GNE-140

GNE-140

Biochem/physiol Actions

GNE-140 is an active site-targeting, potent and selective lactate dehydrogenase (LDH) inhibitor (LDH-A/B/C IC50 = 3/5/5 nM; LDH-A IC50 = 22 nM with mixed GNE-140 diastereomers; malate dehydrogenases MDH1/2 IC50 >10 µM; 301 kinases IC50 >1 µM) that reduces cellular lactate (IC50 = 670 nM; MIA PaCa-2) and upregulates pyruvate levels. GNE-140 affects glycolysis-dependent cancer proliferation (IC50 = 430 nM; MIA PaCa-2 & KP-2) & survival, but not oxidative phosphorylation (OXPHOS)-dependent growth. Due to rapid clearance, GNE-140 is ineffective against MIA PaCa-2 tumor growth with only transient lactate-reducing efficacy in tumor tissue in mice in vivo (100-400 mg/kg b.i.d. p.o.).

Active site-targeting, potent and selective lactate dehydrogenase (LDH) inhibitor that affects glycolysis-dependent cancer proliferation & survival.

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3576531 GNE-140 white to beige SIGMA-ALDRICH −20°C DMSO: 2 mg/mL, clear powder ≥98% (HPLC)
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3576532 GNE-140 white to beige SIGMA-ALDRICH −20°C DMSO: 2 mg/mL, clear powder ≥98% (HPLC)
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