2-(4-(2-Methylpyridin-4-Yl)Phenyl)-N-(4-(Pyridin-3-Yl)Phenyl)Acetamide 2-(4-(2-甲基吡啶-4-基)苯基)-N-(4-(吡啶-3-基)苯基)乙酰胺
CAS 1243243-89-1 MFCD343243891
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- Wnt-C59 is a potent porcupine (PORCN) inhibitor. Wnt-C59 inhibits PORCN activity in vitro at nanomolar concentrations, as assessed by inhibition of Wnt palmitoylation, Wnt interaction with the carrier protein Wntless/WLS, Wnt secretion, and Wnt activation of β-catenin reporter activity. In mice, Wnt-C59 displayed good bioavailability, as once daily oral administration was sufficient to maintain blood concentrations well above the IC(50). C59 blocked progression of mammary tumors in MMTV-WNT1 transgenic mice while downregulating Wnt/β-catenin target genes. Porcupine (PORCN) is a membrane bound O-acyltransferase that is required for Wnt palmitoylation, secretion, and biologic activity.
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