ARUK3001185

ARUK3001185 is an inhibitor of palmitoleoyl-protein carboxylesterase NOTUM (IC50 = 6.7 nM), an enzyme involved in the deacylation of Wnt. It is selective for NOTUM over a panel of 39 serine hydrolases and 485 kinases, including casein kinase 1 (CK1) and glycogen synthase kinase 3 (GSK3), at 10 µM and a panel of 47 receptors, ion channels, transporters, and enzymes at 30 µM, but does inhibit the serotonin (5-HT) receptor subtype 5-HT3A, alpha4beta2 subunit-containing nicotinic acetylcholine receptors (nAChRs), and monoamine oxidase A (MAO-A, IC50s = 4.5, 10, and 28 µM, respectively). ARUK3001185 prevents NOTUM-induced decreases in Wnt3a signaling in a cell-based reporter assay (EC50 = 110 nM).Formal Name: 1-[2,4-dichloro-3-(trifluoromethyl)phenyl]-1H-1,2,3-triazole. CAS Number: 2411969-39-4. Synonyms: 1-Phenyl-1H-1,2,3-triazole 1. Molecular Formula: C9H4Cl2F3N3. Formula Weight: 282.1. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 5 mg/ml. lambdamax: 288 nm. SMILES: FC(F)(C1=C(Cl)C(N2C=CN=N2)=CC=C1Cl)F. InChi Code: InChI=1S/C9H4Cl2F3N3/c10-5-1-2-6(17-4-3-15-16-17)8(11)7(5)9(12,13)14/h1-4H. InChi Key: XVFXHCLMGYJAQI-UHFFFAOYSA-N.