1269802-97-2

NHI 2 is an inhibitor of lactate dehydrogenase A (LDHA; IC₅₀ = 14.7 μM). It is selective for LDHA over LDHB (IC₅₀ = 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 (IC₅₀ = 33.4 μM).

NHI-2 is a lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 14.7 μM. NHI-2 shows selective for LDHA over LDHB (IC50 = 55.8 μM). NHI-2 is an efficient anti-glycolytic agent. NHI-2 enhances apoptosis, induces cell cycle arrest at S/G2 phases. NHI-2 has a broad spectrum anti-proliferative activity in cancer cells. NHI-2 affects extracellular acidification rate and ATP production. NHI-2 suppress tumor growth in mice[1][2].

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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]