Chemical Name: N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine
Biological ActivityGSK J1 is a 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.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Inhibition of demethylases by GSK-J1/J4.
Heinemann et al.
A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.
Kruidenier et al.
Citations for GSK J1
The citations listed below are publications that use Tocris products. Selected citations for GSK J1 include:
2 Citations: Showing 1 - 2
Signalling couples hair follicle stem cell quiescence with reduced histone H3 K4/K9/K27me3 for proper tissue homeostasis.
Authors: Lee Et al.
Cancer Metab 2016;7:11278
Succinate dehydrogenase inhibition leads to epithelial-mesenchymal transition and reprogrammed carbon metabolism.
Authors: Aspuria Et al.
Nat Commun 2015;2:21
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