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UNC 0224
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
UNC 0224图片
CAS NO:1197196-48-7
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
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 SMILESCN1CCCN(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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation 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.