中文同义词:
7-[2-[2-(二甲基氨基)乙氧基]乙氧基]-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;G9A抑制剂(UNC0321)
英文同义词:
UNC0321;7-(2-(2-(diMethylaMino)ethoxy)ethoxy)-6-Methoxy-2-(4-Methyl-1,4-diazepan-1-yl)-N-(1-Methylpiperidin-4-yl)quinazolin-4-aMine;7-[2-[2-(Dimethylamino)ethoxy]ethoxy]-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6-methoxy-N-(1-methyl-4-piperidinyl)-4-quinazolinamine;UNC0321(UNC-0321);UNC 0321; UNC-0321; UNC0321; UNC-0321;4-Quinazolinamine, 7-[2-[2-(dimethylamino)ethoxy]ethoxy]-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6-methoxy-N-(1-methyl-4-piperidinyl)-
沸点
664.7±65.0 °C(Predicted)
密度
1.150±0.06 g/cm3(Predicted)
酸度系数(pKa)
9.34±0.70(Predicted)
生物活性
UNC0321 是一种有效的选择性组蛋白甲基转移酶 G9a 抑制剂，Ki 为 63 pM，IC50 值为 6-9 nM。UNC0321 还抑制 GLP，IC50 值为 15-23 nM。UNC0321 对 SET7/9，SET8/PreSET7，PRMT3 和 JMJD2E 无活性。
靶点
G9a
63 pM (Ki)
G9a
6-9 nM (IC 50 )
GLP
15-23 nM (IC 50 )
G9a
63 pM (Ki)
G9a
6-9 nM (IC 50 )
体外研究
In G9a ECSD and CLOT assays, the IC 50 values of 9 nM and 6 nM for UNC0321 (Compound 29), respectively. In GLP ECSD and CLOT assays, the IC 50 values of 15 nM and 23 nM for UNC0321, respectively.
UNC0321 (Compound 3) reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 11 μM.
