NHI-1

NHI-1 is a potent small molecule inhibitor of Lactate Dehydrogenase A (LDHA), an enzyme that catalyzes the conversion of pyruvate to lactate. It is primarily used as a pharmacological tool to investigate the role of the 'LDHA-lactate axis' in various pathologies, including cancer and metabolic disorders. In the context of type 2 diabetes, NHI-1 has been shown to counteract the inhibitory effects of branched-chain α-keto acids (BCKAs) on glucose-stimulated insulin secretion (GSIS) in pancreatic β-cells. By blocking LDHA, NHI-1 prevents the redirection of glucose metabolism toward lactate production and instead promotes oxidative phosphorylation via the tricarboxylic acid (TCA) cycle, thereby restoring β-cell function and improving glucose tolerance in preclinical models. It is also widely studied in oncology for its potential to inhibit the Warburg effect in solid tumors.

Other names

Methyl 1-hydroxy-6-phenyl-4-(trifluoromethyl)-1H-indole-2-carboxylate