GSK2837808A is a potent and selective inhibitor of lactate dehydrogenase A (LDHA) with IC50 values of 1.9 nM for LDHA and 14 nM for LDHB.

LDHB:1.9 nM, LDHA:1.9 nM

GSK2837808A inhibits lactate production in hypoxia but at higher concentrations than in normoxia (EC50=10 μM). It also reduces ECAR (EC50=10 μM). LDH inhibition by GSK2837808A alters multiple metabolic pathways in Snu398 cells. GSK2837808A rapidly and profoundly inhibits lactate production rates in multiple cancer cell lines including hepatocellular and breast carcinomas. GSK2837808A potency does not correlate with LDHA, LDHB, or the total LDH expression levels. The potency of GSK2837808A across 30 cancer cell lines with different LDHA and LDHB expression levels range from 400 nM to no effect (EC50 reported as 30 μM).

GSK2837808A (p.o.; 50 mg/kg in rats; 100 mg/kg in mice) treatment, causes blood compound levels at or below the detection limit of 2.5 ng/mL. Clearance following IV infusion of GSK2837808A at 0.25 mg/kg is displayed to be 69 mL/minute/kg in rats and it exceeds the animal liver blood flow.