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.
Sold for research purposes under agreement from GlaxoSmithKline.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 649.62. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.54 mL||7.7 mL||15.39 mL|
|5 mM||0.31 mL||1.54 mL||3.08 mL|
|10 mM||0.15 mL||0.77 mL||1.54 mL|
|50 mM||0.03 mL||0.15 mL||0.31 mL|
References are publications that support the products' biological activity.
Billiard et al (2013) Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells. Cancer Metab. 1 19 PMID: 24280423
Xie et al (2014) Targeting lactate dehydrogenase-A inhibits tumorigenesis and tumor progression in mouse models of lung cancer and impacts tumor-initiating cells. Cell.Metab. 19 795 PMID: 24726384
If you know of a relevant reference for GSK 2837808A, please let us know.
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Keywords: GSK 2837808A, supplier, GSK2837808A, potent, selective, lactate, dehydrogenase, A, LDHA, inhibitors, inhibits, H2B, transcription, Lactate, Dehydrogenase, A, Lactate, Dehydrogenase, A, Tocris Bioscience
2 Citations for GSK 2837808A
Citations are publications that use Tocris products. Selected citations for GSK 2837808A include:
Brighenti et al (2017) The inhibition of lactate dehydrogenase A hinders the transcription of histone 2B gene independently from the block of aerobic glycolysis. Biochem.Biophys.Res.Commun. 485 742 PMID: 28257841
Massey (2017) Modification of tumour cell metabolism modulates sensitivity to Chk1 inhibitor-induced DNA damage. Sci Rep 7 40778 PMID: 28106079
Do you know of a great paper that uses GSK 2837808A from Tocris? If so please let us know.
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