NHI-2 is an inihbitor of Lactate dehydrogenase-A (LDH-A, LDHA), a key enzyme necessary to sustain glycolysis, the major pathway used by many cancer cells for cell growth and proliferation (the Warburg effect). NHI-2 has anti-glycolytic activity against a variety of cancer cells. NHI-2 inhibited cell growth of pancreatic cancer LPC006 and PANC-1 cells and enhanced the antiproliferative effects of Gemcitabine and caused apoptosis in colon cancer HCT116 cells.
NHI-2 is an inihbitor of Lactate dehydrogenase-A (LDH-A, LDHA).
Epilepsy affects millions globally with a significant portion exhibiting pharmacoresistance. Abnormal neuronal activity elevates brain lactate levels, which prompted the exploration of its receptor, the hydroxycarboxylic acid receptor 1 (HCAR1) known to downmodulate neuronal activity in physiological conditions. This study
A head-to-head study of representative examples of N-hydroxyindole-2-carboxylates (NHI) and malonic derivatives (Mal) as LDH-A inhibitors was conducted, comparing the enzyme inhibition potency, cellular uptake, reduction of lactate production in cancer cells and anti-proliferative activity. Among the compounds tested, methyl
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