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} LGK974 is a potent and specific small molecule inhibitor of PORCN (IC50 = 0.4 nM).{27368} It greatly reduces Wnt secretion without decreasing its synthesis and without increasing cytotoxicity.{27368} LGK974 is orally bioavailable in mice and induces tumor regression in mouse breast tumors produced by mammary tumor virus-driven Wnt1 signaling.{27368} It also blocks carcinogenesis in other Wnt-related tumors at doses that have limited impact on stem cell renewal.{27368,27367,21934}