UNC0224
G9a histone methyl transferase inhibitor / UNC0224 is a potent inhibitor of histone methyltransferases G9a / EHMT2 (IC50 = 15 nM) and GLP / EHMT1 (IC50 ~ 39 nM) but not SET7/9 and SET8.1-3 Has been employed, as part of a small molecule cocktail, to reprogram somatic cells to pluripotent stem cells.4
Biochemicals & reagents
1197196-48-7
1 Liu et al. (2009), Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a; J. Med. Chem., 52 7950 2 Liu et al. (2010), Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxyquinazolines; J. Med. Chem., 53 5844 3 Leenders et al. (2019), Novel SAR for quinazoline inhibitors of EHMT1 and EHMT2; Bioorg. Med. Chem. Lett., 29 2516 4 Guan et al. (2022), Chemical reprogramming of human somatic cells to pluripotent stem cells; Nature, 605 325
-20°C
TARGET: Protein methyltransferase -- PATHWAY: Chromatin; Posttranslational modification -- RESEARCH AREA: Epigenetics; Stem cells