WC522 is a selective small molecule inhibitor of Dvl2-PDZ-cholesterol interaction, effectively suppresses both Wnt-independent and Wnt-stimulated β-catenin signaling activity in Dvl2-expressing APC-truncated CRC cells.
WC522 occupies the region where Dvl2-PDZ interacts with cholesterol molecules in the membrane.
WC522B (biotinylated derivative of WC522) captured Dvl2 but not Dvl1 and Dvl3 in both HCT15 and HCT116 cells 
WC522 dose-dependently inhibits HCT15 cell viability and induces cell apoptosis.
WC522 potently inhibits β-catenin stability and β-catenin transcriptional activity in HCT15 and Caco2 cells, WC522 also suppresses β-catenin signaling in DLD1 and LOVO cells.
WC522 is effective against all Dvl-expressing APC-truncated CRC cells regardless of the length of the truncated APC.
WC522 blocks cell proliferation of APC-truncated CRC cells, with little to no antiproliferative effect against normal colon epithelial (CCD-18Co) cells, induces apoptosis of APC-truncated CRC cells.
WC522 (200 mg/kg, subcutaneous injection) blocks CRC tumors HCT15 xenografts in mice and effectively suppresses the level of active β-catenin, does not inhibit tumor growth of Dvl2-KO HCT15 xenografts.