GNF-6231 (GNF6231) is a potent, selective and orally bioavailable Porcupine (PORCN) inhibitor with IC50 of 0.8 nM.
GNF-6231 has no appreciable activities for more than 200 off-targets, and IC50 of >10 uM against all CYP isoforms.
GNF-6231 reduces Axin2 mRNA levels and inhibits Wnt secretion and pathway activation, induces robust antitumor efficacy in a mouse MMTV-WNT1 xenograft tumor model.
