GSK-J1 (Free acid)(J48-904B)
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Description :JMJ H3K27 Demethylase Inhibitor (Cell Imperm)
CAS Registry Number :1373422-53-7
Molecular Formula :C22H23N5O2
Appearance :Pale yellow powder
Molecular Weight :389.5
Solubilization :May be dissolved in DMSO (20 mg/ml, warm)
Storage and Stability :Store desiccated as supplied at ambient temperature for up to 2 years. Store solutions at -20oC for up to 3 months.
Scientific Background :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.
1. L Kruidenier et al. Nature 2012 488:404
Molecular Structure :
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Research Areas :Cancer, Cell Cycle, Inflammation