Wnt-C59 is a potent (IC50 = 74 pmol/L) inhibitor of Porcupine (PORCN), a Wnt-acyltransferase. 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. Wnt-C59 was able to efficiently differentiate pluripotent stem cells into cortical neurons (CTIP2+/COUP-TF1). Wnt-C59 was also able to dramatically attenuate kidney fibrosis via inhibition of collagen mRNA expression and expression of inflammatory cytokines.
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