Galloflavin inhibits both human LDH isoforms by preferentially binding the free enzyme, without competing with the substrate or cofactor. The calculated Ki values for pyruvate are 5.46 mm (LDH-A) and 15.06 mm (LDH-B). In cultured tumor cells, galloflavin blocks aerobic glycolysis at micromolar concentrations, not interferes with cell respiration, and induces cell death by triggering apoptosis.