Catalog Number: 4593
Chemical Name: N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine
Biological Activity
Potent inhibitor of the H3K27 histone demethylases JMJD3 (KDM6B) and UTX (KDM6A) (IC50 values are 28 and 53 nM respectively). Also inhibits KDM5B, KDM5C and KDM5A (IC50 values are 170, 550 and 6,800 nM respectively). Exhibits no activity against a panel of other histone demethylases (IC50 >20 μM), and displays no significant inhibitory activity against 100 protein kinases at a concentration of 30 μM. Ethyl ester derivative also available.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in ethanol
  • Purity:
  • Storage:
    Desiccate at RT
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the GSK J1 probe summary on the SGC website.
Other Product-Specific Information:
Background References
  1. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.
    Kruidenier et al.
    Nature, 2012;488:404
  2. Inhibition of demethylases by GSK-J1/J4.
    Heinemann et al.
    Nature, 2014;514:E1

The citations listed below are publications that use Tocris products. Selected citations for GSK J1 include:

Showing Results 1 - 2 of 2

  1. Signalling couples hair follicle stem cell quiescence with reduced histone H3 K4/K9/K27me3 for proper tissue homeostasis.
    Authors: Lee Et al.
    Cancer Metab
  2. Succinate dehydrogenase inhibition leads to epithelial-mesenchymal transition and reprogrammed carbon metabolism.
    Authors: Aspuria Et al.
    Nat Commun
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