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UNC0321 is an inhibitor of the histone methyltransferases G9a and G9a-like protein (GLP; IC50s = 9 and 15 nM, respectively).1 It is selective for G9a and GLP over SET domain-containing protein 7 (SET7), SET8, protein arginine methyltransferase 3 (PRMT3), and jumonji domain-containing 2E (JMJD2E; IC50s = >10,000 nM for all). UNC0321 decreases the levels of dimethylated lysine 9 on histone H3 (H3K9me2) in MDA-MB-231 cells (IC50 = 11 µM) without inducing cytotoxicity (EC50 = >40 µM).2
WARNING This product is not for human or veterinary use.
1. Protein lysine methyltransferase G9a inhibitors: Design, synthesis, and structure activity relationships of 2,4-
2. Optimization of cellular activity of G9a inhibitors 7-