Wnt-C59, Highly potent PORCN inhibitor, Each

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Wnt-C59 is a highly potent inhibitor of MBOAT (membrane-bound O-acyltranferase) family member Porcupine (PORCN) (IC50 = 74 pM) that mediates WNT palmitoylation and secretion. Wnt-C59 potently inhibits the processing of both canonical (1, 2, 3a, 6, 7b, 8a, 9a, 9b, 10) and non-canonical (4, 5a, 11, 16) Wnt subtypes. Wnt-C59 blocks progression of mammary tumors in MMTV-WNT1 transgenic mice and downregulates Wnt/β-catenin target genes. Wnt-C59 treated tumors show a decrease in β-catenincatenin, CyclinD1 and c-Myc. Wnt-C59 induces cardiomyocyte differentiation from human iPSCs following culture with CHIR 99021 (Cat. No. 4423). Wnt-C59 efficiently induces neural differentiation of CTIP2 /COUP-TF1- cells from PSCs in culture. When grafted into the cortex of adult mice, develop abundant axonal fiber extension toward the spinal cord. Cell permeable and orally bioavailable.