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A homogeneous time-resolved fluorescence (HTRF)-based binding assay has been established to measure the binding of the histone methyltransferase (HMT) G9a to its inhibitor CJP702 (a biotin analog of the known peptide–pocket inhibitor, BIX-01294). This assay was used to characterize G9a inhibitors. As expected, the peptide–pocket inhibitors decreased the G9a–CJP702 binding signal in a concentration-dependent...
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