Home Metabolism Dehydrogenase inhibitor - LDH inhibitor GSK 2837808A For research use only.

GSK 2837808A

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

GSK 2837808A Chemical Structure

CAS No. 1445879-21-9

Purity & Quality Control

Batch: S859001 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.11%
99.11

GSK 2837808A Related Products

Signaling Pathway

Dehydrogenase Signaling Pathways

Dehydrogenase Signaling Pathway

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
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]
Cell Research 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.
In Vivo
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]
Animal Research 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

Chemical Information & Solubility

Molecular Weight 649.62 Formula

C31H25F2N5O7S
CAS No. 1445879-21-9 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (153.93 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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. )

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

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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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