LF3

LF3 is an inhibitor of the protein-protein interaction between ?-catenin and T cell factor 4 (TCF4).{61916} It inhibits the ?-catenin-TCF4 interaction in an immunoprecipitation assay and prevents ?-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).{61917} 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.{61918}