GSK 2837808A

Catalog No.S8590

For research use only.

GSK2837808A is a selective LDHA (lactate dehydrogenase A) inhibitor with IC50 of 2.6 nM and 43 nM for hLDHA and hLDHB, respectively.

GSK 2837808A Chemical Structure

CAS No. 1445879-21-9

Purity & Quality Control

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Biological Activity

Description GSK2837808A is a selective LDHA (lactate dehydrogenase A) inhibitor with IC50 of 2.6 nM and 43 nM for hLDHA and hLDHB, respectively.
Targets
hLDHA [1]
(Cell-free assay)
hLDHB [1]
(Cell-free assay)
2.6 nM 43 nM
In vitro

GSK 2837808A rapidly and profoundly inhibits lactate production rates in multiple cancer cell lines including hepatocellular and breast carcinomas. GSK 2837808A increases rates of oxygen consumption in hepatocellular carcinoma cells at dose up to 3 microM, while higher concentrations directly inhibits mitochondrial function. GSK 2837808A dose dependently potentiates PKM2 activity, inhibits proliferation of Snu398 cells and induces apoptosis in Snu398 cells.[1]

In vivo

GSK 2837808A rapidly and profoundly inhibits lactate production rates in multiple cancer cell lines including hepatocellular and breast carcinomas. GSK 2837808A increases rates of oxygen consumption in hepatocellular carcinoma cells at dose up to 3 microM, while higher concentrations directly inhibits mitochondrial function. GSK 2837808A dose dependently potentiates PKM2 activity, inhibits proliferation of Snu398 cells and induces apoptosis in Snu398 cells.[1]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: MDA-MB-453 cells
  • Concentrations: 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM
  • Incubation Time: 2 h, 6 h
  • Method:

    MDA-MB-453 cells are cultured in normoxic (21% oxygen) or hypoxic (1%) conditions overnight in DMEM supplemented with 5% FBS. Medium is exchanged with physiological DMEM (5 mM glucose, 0.5 mM glutamine, no FBS) containing DMSO or GSK 2837808A at multiple concentrations and collected after 2 h for hypoxic cells and 6 h for normoxic cells. Lactate concentrations are quantified using a YSI 2900 Biochemistry Analyzer with a lactate oxidase probe.

Animal Research:

[1]

  • Animal Models: male CD mice, male Sprague–Dawley rats
  • Dosages: 50 mg/kg in rats, 100 mg/kg in mice, 0.25 mg/kg
  • Administration: Oral gavage, IV

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(153.93 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 649.62
Formula

C31H25F2N5O7S

CAS No. 1445879-21-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=NC(=NC=C1C2=CC3=NC=C(C(=C3C=C2)NC4=CC(=CC(=C4)C(=O)O)OC5=CC(=CC(=C5)F)F)S(=O)(=O)NC6CC6)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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