GSK-J1 (1373422-53-7) is a 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 GSK-J1 is useful as a standard in in vitro assays. A cell permeable ethyl ester analog is also available, see GSK-J4 (cat.# 10-1394).
1) Kruidenier et al. (2012), A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response; Nature, 488 404
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