WC522 blocks the cholesterol-dishevelled interaction leading to inhibition of ß-catenin signaling. It specifically inhibits the Dvl2-PDZ-cholesterol interaction (IC50 = 40 nM) leading to suppression of both Wnt-independent and Wnt-stimulated ß-catenin signaling (IC50 = 150 nM). WC522 inhibits cell proliferation in APC-truncated colorectal carcinoma cells and colorectal carcinoma HCT15 xenografts in mice.
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