WC522 | Cholesterol-Dvl2 inhibitor | Probechem Biochemicals

Chemical Structure : WC522

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WC522 (Dvl2-PDZ-cholesterol interaction inhibitor)

货号: PC-24367Not For Human Use, Lab Use Only.

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.

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生物&药学活性

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.

物理化学性质&存储条件

分子量	380.53
分子式	C24H32N2O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N2,N2-diethyl-N4',N4'-dipropyl-[1,1'-biphenyl]-2,4'-dicarboxamide

参考文献

1. Sharma A, et al. Nat Chem Biol. 2025 Apr 16. doi: 10.1038/s41589-025-01870-y.

WC522 (Dvl2-PDZ-cholesterol interaction inhibitor)

生物&药学活性

物理化学性质&存储条件

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WC522 (Dvl2-PDZ-cholesterol interaction inhibitor)

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物理化学性质&存储条件

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