LDH-IN-1

LDH-IN-1 is a novel pyrazole-based inhibitor of human lactate dehydrogenase (LDH) with IC50s of 32 and 27 nM for LDHA and LDHB, respectively. LDH-IN-1 inhibits the growth of MiaPaCa2 pancreatic cancer and A673 sarcoma cells with IC50s of 2.23 and 1.21 μM) . Dose response treatment of MiaPaCa-2 cells with LDH-IN-1 shows effects on cellular proliferation at concentrations as low as 250 nM and with nearly complete arrest of cell growth at 20 μM[1].LDH-IN-1 exhibits low nM inhibition of both LDHA and LDHB (IC50=32, 27 nM, respectively), submicromolar inhibition of lactate production, and inhibition of lactate in MiaPaCa2 pancreatic cancer and A673 sarcoma cells (IC50=0.517, 0.854μM, respectively) .LDH-IN-1 shows clearance values that far exceed hepatic blood flow in mouse species (90 mL/min/kg), with in vivo clearances of 227 mL/min/kg.