UU-T02 is a potent, selective small-molecule inhibitor of β-catenin/Tcf4 interaction. The β-catenin/T-cell factor (Tcf) protein−protein interaction (PPI) plays a critical role in the β-catenin signaling pathway which is hyperactivated in many cancers and fibroses. UU-T02 disrupted β-catenin/Tcf PPI with a Ki of 1.36 μM in the fluorescence polarization (FP) competitive inhibition assay and displayed 175- and 64-fold selectivity over β-catenin/E-cadherin and β-catenin/APC, respectively.
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