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GSK2837808A

Catalog No. T15435   CAS 1445879-21-9

GSK2837808A is a potent and selective inhibitor of lactate dehydrogenase A (LDHA) (IC50s: 1.9 and 14 nM for LDHA and LDHB, respectively).

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GSK2837808A Chemical Structure
GSK2837808A, CAS 1445879-21-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 40.00
5 mg In stock $ 123.00
10 mg In stock $ 197.00
25 mg In stock $ 359.00
50 mg In stock $ 481.00
100 mg In stock $ 698.00
1 mL * 10 mM (in DMSO) In stock $ 177.00
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Purity: 99.78%
Purity: 98.25%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GSK2837808A is a potent and selective inhibitor of lactate dehydrogenase A (LDHA) (IC50s: 1.9 and 14 nM for LDHA and LDHB, respectively).
Targets&IC50 LDHB:1.9 nM, LDHA:1.9 nM
In vitro GSK2837808A inhibits lactate production in hypoxia but at higher concentrations than in normoxia (EC50=10 μM). It also reduces ECAR (EC50=10 μM). LDH inhibition by GSK2837808A alters multiple metabolic pathways in Snu398 cells. GSK2837808A rapidly and profoundly inhibits lactate production rates in multiple cancer cell lines including hepatocellular and breast carcinomas. GSK2837808A potency does not correlate with LDHA, LDHB, or the total LDH expression levels. The potency of GSK2837808A across 30 cancer cell lines with different LDHA and LDHB expression levels range from 400 nM to no effect (EC50 reported as 30 μM).
In vivo GSK2837808A (p.o.; 50 mg/kg in rats; 100 mg/kg in mice) treatment, causes blood compound levels at or below the detection limit of 2.5 ng/mL. Clearance following IV infusion of GSK2837808A at 0.25 mg/kg is displayed to be 69 mL/minute/kg in rats and it exceeds the animal liver blood flow.
Molecular Weight 649.62
Formula C31H25F2N5O7S
CAS No. 1445879-21-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 95 mg/mL (146.24 mM)

TargetMolReferences and Literature

1. Billiard J, et al. Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells. Cancer Metab. 2013 Sep 6;1(1):19.

TargetMolCitations

1. Chen C, Zhang X, Wang Y, et al. Translational and Post-translational Control of Human Naïve versus Primed Pluripotency. iScience. 2021: 103645. 2. Zhang Y T, Xing M L, Fang H H, et al.Effects of lactate on metabolism and differentiation of CD4+T cells.Molecular Immunology.2023, 154: 96-107.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Bioactive Compounds Library Max NO PAINS Compound Library Anti-Cancer Metabolism Compound Library Glycometabolism Compound Library Glutamine Metabolism Compound Library Bioactive Compound Library Metabolism Compound Library Anti-Metabolism Disease Compound Library

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Keywords

GSK2837808A 1445879-21-9 Metabolism Dehydrogenase Inhibitor inhibit LDH Lactate Dehydrogenase GSK-2837808A inhibitor

 

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