Name: GSK503
Price: 306.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    GSK503 is a potent inhibitor of EZH2.
    Enhancer of zeste homolog 2 (EZH2) is a histone-lysine N-methyltransferase enzyme that catalyses trimethylation of lysine 27 in histone 3 (H3K27me3), and then induces chromatin compaction and consequently inhibits target genes transcription.
    GSK503 is a potent EZH2 inhibitor with anticancer activity. In human melanoma cells, GSK503 significantly reduced H3K27me3 levels, induced G1 cell cycle arrest and slowed down cell growth [1].
    In mice, GSK503 induced reversible weight loss by ~10%. In mice with skin melanomas, GSK503 reduced H3K27me3 levels in tumour and stromal cells, and significantly reduced the emergence of new skin melanomas. Also, GSK503 significantly inhibited the proliferation of tumour cells. In C57Bl/6 mice xenografted murine B16-F10 melanoma cells, GSK503 significantly reduced H3K27me3 levels and inhibited tumor growth. Also, GSK503 inhibited lymph node and lung metastases of melanoma and reduced lung nodule counts. GSK503 increased the expression of deoxycytidine kinase (DCK), adenosylmethionine decarboxylase 1 (AMD1) and WD repeat domain 19 (WDR19), which were EZH2 target genes [1].
- Properties
  - Alternative Name
    
    (Z)-N-((2-hydroxy-4,6-dimethylpyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carbimidic acid
    
    CAS Number
    
    1346572-63-1
    
    Molecular Formula
    
    C31H38N6O2
    
    Molecular Weight
    
    526.67
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥21.65 mg/mL in DMSO; insoluble in H2O; ≥26.85 mg/mL in EtOH with gentle warming
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. R.Martin Mateos, T.M.De Assuncao, et al. "Enhancer of Zeste Homologue 2 inhibition attenuates TGF-β dependent hepatic stellate cell activation and liver fibrosis." Cellular and Molecular Gastroenterology and Hepatology Available online 15 September 2018.
    2. Sarmento OF, Svingen PA, et al. "The Role of the Histone Methyltransferase Enhancer of Zeste Homolog 2 (EZH2) in the Pathobiological Mechanisms Underlying Inflammatory Bowel Disease (IBD)." J Biol Chem. 2017 Jan 13;292(2):706-722. PMID:27909059

GSK503

GSK503

Background

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