UNC 0224 是一种有效的选择性组蛋白甲基转移酶 G9a 抑制剂，Ki 为 2.6 nM，IC50 为 15 nM，Kd 为 23 nM。 UNC 0224 还有效抑制 b\u003eGLP，检测依赖的 IC50 值为 20-58 nM。 UNC 0224 对 SET7/9、SET8/PreSET7、PRMT3 和 JMJD2E 无效。
| Cas No. | 1197196-48-7 |
| 化学名 | 7-[3-(dimethylamino)propoxy]-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine |
| Canonical SMILES | CN1CCCN(CC1)C2=NC3=CC(=C(C=C3C(=N2)NC4CCN(CC4)C)OC)OCCCN(C)C |
| 分子式 | C26H43N7O2 |
| 分子量 | 485.67 |
| 溶解度 | ≥ 48.6mg/mL in DMSO, ≥ 44 mg/mL in EtOH |
| 储存条件 | Store at 4℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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. |
