Cayman G007-LK

G007-LK is an inhibitor of the tankyrases TNKS1 and TNKS2 (IC₅₀s = 46 and 25 nM, respectively). It is selective for TNKS1 and TNKS2 over a panel of 90 kinases, 16 phosphatases, and 73 g protein-coupled receptors (GPCRs) when used at a concentration of 10 µM. G007-LK inhibits colony formation of COLO 320 DM and SW403 colorectal cancer cell lines when used at a concentration of 200 µM, as well as human hepatocellular carcinoma (HCC) cells in a dose-dependent manner.^, It increases expression of intestinal differentiation markers in COLO 320 DM and HCT15 cells when used at a concentration of 100 nM. G007-LK inhibits Wnt3A-induced signaling in human HEK293 and mouse 10T1/2 cells. G007-LK (20 mg/kg, i.p., twice daily) also inhibits tumor growth in COLO 320 DM and SW403 mouse xenograft models, however, it leads to intestinal toxicity when administered at a dose of 30 mg/kg twice daily, leading to moribundity and death.

WARNING This product is not for human or veterinary use.