Description
NHI 2 is an inhibitor of lactate dehydrogenase A (LDHA; IC
50 = 14.7 μM). It is selective for LDHA over LDHB (IC
50 = 55.8 μM). It inhibits lactate production in HeLa cells when used at concentrations of 100 and 200 μM. NHI 2 is cytotoxic to HeLa cells (IC
50 = 33.4 μM).
References
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
5) Lea?et al. (2016)?Inhibition of growth by combined treatment with inhibitors of Lactate Dehydrogenase and either Phenformin of Inhibitors of 6-Phosphofructo-2-kinase / Fructose-2,6-bisphosphatase 3; Anticancer Research,?36?1479 [Focus Biomolecules Citation]