GSK2837808A

SKU: orb1308248

Description

GSK2837808A

Research Area

Metabolism Research

Key Properties

• CAS Number: 1445879-21-9
• MW: 649.62
• Purity: 99.78% (May vary between batches)
• Formula: C₃₁H₂₅F₂N₅O₇S
• SMILES: COc1ncc(-c2ccc3c(Nc4cc(Oc5cc(F)cc(F)c5)cc(c4)C(O)=O)c(cnc3c2)S(=O)(=O)NC2CC2)c(OC)n1
• Target: Dehydrogenase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (6.16 mM);DMSO:102 mg/mL (157.01 mM)

Bioactivity

• Target IC50:
  LDHB:1.9 nM|LDHA:1.9 nM
• 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.
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• 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).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, GSK2837808A, GSK-2837808A, Lactate Dehydrogenase, LDHB, LDH, LDHA, Inhibitor

Compound Identifiers

PubChem CID

71533725