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
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
