UNC0321是高亲和性G9a抑制剂，Ki为63 pM。UNC0321是第一个皮摩尔级G9a抑制剂，也是迄今为止G9a抑制剂中活性最强的。
CAS：1238673-32-9
分子式：C27H45N7O3
分子量：515.69
纯度：98%
存储：Store at -20°C

Background:

UNC0321 is a potent and selective G9a inhibitor with Ki of 63 pM, UNC0321 is the first G9a inhibitor with picomolar potency and the most potent G9a inhibitor to date.IC50 value: 63 pM(Ki); 9 nM (ECSD assay) [1]Target: G9aIt was found that replacing the 5-carbon chain in compound 13 with an ethoxyethyl chain resulted in compound 29{UNC0321} (IC50 = 6 nM (CLOT) and 9 nM (ECSD)), the most potent G9a inhibitor to date. 29 had a Morrison Ki of 63 pM and was about 40-fold more potent than 10 (Morrison Ki = 2.6 nM) and 250-fold more potent than 3a (Morrison Ki = 16 nM) in this G9a MCE assay. UNC0321 potentially useful small molecule tools for the biomedical research community to investigate the biology of G9a and its role in chromatin remodeling as well as PTMs of other proteins.

[1]. Liu F, et al. Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. J Med Chem. 2010 Aug 12;53(15):5844-57. [2]. Liu F, et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54(17):6139-50.