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GSK2837808A is a potent, selective lactate dehydrogenase A (LDHA) inhibitor (IC50 values are 1.9 and 14 nM for LDHA and LDHB respectively). GSK2837808A inhibits lactate production in selected cancer cell lines. GSK2837808A reduces glucose uptake and enhances mitochondrial oxygen consumption in Snu398 hepatocellular carcinoma cells. GSK2837808A inhibits proliferation and induces apoptosis in Snu398 cells. GSK2837808A inhibits transcription of histone 2B (H2B) gene in HCT116 and NCM460 cells. GSK2837808A is cell permeable. GSK2837808A rapidly and profoundly inhibits lactate production rates in multiple cancer cell lines including hepatocellular and breast carcinomas. The potency of GSK2837808A across 30 cancer cell lines with different LDHA and LDHB expression levels ranges from 400 nM to no effect (EC50 reported as 30 μM). GSK2837808A potency does not correlate with LDHA, LDHB, or the total LDH expression levels. GSK2837808A inhibits lactate production in hypoxia but at higher concentrations than in normoxia (EC50=10 μM). It also reduces ECAR with EC50=10 μM. LDH inhibition by GSK2837808A alters multiple metabolic pathways in Snu398 cells. Oral dosing of GSK2837808A at 50 mg/kg in rats or 100 mg/kg in mice results in blood compound levels at or below the detection limit of 2.5 ng/mL.
| Molecular Weight | 649.62 |
| Formula | C31H25F2N5O7S |
| CAS Number | 1445879-21-9 |
| Form | Solid |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related LDH Products |
|---|
| Galloflavin
Galloflavin is a lactate dehydrogenase inhibitor; impairs aerobic glycolysis. |
| NHI-2
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). |
| AZ-33
AZ-33 (LDHA-IN-4) is a potent lactate dehydrogenase A (LDHA) inhibitor with IC50 of 0.5 μM. |
| GNE-140 racemate
GNE-140 racemate is a racemic mixture of (R)-GNE-140 and (S)-GNE-140. GNE-140 racemate is also a potent lactate dehydrogenase A (LDHA) inhibitor. |
| (R)-GNE-140
(R)-GNE-140 is a selective inhibitor of LDHA and LDHB with IC50 of 3 nM and 5 nM, respectively. (R)-GNE-140 is 18 times more potent than its S-type isomer. |
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