UNC 0224 |
| Catalog No.GC15688 |
A potent inhibitor of G9a histone methyltransferase
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1197196-48-7
Sample solution is provided at 25 µL, 10mM.
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UNC0224 is a potent and selective G9a inhibitor with IC50 of 15 nM in the G9a Thioglo assay.IC50 value: 15 nM [1]Target: G9aUNC0224 (Compound 8) also potently inhibited GLP with an IC50 of 20 nM and 58 nM in the Thioglo assay and and AlphaScreen, respectively. 8 was more than 1000-fold selective for G9a over SET7/9 (a H3K4 HMT) and SET8/PreSET7 (a H4K20 HMT) in Thioglo-based biochemical assays [1] [2].
References:
[1]. Liu F, et al. Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a. J Med Chem. 2009 Dec 24;52(24):7950-3.
[2]. 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.
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