Biological Activity
gsk2837808a is a potent, selective lactate dehydrogenase a (ldha) inhibitor (ic50 values are 1.9 and 14 nm for ldha and ldhb respectively).in snu398 but not hepg2 hepatocellular carcinoma cells. gsk2837808a (10 μm) reduces glucose consumption.after intravenous injection of gsk2837808a at 0.25 mg/kg in rats, the clearance is shown to be 69 ml/min/kg, which exceeds the blood flow of the animal liver. oral administration of gsk2837808a at 50 mg/kg or 100 mg/kg in rats or mice, respectively, resulted in blood compound levels reaching or below the detection limit of 2.5 ng/ml.[1]. billiard j, dennison j b, briand j, et al. quinoline 3-sulfonamides inhibit lactate dehydrogenase a and reverse aerobic glycolysis in cancer cells. cancer & metabolism, 2013, 1(1): 19-19.
