NHI-2
LDHA inhibitor / NHI-2 is a selective inhibitor of Lactate Dehydrogenase A (LDHA) – IC50 in vitro = 14.7 µM (NADH), 10.5 µM (Pyruvate).1 NHI-2 has also shown cellular growth inhibitory effects against pancreatic cancer cells (PANC-1 cells IC50 = 22.2 µM normoxic and 4.0 µM hypoxic; LPC006 cells IC50 = 17.8 µM normoxic and 1.1 µM hypoxic) with increased efficacy in a cancer cells hypoxic environment.2 LDHA is a key enzyme involved in the Warburg effect and a cancer cells ability to survive in a hypoxic environment.
Biochemicals & reagents
1269802-97-2
1) Granchi et al., (2013), Assessing the differential action on cancer cells of LDH-A inhibitors based on the N-hydroxyindole-2-carboxylate (NHI) and malonic (MaI) scaffolds; Org.Biomol.Chem. 11 6588 2) Maftouh et al. (2014), Synergistic interaction of novel lactate dehydrogenase inhibitors with gemcitabine against pancreatic cancer cells in hypoxia; Br.J.Cancer 110 172 3) Granchi et al., (2011), Discovery of N-Hydroxyindole-based Inhibitors of Human Lactate Dehydrogenase Isoform A (LDH-A) as Starvation Agents against Cancer Cells; J.Med.Chem. 54 1599 4) Allison, et al., (2014), Identification of LDH-A as a therapeutic target for cancer cell killing via (i) p53/NAD(H)-dependent and (ii) p-53-independent pathways; Oncogenesis 3 e102
-20°C
TARGET: Dehydrogenase (GAPDH, GPDH, IMPDH, PHGDH, LDH, DHODH, ALDH, GDH, IDH, UGDH, DPD, DHPDH, KGDH, PDH, and MDH); Energy production -- PATHWAY: NAD, NADP pathways; Warburg effect -- RESEARCH AREA: Oxidative stress -- DISEASE AREA: Cancer