GSK 2837808A

Catalog No.S8590 Batch:S859001

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Technical Data

Formula

C31H25F2N5O7S
Molecular Weight 649.62 CAS No. 1445879-21-9
Solubility (25°C)* In vitro DMSO 100 mg/mL (153.93 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
2.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:

[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 Study:

[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

Selleck's GSK 2837808A has been cited by 1 publication

Metabolic lactate production coordinates vasculature development and progenitor behavior in the developing mouse neocortex [ Nat Neurosci, 2022, 25(7):865-875] PubMed: 35726058

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.