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Product Details
Synonyms N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine
Product Type Chemical
Formula C22H23N5O2
MW 389.5
CAS 1373422-53-7
Purity Chemicals ≥95%
Appearance Solid.
Solubility Soluble in DMSO.
Declaration Manufactured by SynKinase.
Other Product Data Target: JMJD3 - UTX | Kinase Group: N/A | Substrate: N/A
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
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Product Specification Sheet
Datasheet Download PDF
GSK-J1 is a potent inhibitor of the H3K27 histone demethylases JMJD3 (KDM6B) and UTX (KDM6A), with IC50 values of 28nM and 53nM, respectively. GSK-J1 also has less potent inhibitory activity against KDM5B, KDM5C and KDM5A, with IC50 values of 170, 550 and 6,800nM, respectively. It shows no activity against other histone demethylases (IC50 >20μM), and displays no significant inhibitory activity against 100 protein kinases at a concentration of 30μM.
Product References
  1. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response: J. Kruidenier, et al.; Nature 488, 404 (2012)
  2. Inhibition of demethylases by GSK-J1/J4: B. Heinemann, et al.; Nature 514, E1 (2014)
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