Name: GSK621
Price: 202.00 USD

- Overview
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    Background
    
    GSK621 is a specific and potent agonist of AMP-activated protein kinase (AMPK) with IC50 values ranging from 13 to 30 µM for cell lines [1].
    AMPK is a heterotrimeric serine/threonine kinase. It is a sensor of cellular energy. It regulates multiple cellular metabolic pathways. Activation of AMPK inactivates the phosphorylation of acetyl-Coa carboxylase (ACC), and hence inhibits the biosynthesis of fatty acid. Activation of AMPK also inhibits protein synthesis that is dependent on mammalian target of rapamycin complex 1. AMPK also promotes autophagy, fatty acid oxidation, glucose uptake and glycolysis [1].
    In cells, at the opposite, GSK621 showed more potency to activate AMPK than A-769662, based on the ACC phosphorylation level. In MOLM-14 cells, 200 µM A-769662 is just as potent as 30 µM GSK621 to induce the phosphorylation of ULK1 (S555) and ACC (S79), two direct AMPK substrates. In AML cell lines (OCI-AML3, HL-60 and MOLM-14) and primary AML samples, the phosphorylation at AMPKα T172, a marker of AMPK activation, was markedly increased, and the phosphorylation of ULK1 (S555) and ACC (S79) was stimulated by GSK621 [1].
    In animals with xenograft MOLM-14 cells, intraperitoneal injection of GSK621 at 30 mg/kg twice daily reduced leukemia growth and markedly extended survival compared to treatment with 10 mg/kg GSK621 twice daily or vehicle. These results correlated to increased AMPK activity indicated by the induction of apoptosis and increased ACC S79 phosphorylation [1].
- Properties
  - Categories
    
    AMPK agonist
    
    Alternative Name
    
    6-chloro-5-(2'-hydroxy-3'-methoxy-[1,1'-biphenyl]-4-yl)-3-(3-methoxyphenyl)-1H-pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione
    
    CAS Number
    
    1346607-05-3
    
    Molecular Formula
    
    C26H20ClN3O5
    
    Molecular Weight
    
    489.91
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥28.5 mg/mL in DMSO
    
    Storage
    
    Store at 2-8°C
    
    SMILES
    
    COC1=CC=CC(C2=CC=C(N3C(Cl)=CC(NC(N4C5=CC=CC(OC)=C5)=O)=C3C4=O)C=C2)=C1O
    
    * For Research Use Only
- Reference
  - 1. Gulisudumu Maitiabula, Feng Tian, et al. " Liver PP2A-Cα protects from parenteral nutrition-associated hepatic steatosis." Cell Mol Gastroenterol Hepatol. 2022 May 26;S2352-345X(22)00090-X. PMID: 35643235
    2. Leeanna El-Houjeiri, Elite Possik, et al. "The transcription factors TFEB and TFE3 link the FLCN-AMPK signaling axis to innate immune response and pathogen resistance."bioRxiv. 2018 November 6.

Documents

COA (Certificate Of Analysis)

MSDS (Material Safety Data Sheet)

Datasheet

GSK621

GSK621

Background

Documents

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