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Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase g9a

Ramzi F Sweis, Marina Pliushchev, Peter J Brown, Jun Guo, Fengling Li, David Maag, Andrew M Petros, Nirupama B Soni, Chris Tse, Masoud Vedadi, Michael R Michaelides, Gary G Chiang, William N Pappano

ACS Med Chem Lett. 2014 Jan 2;5(2):205-9.

PMID: 24900801

Abstract:

G9a is a histone lysine methyltransferase responsible for the methylation of histone H3 lysine 9. The discovery of A-366 arose from a unique diversity screening hit, which was optimized by incorporation of a propyl-pyrrolidine subunit to occupy the enzyme lysine channel. A-366 is a potent inhibitor of G9a (IC50: 3.3 nM) with greater than 1000-fold selectivity over 21 other methyltransferases.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP1527503112 A-366 A-366 1527503-11-2 Price
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