G007-LK is a potent, specific, metabolically stable TNKS1/2 inhibitor with IC50 of 46 nM and 25 nM, respectively.
G007-LK reduces Wnt/β-catenin signaling by preventing poly(ADP-ribosyl)ation-dependent AXIN degradation, thereby promoting β-catenin destabilization.
G007-LK effectively blocks ligand-driven Wnt/β-catenin signaling in cell culture and displays approximately 50% inhibition of APC mutation-driven signaling in most CRC cell lines, inhibits the g of mouse intestinal organoids cultured ex vivo with IC50 of 80 nM.
G007-LK inhibits in vivo tumor growth in a subset of APC-mutant CRC xenograft models.
