– ZINC02092166 is a novel potent, and selective small-molecule inhibitor for the ?-catenin/Tcf4 protein-protein interaction with Ki of 1.7 and 7.0 uM in AlphaScreen and FP assay (wild-type ?-catenin), respectively; remain affinity for muant catenin V511S, V511S/I569S and R469A with Ki of 20-50 uM; exhibits dual selectivity for ?-catenin/Tcf over ?-catenin/cadherin and ?-catenin/APC PPIs.