产品描述:
Porcupine (PORCN) is a membrane bound O-acyltransferase that mediates palmitoylation of Wnt family proteins.{27064} This step is required for secretion and biologic activity of Wnt proteins, which have roles in embryonic development and cancer.{27064,27062} IWP-L6 is a potent inhibitor of PORCN (EC50 = 0.5 nM).{27202} It suppresses the phosphorylation of disheveled 2 in HEK293 cells. IWP-L6 displays high stability in human plasma (t1/2 > 24 hours) and in zebrafish, but it is much less stable in plasma from mice and rats.{27202} In zebrafish, IWP-L6 blocks Wnt/β-catenin-dependent developmental processes, including tailfin regeneration and posterior axis formation.{27202} It also completely prevents branching morphogenesis in cultured mouse embryonic kidneys at doses of 50 nM and above, indicating complete inhibition of Wnt signaling.{27202}