ICG-001 is a small molecule inhibitor of β-catenin/cyclic AMP responsive element binding protein binding protein (CBP)-mediated transcription (IC50 = 3 μM). By binding CBP, thus blocking interaction with β-catenin, it selectively induces apoptosis in transformed colon cells but not in normal cells and prevents the growth of colon carcinoma cells at 25 μM in vitro. ICG-001 has been used to specifically disrupt the β-catenin pathway in studying epithelial-mesenchymal transition during pulmonary fibrosis. Additionally, ICG-001 disruption of Wnt/β-catenin signaling has been studied in the context of regulating cancer stem cells.
