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Submit ReviewGSK 2837808A
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% (HPLC)
Biological Activity for GSK 2837808A
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.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline.
Compound Libraries for GSK 2837808A
GSK 2837808A is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for GSK 2837808A
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for GSK 2837808A
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 64.96 | 100 |
Preparing Stock Solutions for GSK 2837808A
The following data is based on the product molecular weight 649.62. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 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 for GSK 2837808A
References for GSK 2837808A
References are publications that support the biological activity of the product.
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
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
If you know of a relevant reference for GSK 2837808A, please let us know.
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Keywords: GSK 2837808A, GSK 2837808A supplier, GSK2837808A, potent, selective, lactate, dehydrogenase, A, LDHA, inhibitors, inhibits, H2B, transcription, Lactate, Dehydrogenase, 5189, Tocris Bioscience
17 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
Nidhi et al (2021) The distinct roles of calcium in rapid control of neuronal glycolysis and the tricarboxylic acid cycle. Elife 10 PMID: 33555254
Catherine A et al (2021) Fructose reprogrammes glutamine-dependent oxidative metabolism to support LPS-induced inflammation. Nat Commun 12 1209 PMID: 33619282
David A et al (2022) A high-throughput multiparameter screen for accelerated development and optimization of soluble genetically encoded fluorescent biosensors. Nat Commun 13 2919 PMID: 35614105
Jacqueline D et al (2022) Tumor-Derived Lactic Acid Modulates Activation and Metabolic Status of Draining Lymph Node Stroma. Cancer Immunol Res 10 482-497 PMID: 35362044
Cascone et al (2018) Increased Tumor Glycolysis Characterizes Immune Resistance to Adoptive T Cell Therapy. Cell Metab 27 977 PMID: 29628419
David E et al (2020) Lactate production is a prioritized feature of adipocyte metabolism. J Biol Chem 295 83-98 PMID: 33518012
Georg et al (2020) Metabolic reprogramming of osteoclasts represents a therapeutic target during the treatment of osteoporosis. Sci Rep 10 21020 PMID: 33273570
David E et al (2020) Lactate production is a prioritized feature of adipocyte metabolism. J Biol Chem 295 83-98 PMID: 31690627
Merk et al (2016) Breaking Cryo-EM Resolution Barriers to Facilitate Drug Discovery. Cell 165 1698 PMID: 27238019
Sylvie et al (2023) Mitochondrial pyruvate metabolism regulates the activation of quiescent adult neural stem cells. Sci Adv 9 eadd5220 PMID: 36857455
Randall S et al (2023) Lactate exposure shapes the metabolic and transcriptomic profile of CD8+ T cells. Front Immunol 14 1101433 PMID: 36923405
Lin et al (2017) Lactate-activated macrophages induced aerobic glycolysis and epithelial-mesenchymal transition in breast cancer by regulation of CCL5-CCR5 axis: a positive metabolic feedback loop. Oncotarget 8 110426 PMID: 29299159
Diaz-Garcia et al (2017) Neuronal Stimulation Triggers Neuronal Glycolysis and Not Lactate Uptake. Cell Metab 26 361 PMID: 28768175
Thongon et al (2018) Cancer cell metabolic plasticity allows resistance to NAMPT inhibition but invariably induces dependence on LDHA. Cancer Metab 6 1 PMID: 29541451
Hanse et al (2017) Cytosolic malate dehydrogenase activity helps support glycolysis in actively proliferating cells and cancer. Oncogene 36 3915 PMID: 28263970
Do you know of a great paper that uses GSK 2837808A from Tocris? Please let us know.
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Mouse oocytes lactate uptake.
By
Anonymous on 11/13/2023
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: Oocytes
GSK 2837808A inhibitor titrations were performed at pH 6 with oocytes preincubated for 45 min in a different uptake buffer (75 mM NaCl,2 mM KCl, 0.82 mM MgCl2, 1 mM CaCl2 and 20 mM Mes, pH 6)containing the required concentration of GSK 2837808A prior tomeasuring the uptake of L-[14C]lactate (0.5 mM).
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Cancer Metabolism Research Product Guide
This product guide reviews some of the main areas in cancer metabolism research and lists around 150 products that can be used to investigate metabolic pathways in cancer including:
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Cancer Metabolism Poster
This poster summarizes the main metabolic pathways in cancer cells and highlights potential targets for cancer therapeutics. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways providing potential cancer therapeutic targets.