ICG-001 is a small-molecule antagonist of b-catenin/TCF-mediated transcription (IC50 = 3 uM) and specifically downregulates the expression of a subset of b-catenin/TCF-responsive genes. ICG-001 binds specifically to cyclic AMP response element-binding protein (CBP), therby disrupting interaction of CBP with b-catenin. [1] ICG-001 selectively induces apoptosis in transformed, but not normal colon cells, and reduces in vitro growth of colon carcinoma cells.

ICG-001 has also been shown to attenuate bleomycin-induced lung fibrosis in mice by selective inhibition of Wnt/b-catenin-dependent transcription. [2]

ICG-001 is believed to correct defects in neuronal stem cell differentiation by inhibition of this pathway [3] and associated polytopic protein Presenilin-1 (PS-1), which suggests potential therapies in Alzheimer's disease.

The wnt/b-catenin signalling pathway has been implicated in regulation of cancer stem cells and ICG-001 has been studied in this regard. [4]