Formulation: A crystalline solid
Formal Name: 1-[2,4-dichloro-3-(trifluoromethyl)phenyl]-1H-1,2,3-triazole
Purity: ≥98%
Formula Markup: C9H4Cl2F3N3
Formula Weight: 282,1
Shelf life (days): 730
CAS Number: 2411969-39-4
Notes: ARUK3001185 is an inhibitor of palmitoleoyl-protein carboxylesterase NOTUM (IC50 = 6.7 nM), an enzyme involved in the deacylation of Wnt.{69197} 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, α4β2 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).
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