GSK 2837808A

Catalog #: 5189
17 Citations Datasheet / COA / SDS

Catalog #	Availability	Size / Price	Qty
5189/10

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%

View All Products for Lactate Dehydrogenase A/LDHA Inhibitors

Product Details

Citations (17)

Reviews

Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

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

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:

Sold for research purposes under agreement from GlaxoSmithKline.

Background References

The inhibition of lactate dehydrogenase A hinders the transcription of histone 2B gene independently from the block of aerobic glycolysis.
Brighenti et al.
Biochem.Biophys.Res.Commun., 2017;485:742
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
Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells.
Billiard et al.
Cancer Metab., 2013;1:19
Frontline Science: AMPK regulates metabolic reprogramming necessary for interferon production in human plasmacytoid dendritic cells
HJ Hurley, H Dewald, ZS Rothkopf, S Singh, F Jenkins, P Deb, S De, BJ Barnes, P Fitzgerald
J. Leukoc. Biol., 2020;0(0):.

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

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

Mitochondrial pyruvate metabolism regulates the activation of quiescent adult neural stem cells.
Authors: Sylvie Et al.
Sci Adv 2023;9:eadd5220
Lactate exposure shapes the metabolic and transcriptomic profile of CD8+ T cells.
Authors: Randall S Et al.
Front Immunol 2023;14:1101433
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
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
Fructose reprogrammes glutamine-dependent oxidative metabolism to support LPS-induced inflammation.
Authors: Catherine A Et al.
Nat Commun 2021;12:1209
The distinct roles of calcium in rapid control of neuronal glycolysis and the tricarboxylic acid cycle.
Authors: Nidhi Et al.
Elife 2021;10
Lactate production is a prioritized feature of adipocyte metabolism.
Authors: David E Et al.
J Biol Chem 2020;295:83-98
Lactate production is a prioritized feature of adipocyte metabolism.
Authors: David E Et al.
J Biol Chem 2020;295:83-98
Metabolic reprogramming of osteoclasts represents a therapeutic target during the treatment of osteoporosis.
Authors: Georg Et al.
Sci Rep 2020;10:21020
Cancer cell metabolic plasticity allows resistance to NAMPT inhibition but invariably induces dependence on LDHA.
Authors: Thongon Et al.
Cancer Metab 2018;6:1

Increased Tumor Glycolysis Characterizes Immune Resistance to Adoptive T Cell Therapy.
Authors: Cascone Et al.
Cell Metab 2018;27:977

Lactate-activated macrophages induced aerobic glycolysis and epithelial-mesenchymal transition in breast cancer by regulation of CCL5-CCR5 axis: a positive metabolic feedback loop.
Authors: Lin Et al.
Oncotarget 2017;8:110426

Modification of tumour cell metabolism modulates sensitivity to Chk1 inhibitor-induced DNA damage.
Authors: Massey
Sci Rep 2017;7:40778

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

Cytosolic malate dehydrogenase activity helps support glycolysis in actively proliferating cells and cancer.
Authors: Hanse Et al.
Oncogene 2017;36:3915

Neuronal Stimulation Triggers Neuronal Glycolysis and Not Lactate Uptake.
Authors: Diaz-Garcia Et al.
Cell Metab 2017;26:361

Breaking Cryo-EM Resolution Barriers to Facilitate Drug Discovery.
Authors: Merk Et al.
Cell 2016;165:1698

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