iCRT3 is a selective, cell-permeable β-catenin responsive transcription (CRT) inhibitor with IC50 of 8.2 nM.
iCRT3 interferes with β-cat-TCF4 interaction via direct β-catenin (β-cat) binding, inhibits cellular expression of CRT target genes, including WISP1, AXN2, and CYCD1, in a dose-dependent manner (25-75 uM).
iCRT3 selectively inhibits the proliferation of HCT116 (75 µM), HT29 (75 µM), and several primary human colon cancer cultures (6.25-100 µg/ml).
