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UNC0224

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Chemical Structure| 1197196-48-7 同义名 : -
CAS号 : 1197196-48-7
货号 : A596599
分子式 : C26H43N7O2
纯度 : 99%+
分子量 : 485.665
MDL号 : MFCD18251564
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 16 mg/mL(32.94 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Protein lysine methyltransferase G9a can catalyze methylation of lysine 9 of histone H3 (H3K9) and lysine 373 (K373) of p53, and is found to be overexpressed in human cancers. UNC0224 is a potent and selective G9a inhibitor with IC50 value of 15nM and Kd value of 23nM, respectively. Also, it potently inhibited GLP with an IC50 value of 20nM and 58nM in the Thioglo assay and AlphaScreen, respectively.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.06mL

0.41mL

0.21mL

10.30mL

2.06mL

1.03mL

20.59mL

4.12mL

2.06mL
参考文献

[1]Liu F, Chen X, 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, Chen X, 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.