Pricing updated 2019-06-26. Prices are subject to change without notice.
A-366 is a potent, peptide-competitive inhibitor of the lysine methyltransferase G9a (IC50 = 3.3 nM).1 It displays greater than 1,000-fold selectivity over 21 other methyltransferases.1 A-366 significantly reduces the cellular levels of dimethylation on histone 3 at lysine 9 (H3K9Me2) in PC3 cells without reducing total histone 3, H3K27Me3, or H3K36Me2.1 It also blocks the interaction of the methyl lysine reader protein Spindlin1 with H3K4me3 by binding with a Spindlin1 Tudor domain (Kd = 111 nM).2 See the Structural Genomics Consortium (SGC) website for more information.
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1. Sweis, R.F., Pliushchev, M., Brown, P.J., et al. Discovery and development of potent and selective inhibitors of histone methyltransferase G9a ACS Med.Chem.Lett. 5(2), 205-209 (2014).
Wagner, T., Greschik, H., Burgahn, T., et al. Identification of a small-