UU-T02 is a novel potent, selective small-molecule inhibitor of 尾-Catenin/T-cell factor protein-protein interaction (尾-catenin/Tcf PPI) with a Ki of 1.36 渭M. UU-T02 inhibits canonical Wnt signaling and the growth of colorectal cancer cells.
UU-T02 displays Ki values of 1.4 渭M and 1.3 渭M for 尾-catenin/Tcf PPI in FP assay and in AlphaScreen assay, respectively[2].
UU-T02 inhibits 尾-catenin/Tcf4, 尾-catenin/E-cadherin, 尾-catenin/APC-R3, with the IC50 of 6.3, 680, 210 渭M锛宺espectively[2].
[1]. Huang Z, et al. Targeting the Tcf4 G13ANDE17 binding site to selectively disrupt 尾-catenin/T-cell factor protein-protein interactions. ACS Chem Biol. 2014;9(1):193-201.
[2]. Catrow JL, et al. Discovery of Selective Small-Molecule Inhibitors for the 尾-Catenin/T-Cell Factor Protein-Protein Interaction through the Optimization of the Acyl Hydrazone Moiety. J Med Chem. 2015;58(11):4678-4692.