1243243-89-1

Wnt-C59 (1243243-89-1) is a potent (IC50 = 74 pmol/L) inhibitor of Porcupine (PORCN), a Wnt-acyltransferase.1 Blockage of Wnt-acyltransferase prevents secretion of all Wnt isoforms.? It was able to block progression of mammary tumors in MMTV-WNT1 transgenic mice.1? Wnt-C59 strongly inhibited the growth of intestinal neoplasia in RZ-mutant mice.2? Wnt-C59 was able to efficiently differentiate pluripotent stem cells into cortical neurons (CTIP2+/COUP-TF1).3? Wnt-C59 was also able to dramatically attenuate kidney fibrosis via inhibition of collagen mRNA expression and expression of inflammatory cytokines.4

Wnt-C59 is a porcupine homolog – Drosophila (PORCN) inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase.

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1) Proffitt et al. (2013), Pharmacological Inhibition of the Wnt Acyltransferase PORCN Prevents Growth of Wnt-Driven Mammary Cancer; Cancer Res., 73 502 2) Koo et al. (2015), Porcupine inhibitor suppresses paracrine Wnt-driven growth of Rnf43;Znrf3-mutant neoplasia; Proc. Natl. Acad. Sci.USA, 112 7548 3) Motono et al. (2016), Wnt-C59, a Small-Molecule Wnt Inhibitor, Efficiently Induces Anterior Cortex That Includes Cortical Motor Neurons From Human Pluripotent Stem Cells; Stem Cells Transl.Med., 5 552 4) Madan et al. (2016), Experimental inhibition of porcupine-mediated Wnt O-acylation attenuates kidney fibrosis; Kidney Int., 89 1062