Wnt-C59 (C59) is a highly potent and orally active Porcupine (PORCN) inhibitor, inhibits WNT3A-mediated activation with IC50 of 74 pM. C59 inhibits the activity of all splice variants of murine PORCN. C59 inhibits PORCN acyltransferase activity and blocks activation of all evaluated human Wnts. C59 blocked progression of mammary tumors in MMTV-WNT1 transgenic mice while downregulating Wnt/β-catenin target genes.
