GSK-J1
JMJ H3K27 Demethylase inhibitor (Non-cell permeable) / Potent and selective inhibitor of jumonji H3K27 histone demethylases JMJD3 and UTX (IC50 = 60 nM, human JMJD3). This is the first known inhibitor selective for the H3K27me3-specific JMJ subfamily which binds to the active catalytic site of the enzyme. The COOH group confers cell impermeability and as such is useful as a standard in in vitro assays. A cell permeable ethyl ester analog is also available.
Biochemicals & reagents
1373422-53-7
1) Kruidenier et al. (2012), A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response; Nature, 488 404
RT
TARGET: Protein demethylase -- PATHWAY: Chromatin; Posttranslational modification -- RESEARCH AREA: Epigenetics