GSK 2837808A is a potent, selective lactate dehydrogenase A (LDHA) inhibitor (IC50 values are 1.9 and 14 nM for LDHA and LDHB respectively). Inhibits lactate production in selected cancer cell lines. Reduces glucose uptake and enhances mitochondrial oxygen consumption in Snu398 hepatocellular carcinoma cells. Inhibits proliferation and induces apoptosis in Snu398 cells. Inhibits transcription of histone 2B (H2B) gene in HCT116 and NCM460 cells. Cell permeable.
| Molecular Weight | 649.62 |
| Formula | C31H25F2N5O7S |
| CAS Number | 1445879-21-9 |
| Form | Solid |
| Solubility (25°C) | DMSO 64.96 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| 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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