Name: GSK J1
Price: 225.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    GSK J1 is a potent and selective inhibitor of the histone H3 lysine 27 (H3K27) demethylase JMJD3, a Fe2+- and α-ketoglutarate-dependent oxygenase involved in a variety of physiological functions including the inflammatory response, with the half maximal inhibition concentration IC50 value of 60 nM [1].
    However, GSK J1 has restricted cellular permeability due to its highly polar carboxylate group, which plays a critical role in the binding of GSK J1 to JMJD3. In order to improve the cellular permeability, GSK J1 is esterified to mask the polarity generating an ethyl ester derivative that can be rapidly hydrolyzed to GSK J1 [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
    
    3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoic acid
    
    CAS Number
    
    1373422-53-7
    
    Molecular Formula
    
    C22H23N5O2
    
    Molecular Weight
    
    389.45
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥38.9 mg/mL in DMSO; insoluble in H2O; ≥51.2 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

GSK J1

GSK J1

Background

We Also Recommend

Obatoclax mesylate (GX15-070)

SGI-1776 free base

SMI-4a