GSK 2837808A

Cat. No. 5189

GSK 2837808A C31H25F2N5O7S [1445879-21-9]

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Chemical Name: 3-[[3-[(Cyclopropylamino)sulfonyl]-7-(2,4-dimethoxy-5-pyrimidinyl)-4-quinolinyl]amino]-5-(3,5-difluorophenoxy)benzoic acid

Biological Activity

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.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline.

Technical Data

M.Wt:
649.62
Formula:
C31H25F2N5O7S
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
1445879-21-9

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

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.

Billiard et al (2013) Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells. Cancer Metab. 1 19. PMID: 24280423.

If you know of a relevant reference for GSK 2837808A please let us know.

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.

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Keywords: GSK 2837808A, supplier, GSK2837808A, potent, selective, lactate, dehydrogenase, A, LDHA, inhibitors, inhibits, H2B, transcription, Tocris Bioscience, Lactate Dehydrogenase A Inhibitor products

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