UNC 0224

中文名称:

UNC 0224

中文同义词:

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

英文名称:

UNC 0224

英文同义词:

UNC 0224;4-QuinazolinaMine, 7-[3-(diMethylaMino)propoxy]-2-(hexahydro-4-Methyl-1H-1,4-diazepin-1-yl)-6-Methoxy-N-(1-Methyl-4-piperidinyl)-;N-Debenzyl-N-Methyl-O-deMethyl-O-(3-diMethylaMinopropyl)-BIX 01294;CS-1635;UNC-0224; UNC0224; UNC 0224;7-[3-(Dimethylamino)propoxy]-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6-methoxy-N-(1-methyl-4-piperidinyl)-4-quinazolinamine;7-[3-(dimethylamino)propoxy]-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine

CAS号:

1197196-48-7

分子式:

C26H43N7O2

分子量:

485.67

EINECS号:

相关类别:

细胞生物学试剂;Amines, Aromatics, Heterocycles, Inhibitors, Pharmaceuticals, Intermediates Fine Chemicals

Mol文件:

1197196-48-7.mol

沸点 

641.0±65.0 °C(Predicted)

密度 

1.141±0.06 g/cm3(Predicted)

储存条件 

Sealed in dry,2-8°C

酸度系数(pKa)

9.34±0.70(Predicted)

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 )

G9a 15 nM (IC 50 )

G9a 2.6 nM (Ki)

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.