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Description: BRD9539 is a potent and selective inhibitor that inhibits G9a activity with an IC50 of 6.3 uM, it also inhibits euchromatin histone methyltransferase 2 (EHMT2). Post-translational modifications of histones alter chromatin structure and play key roles in gene expression and specification of cell states. Small molecules that target chromatin-modifying enzymes selectively are useful as probes and have promise as therapeutics, although very few are currently available. G9a (also named euchromatin histone methyltransferase 2 (EHMT2)) catalyzes methylation of lysine 9 on histone H3 (H3K9), a modification linked to aberrant silencing of tumor-suppressor genes, among others.
References: ACS Chem Biol. 2012 Jul 20; 7(7):1152-7.
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