Biological Activity
LDHA-IN-3, as a selenobenzene compound, is a potent, noncompetitive lactate dehydrogenase (LDHA) inhibitor (IC50=145.2 nM). LDHA-IN-3 can be used for the research of cancer[1].
PSTMB (0~500 μM; 48 hours; MCF-7 cells) shows cytotoxic effect[1].PSTMB (0.01~1 μM) shows dose-dependent inhibition of LDHA activity. PSTMB (0~0.5 μM) inhibits LDHA activity in Michaelis-Menten and Lineweaver-Burk plots. PSTMB (30 and 50 μM; HT29 cells) induces ROS production and mitochondrial damage[1].PSTMB can bind to LDHA protein efficiently. PSTMB induces the intrinsic pathway-mediated apoptosis of cancer cells via production of mitochondrial ROS[1].
References
[1]. Kim EY, et al. A Novel Lactate Dehydrogenase Inhibitor, 1-(Phenylseleno)-4-(Trifluoromethyl) Benzene, Suppresses Tumor Growth through Apoptotic Cell Death. Sci Rep. 2019;9(1):3969. Published 2019 Mar 8.
