TW-37 is a potent, nonpeptidic small-molecule inhibitor of Bcl-2 with Ki of 290 nM, also binds to Bcl-xL and Mcl-1 with high affinities.
TW-37 potently inhibits cell growth in PC-3 prostate cancer cells with an IC(50) value of 200 nM and effectively induces apoptosis in a dose-dependent manner.
TW-37 shows antiangiogenic effect against endothelial cells (IC50=1.8 uM) with no cytotoxic effects for fibroblasts.
TW-37 induces endothelial cell apoptosis by mitochondrial depolarization and activation of caspase-9 and caspase-3, decreases the density of functional human microvessels in mouse model of human angiogenesis.
