A-366, a chemical probe, is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC 50 s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC 50 =182.6 nM). A-366 displays high affinity at human histamine H3 receptor (K i =17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families.
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