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. IC50 & Target: IC50: 32 nM (LDHA), 27 nM (LDHB)^[1] In Vitro: 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 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]. In Vivo: LDH-IN-1 shows clearance values that far exceed hepatic blood flow (HBF) in mouse species (90 mL/min/kg), with in vivo clearances of 227 mL/min/kg^[1].