GNF-6231 is a potent, orally active and selective Porcupine inhibitor with IC50=0.8 nM (Wnt3a Co-culture RGA). GNF-6231 demonstrated excellent pathway inhibition and induced robust antitumor efficacy in a mouse MMTV-WNT1 xenograft tumor model. Blockade of aberrant Wnt signaling is an attractive therapeutic approach in multiple cancers. Wnt signaling is tightly controlled during cellular proliferation, differentiation, and embryonic morphogenesis. Aberrant activation of this pathway plays a critical role in a variety of cancers, such as cutaneous squamous cell carcinoma (SCC), breast cancer, and colorectal cancer.
