1197196-48-7
1197196-48-7 结构式
基本信息
中文别名
G9A抑制剂(UNC0224)7-[3-(二甲基氨基)丙氧基]-2-(六氢-4-甲基-1H-1,4-二氮杂卓-1-基)-6-甲氧基-N-(1-甲基-4-哌啶基)-4-喹唑啉胺
英文别名
CS-1635UNC 0224
UNC-0224
UNC0224
UNC 0224
N-Debenzyl-N-Methyl-O-deMethyl-O-(3-diMethylaMinopropyl)-BIX 01294
7-[3-(dimethylamino)propoxy]-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
7-[3-(Dimethylamino)propoxy]-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6-methoxy-N-(1-methyl-4-piperidinyl)-4-quinazolinamine
4-QuinazolinaMine, 7-[3-(diMethylaMino)propoxy]-2-(hexahydro-4-Methyl-1H-1,4-diazepin-1-yl)-6-Methoxy-N-(1-Methyl-4-piperidinyl)-
所属类别
生物化工：激动剂抑制剂物理化学性质
沸点641.0±65.0 °C(Predicted)
密度1.141±0.06 g/cm3(Predicted)
储存条件2-8°C
储存条件Sealed in dry,2-8°C
溶解度Soluble to 100 mM in 1eq. HCl and to 100 mM in DMSO
酸度系数(pKa)9.34±0.70(Predicted)
形态粉末
颜色White to yellow
常见问题列表
生物活性
UNC0224 是一种有效的选择性的组蛋白甲基转移酶 G9a 抑制剂，Ki 为 2.6 nM，IC50 值为 15 nM，Kd 为 23 nM。UNC0224 还有效抑制 GLP，IC50 值为 20-58 nM。UNC0224 对 SET7/9，SET8/PreSET7，PRMT3 和 JMJD2E 无活性。靶点
|
G9a 15 nM (IC 50 ) |
G9a 2.6 nM (Ki) |
G9a 23 nM (Kd) |
GLP 20-58 nM (IC 50 ) |
体外研究
In G9a ECSD and CLOT assays, the IC
50
values of 43 nM and 57 nM for UNC0224 (Compound 10), respectively. In GLP ECSD and CLOT assays, the IC
50
values of 50 nM and 58 nM for UNC0224, respectively. In ITC experiments, the K
d
value of UNC0224 to the G9a protein is 23 nM.