GSK 2837808A

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GSK 2837808A | CAS No. 1445879-21-9 | Lactate Dehydrogenase A/LDHA Inhibitors
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Description: Potent and selective LDHA inhibitor

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

Purity: ≥98%

Product Details
Citations (17)

Biological Activity

GSK 2837808A is a potent and selective lactate dehydrogenase A and B (LDHA and LDHB) inhibitor (IC50 values are 2.6 and 43 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.

Technical Data

Soluble to 100 mM in DMSO
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline.

Product Datasheets

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Citations for GSK 2837808A

The citations listed below are publications that use Tocris products. Selected citations for GSK 2837808A include:

17 Citations: Showing 1 - 10

  1. Mitochondrial pyruvate metabolism regulates the activation of quiescent adult neural stem cells.
    Authors: Sylvie Et al.
    Sci Adv  2023;9:eadd5220
  2. Lactate exposure shapes the metabolic and transcriptomic profile of CD8+ T cells.
    Authors: Randall S Et al.
    Front Immunol  2023;14:1101433
  3. A high-throughput multiparameter screen for accelerated development and optimization of soluble genetically encoded fluorescent biosensors.
    Authors: David A Et al.
    Nat Commun  2022;13:2919
  4. Tumor-Derived Lactic Acid Modulates Activation and Metabolic Status of Draining Lymph Node Stroma.
    Authors: Jacqueline D Et al.
    Cancer Immunol Res  2022;10:482-497
  5. Fructose reprogrammes glutamine-dependent oxidative metabolism to support LPS-induced inflammation.
    Authors: Catherine A Et al.
    Nat Commun  2021;12:1209
  6. The distinct roles of calcium in rapid control of neuronal glycolysis and the tricarboxylic acid cycle.
    Authors: Nidhi Et al.
    Elife  2021;10
  7. Lactate production is a prioritized feature of adipocyte metabolism.
    Authors: David E Et al.
    J Biol Chem  2020;295:83-98
  8. Lactate production is a prioritized feature of adipocyte metabolism.
    Authors: David E Et al.
    J Biol Chem  2020;295:83-98
  9. Metabolic reprogramming of osteoclasts represents a therapeutic target during the treatment of osteoporosis.
    Authors: Georg Et al.
    Sci Rep  2020;10:21020
  10. Cancer cell metabolic plasticity allows resistance to NAMPT inhibition but invariably induces dependence on LDHA.
    Authors: Thongon Et al.
    Cancer Metab  2018;6:1


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