1197196-48-7
1197196-48-7 結(jié)構(gòu)式
基本信息
中文別名
G9A抑制劑(UNC0224)7-[3-(二甲基氨基)丙氧基]-2-(六氫-4-甲基-1H-1,4-二氮雜卓-1-基)-6-甲氧基-N-(1-甲基-4-哌啶基)-4-喹唑啉胺
英文別名
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)-
所屬類別
生物化工：激動劑抑制劑物理化學性質(zhì)
沸點641.0±65.0 °C(Predicted)
密度1.141±0.06 g/cm3(Predicted)
儲存條件2-8°C
儲存條件Sealed in dry,2-8°C
溶解度Soluble to 100 mM in 1eq. HCl and to 100 mM in DMSO
酸度系數(shù)(pKa)9.34±0.70(Predicted)
形態(tài)粉末
顏色White to yellow
常見問題列表
生物活性
UNC0224 是一種有效的選擇性的組蛋白甲基轉(zhuǎn)移酶 G9a 抑制劑，Ki 為 2.6 nM，IC50 值為 15 nM，Kd 為 23 nM。UNC0224 還有效抑制 GLP，IC50 值為 20-58 nM。UNC0224 對 SET7/9，SET8/PreSET7，PRMT3 和 JMJD2E 無活性。靶點
|
G9a 15 nM (IC 50 ) |
G9a 2.6 nM (Ki) |
G9a 23 nM (Kd) |
GLP 20-58 nM (IC 50 ) |
體外研究
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.