LF3

一种β-catenin-TCF4蛋白-蛋白相互作用抑制剂；在免疫共沉淀实验中抑制β-catenin-TCF4相互作用，并在10µM浓度下防止HEK293细胞中β-catenin诱导的SCN5A启动子活性抑制；在HL-1心肌细胞中增加Nav1.5水平；对GES-1、HGC-27、MKN45和AGS胃癌细胞具有细胞毒性（IC50值分别为24.68µM、18.2µM、489µM和56.76µM）；在25mg/kg剂量下，可降低全肺切除诱导的肺动脉高压大鼠模型中的肺动脉收缩压（PASP）和右心室收缩压（RVHI）。An inhibitor of the β-catenin-TCF4 protein-protein interaction; inhibits the β-catenin-TCF4 interaction in an immunoprecipitation assay and prevents β-catenin-induced inhibition of SCN5A promoter activity in HEK293 cells at 10 µM; increases levels of Nav1.5 in HL-1 cardiomyocytes; is cytotoxic to GES-1, HGC-27, MKN45, and AGS gastric cancer cells (IC50s = 24.68, 18.2, 489, and 56.76 µM, respectively); decreases PASP and RVHI in a rat model of total pneumonectomy-induced pulmonary hypertension at 25 mg/kg.分子式C20H24N4O2S2分子量416.6O=S(N)(C1=CC=C(NC(N2CCN(CC2)CC=CC3=CC=CC=C3)=S)C=C1)=O