GSK 2837808A

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Cat.No. 5189 - GSK 2837808A | C31H25F2N5O7S | CAS No. 1445879-21-9
Description: Potent, 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% (HPLC)
Datasheet
Citations (2)
Literature

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.

Compound Libraries

GSK 2837808A is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 649.62
Formula C31H25F2N5O7S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1445879-21-9
PubChem ID 71533725
InChI Key RZBCPMYJIARMGV-UHFFFAOYSA-N
Smiles O=S(C2=C(NC3=CC(OC5=CC(F)=CC(F)=C5)=CC(C(O)=O)=C3)C1=CC=C(C6=CN=C(OC)N=C6OC)C=C1N=C2)(NC4CC4)=O

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 64.96 100

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

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


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Keywords: GSK 2837808A, supplier, GSK2837808A, potent, selective, lactate, dehydrogenase, A, LDHA, inhibitors, inhibits, H2B, transcription, 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


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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis

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