Uses
A cell-permeable, non-cytotoxic N-hydroxyindole (NHI) carboxylate that acts as a potent, reversible, and isoform selective inhibitor of lactic dehydrogenase (LDH) A/LDH-1. Inhibition appears to be competitive with respect to both pyruvate (Ki = 4.7 µM) and NADH (cofactor; Ki = 8.9 µM). Acts by occupying the whole substrate pocket and part of the cofactor pocket of LDH-A. Blocks the growth of various cancer cell lines by causing an arrest at G1 phase and inducing apoptosis (IC50 = 10.8, 10.6, 11.4, and 31.5 µM for A2780/cOHP, MSTO-211H, NIH-H28, and H630 cells, respectively). Exhibits enhanced anticancer activity under hypoxic conditions (GI50 = 0.90 µM/hypoxia vs. 16.3 µM/normoxia in LPC006 cultures) and strongly synergizes with gemcitabine.Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
