LDH-IN-1是一种新的基于吡唑的人乳酸脱氢酶(LDH)抑制剂，对于LDHA和LDHB的IC50值分别为32和27nM。
CAS：1964515-43-2
分子式：C30H26N4O4S2
分子量：570.68
纯度：98%
存储：Store at -20°C

Background:

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 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].

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].

[1]. Rai G, et al. Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH). J Med Chem. 2017 Nov 22;60(22):9184-9204.