Description:

IWP-2, N-(6-Methyl-2-benzothiazolyl)-2-[(3,4,6,7-tetrahydro-4-oxo-3-phenylthieno[3,2-d]pyrimidin-2-yl)thio]-acetamide, is a specific inhibitor of the O-acyltransferase Porcupine with IC50=27nM (Ref.). Inhibition blocks the production of Wnt proteins that require fatty acid modifications, thus disrupting Wnt-dependent signaling. Porcupine inhibitor represent a novel class of potential therapeutics for cancer and other WNT dependent diseases.

Ref: B. Chen, et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat. Chem. Biol. 5, 100 (2009)

Biological Activity:

In a cell-based assay measuring the activation of the TCF reporter gene, this compound gives IC50 of 30 nM.

CAS: 686770-61-6