A specific inhibitor of Wnt/β-catenin signaling pathway. It down-regulates beta-catenin/T cell factor signaling by specifically binding to cyclic AMP response element-binding protein (CBP). ICG-001 selectively induces apoptosis in transformed cells but not in normal colon cells, reduces in vitro growth of colon carcinoma cells, and is efficacious in the Min mouse and nude mouse xenograft models of colon cancer.