Cat. No. 4593
Chemical Name: N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetra
Biological ActivityPotent 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.
Licensing InformationThis 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.
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.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Heinemann et al (2014) Inhibition of demethylases by GSK-J1/J4. Nature 514 E1. PMID: 25279926.
Kruidenier et al (2012) A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature 488 404. PMID: 22842901.
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Citations are publications that use Tocris products. Selected citations for GSK J1 include:
Lee et al (2016) Signalling couples hair follicle stem cell quiescence with reduced histone H3 K4/K9/K27me3 for proper tissue homeostasis. Cancer Metab 7 11278. PMID: 27080563.
Aspuria et al (2015) Succinate dehydrogenase inhibition leads to epithelial-mesenchymal transition and reprogrammed carbon metabolism. Nat Commun 2 21. PMID: 25671108.
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Keywords: GSK J1, supplier, GSKJ1, histone, demethylases, inhibitors, inhibits, UTX, JMJD3, H3K27, epigenetics, jumonji, demethylation, sgc, Tocris Bioscience, Histone Demethylase Inhibitor products