GSK 2837808A

Name: GSK 2837808A
Brand: Tocris Bioscience
SKU: 5189
Rating: 5 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 5189

(1)

Citations (36)

COA / SDS

Potent and selective LDHA inhibitor

Key Product Details

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)
Molecular Weight:	649.62

View Full Technical Details for GSK 2837808A

Technical Data
Citations / Reviews (1)

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 for GSK 2837808A

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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	7.70 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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References for GSK 2837808A

References are publications that support the biological activity of the product.

Xie Targeting lactate dehydrogenase-A inhibits tumorigenesis and tumor progression in mouse models of lung cancer and impacts tumor-initiating cells. Cell.Metab. 2014 PMID: 24726384
Brighenti The inhibition of lactate dehydrogenase A hinders the transcription of histone 2B gene independently from the block of aerobic glycolysis. Biochem.Biophys.Res.Commun. 2017 PMID: 28257841
Billiard Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells. Cancer Metab. 2013 PMID: 24280423