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KYA1797K is an inhibitor of Wnt/β-catenin signaling.1 It inhibits expression of a reporter induced by Wnt3a-conditioned medium in HEK293 cells (IC50 = 0.75 μM). KYA1797K binds to the regulators of G-protein signaling (RGS) domain of axin and increases activation of GSK3β, as well as phosphorylation of β-catenin and Ras, in HEK293 cells when used at a concentration of 25 μM. It decreases β-catenin and Ras protein levels and inhibits colony formation in SW480 cells in a concentration-dependent manner. KYA1797K inhibits the growth of SW480, LoVo, DLD1, and HCT15 cells (GI50s = 5, 4.8, 4.5, and 4.2 μM, respectively). It reduces tumor growth in a D-MT colorectal cancer mouse xenograft model when administered at a dose of 20 mg/kg.
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