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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 |
|---|
| Nedosiran sodium
Nedosiran sodium is a GalNAc-dsRNA conjugate designed to inhibit production of the hepatic lactate dehydrogenase (LDH) enzyme. |
| MS6105
MS6105 is an LDH protein hydrolysis-targeted chimera (PROTAC) with anticancer activity for studies related to pancreatic cancer. |
| CHK-336
CHK-336 is an inhibitor of the lactate dehydrogenase LDHA and can be used in studies related to primary hyperoxaluria. |
| FX-11
FX-11 (LDHA Inhibitor FX11) is a potent lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 23.3 μM for HeLa cell and a Ki value of 8 μM. FX-11 can reduce ATP levels, induce oxidative stress and ROS production, and cause cell death. |
| (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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