Bio-Connect
Chemical Structure
Chemical Structure
Chemical Structure

GSK2837808A [1445879-21-9]

Research Use Only
AG-CR1-3685
AdipoGen Life Sciences
CAS Number1445879-21-9
Product group Chemicals
Estimated Purity>98%
Molecular Weight649.6
Price on request
Packing Size
Large volume orders?
Order with a bulk request

Overview

  • Supplier
    AdipoGen Life Sciences
  • Product Name
    GSK2837808A [1445879-21-9]
  • Delivery Days Customer
    10
  • CAS Number
    1445879-21-9
  • Certification
    Research Use Only
  • Estimated Purity
    >98%
  • Hazard Information
    Warning
  • Molecular Formula
    C31H25F2N5O7S
  • Molecular Weight
    649.6
  • Scientific Description
    Chemical. CAS: 1445879-21-9. Formula: C31H25F2N5O7S. MW: 649.6. . Potent and selective cell-permeable inhibitor of lactate dehydrogenase A (LDHA) (IC50 values are 2.6 and 43 nM for LDHA and LDHB, respectively). Decreases glycolysis. Useful agent for immunometabolism research. Exhibits antitumoral activity. 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. Lactate dehydrogenase A (LDHA) is an important enzyme involved in fermentative glycolysis, important in tumor initiation and metabolism. Cancer cells rely on increased glycolysis resulting in increased lactate production in addition to aerobic respiration in the mitochondria, even under normal oxygen concentrations (a process known as the Warburg effect). This renders LDHA a promising molecular target for the treatment of various cancers. - Potent and selective cell permeable inhibitor of lactate dehydrogenase A (LDHA) (IC50 values are 2.6 and 43 nM for LDHA and LDHB, respectively). Decreases glycolysis. Useful agent for immunometabolism research. Exhibits antitumoral activity. 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. Lactate dehydrogenase A (LDHA) is an important enzyme involved in fermentative glycolysis, important in tumor initiation and metabolism. Cancer cells rely on increased glycolysis resulting in increased lactate production in addition to aerobic respiration in the mitochondria, even under normal oxygen concentrations (a process known as the Warburg effect). This renders LDHA a promising molecular target for the treatment of various cancers.
  • SMILES
    FC1=CC(F)=CC(OC2=CC(C(O)=O)=CC(NC3=C(C=NC4=C3C=CC(C5=C(N=C(N=C5)OC)OC)=C4)S(NC6CC6)(=O)=O)=C2)=C1
  • Storage Instruction
    -20°C,2°C to 8°C
  • UNSPSC
    12352200

References

  • Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells: Cancer Metab. 1, 19 (2013)
  • Targeting lactate dehydrogenase-A inhibits tumorigenesis and tumor progression in mouse models of lung cancer and impacts tumor initiating cells: H. Xie, et al.; Cell Metab. 19, 795 (2014)
  • A guide to immunometabolism for immunologists: L.A. O'Neill, et al.; Nat. Rev. Immunol. 16, 553 (2016)
  • The inhibition of lactate dehydrogenase A hinders the transcription of histone 2B gene independently from the block of aerobic glycolysis: E. Brighenti, et al.; BBRC 485, 742 (2017)