Name: GSK J4 HCl
Price: 280.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    GSK J4 is a potent cell-permeable inhibitor of the histone H3 lysine 27 (H3K27) demethylase JMJD3, an essential component of regulatory transcriptional chromatin complexes, with the half maximal inhibition concentration IC50 value > 50 μM in vitro [1].
    GSK J4 is an ethyl ester derivative of GSK J1, which is a potent JMJD3 inhibitor (IC50: 60 nM) with restricted cellular permeability due to the highly polar carboxylate group, and rapidly hydrolyzed by macrophage esterase upon administration leading to the generation of pharmacologically relevant intracellular concentration of GSK-J1 [1].
    GSK J4 has also been found to dose-dependently inhibit the production of tumor-necrosis factor-α (TNF-α), a LPS-driven cytokine involved in various fnflammatory disorders, with IC50 value of 9μM [1].
    
    [1] Kruidenier L, Chung CW, Cheng Z, Liddle J, Che K, Joberty G, Bantscheff M, Bountra C, Bridges A, Diallo H, Eberhard D, Hutchinson S, Jones E, Katso R, Leveridge M, Mander PK, Mosley J, Ramirez-Molina C, Rowland P, Schofield CJ, Sheppard RJ, Smith JE, Swales C, Tanner R, Thomas P, Tumber A, Drewes G, Oppermann U, Patel DJ, Lee K, Wilson DM. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012 Aug 16;488(7411):404-8. doi: 10.1038/nature11262.
- Properties
  - Alternative Name
    
    ethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate
    
    CAS Number
    
    1373423-53-0(free base)
    
    Molecular Formula
    
    C24H27N5O2·HCl
    
    Molecular Weight
    
    453.96
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥13.9 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Silasi M, You Y, et al. "Human Chorionic Gonadotropin modulates CXCL10 Expression through Histone Methylation in human decidua." Sci Rep. 2020;10(1):5785. PMID:32238853
    2. Li N, Yang L, et al. "BET bromodomain inhibitor JQ1 preferentially suppresses EBV-positive nasopharyngeal carcinoma cells partially through repressing c-Myc." Cell Death Dis. 2018 Jul 9;9(7):761. PMID:29988031

GSK J4 HCl

GSK J4 HCl

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