LGK974 (WNT974) is a potent and specific small-molecule Porcupine (PORCN) inhibitor with IC50 of 1 nM in the PORCN radioligand binding assay.
WNT974 potently inhibits Wnt signaling with IC50 of 0.4 nM, with no major cytotoxicity.
WNT974 reduces Wnt-dependent LRP6 phosphorylation and the expression of Wnt target genes, such as AXIN2.
WNT974 is potent and efficacious in multiple tumor models at well-tolerated doses in vivo.
