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LF3 is an inhibitor of the protein-protein interaction between β-catenin and T cell factor 4 (TCF4).1 It inhibits the β-catenin-TCF4 interaction in an immunoprecipitation assay and prevents β-catenin-induced inhibition of SCN5A promoter activity in HEK293 cells when used at a concentration of 10 µM. LF3 increases levels of the voltage-gated sodium channel Nav1.5 in HL-1 cardiomyocytes. It is cytotoxic to GES-1, HGC-27, MKN45, and AGS gastric cancer cells (IC50s = 24.68, 18.2, 489, and 56.76 µM, respectively).2 In vivo, LF3 (25 mg/kg) decreases pulmonary artery systolic pressure (PASP) and the right ventricular hypertrophy index (RVHI) in a rat model of total pneumonectomy-induced pulmonary hypertension.3
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1. A small-
2. A novel UBE2T inhibitor suppresses Wnt/β-
3. Small-