UNC0321 |
| カタログ番号GC37856 |
UNC0321 は、強力で選択的なヒストンメチルトランスフェラーゼ G9a 阻害剤で、Ki は 63 pM、アッセイ依存の IC50 値は 6 ～ 9 nM です。 UNC0321 は、15 ～ 23 nM のアッセイ依存 IC50 値で GLP も阻害します。 UNC0321 は、SET7/9、SET8/PreSET7、PRMT3、および JMJD2E に対して非アクティブです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1238673-32-9
Sample solution is provided at 25 µL, 10mM.
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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 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.
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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