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.
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