteoporotic and anti-obesity activities.
