(R)-GNE-140 | Lactate dehydrogenase inhibitor

GNE-140 chemical structure

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(R)-GNE-140 (2003234-63-5) is a  potent (IC50’s: LDHA = 3 nM, LDHB = 5 nM, LDHC = 5 nM) pan-lactate dehydrogenase inhibitor.1 It significantly decreased lactate levels in vivo, although the effects were transient.  GNE-140 suppressed lactic acid production, severely stunted glucose utilization, and impeded the anaerobic glycolytic pathway in MDA-MB-231 triple negative breast cancer cells.2

References/Citations:

  1. Boudreau et al. (2016), Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition; Nat. Chem. Biol. 12 779
  2. Mazzio (2021), Triple Isozyme Lactic Acid Dehydrogenase Inhibition in Fully Viable MDA-MB-231 Cells Induces Cytostatic Effects That Are Not Reversed by Exogenous Lactic Acid; Biomolecules 11 1751
(R)-GNE-140 supplier, 2003234-63-5, GNE-140, GNE-140 supplier, GNE140, lactate dehydrogenase inhibitor, LDHA inhibitor, LDHB inhibitor

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(R)-GNE-140 (2003234-63-5) is a  potent (IC50’s: LDHA = 3 nM, LDHB = 5 nM, LDHC = 5 nM) pan-lactate dehydrogenase inhibitor.1 It significantly decreased lactate levels in vivo, although the effects were transient.  GNE-140 suppressed lactic acid production, severely stunted glucose utilization, and impeded the anaerobic glycolytic pathway in MDA-MB-231 triple negative breast cancer cells.2

References/Citations:

  1. Boudreau et al. (2016), Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition; Nat. Chem. Biol. 12 779
  2. Mazzio (2021), Triple Isozyme Lactic Acid Dehydrogenase Inhibition in Fully Viable MDA-MB-231 Cells Induces Cytostatic Effects That Are Not Reversed by Exogenous Lactic Acid; Biomolecules 11 1751