Catalog Number: 5189
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.
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.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline.
Background References
  1. Targeting lactate dehydrogenase-A inhibits tumorigenesis and tumor progression in mouse models of lung cancer and impacts tumor-initiating cells.
    Xie et al.
    Cell.Metab., 2014;19:795
  2. Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells.
    Billiard et al.
    Cancer Metab., 2013;1:19
Citations:

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

2 Citations: Showing 1 - 2
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  1. Modification of tumour cell metabolism modulates sensitivity to Chk1 inhibitor-induced DNA damage.
    Authors: Massey
    Sci Rep 2017;7:40778
  2. The inhibition of lactate dehydrogenase A hinders the transcription of histone 2B gene independently from the block of aerobic glycolysis.
    Authors: Brighenti Et al.
    Biochem.Biophys.Res.Commun. 2017;485:742

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