中文名称:
N-(1-环己基-4-哌啶基)-2-[六氢-4-异丙基-1H-1,4-二氮杂卓-1-基]-6-甲氧基-7-[3-(1-哌啶基)丙氧基]-4-喹唑啉胺
中文同义词:
N-(1-环己基-4-哌啶基)-2-[六氢-4-异丙基-1H-1,4-二氮杂卓-1-基]-6-甲氧基-7-[3-(1-哌啶基)丙氧基]-4-喹唑啉胺;G9A抑制剂(UNC0646)
英文同义词:
UNC0646;N-(1-cyclohexylpiperidin-4-yl)-2-(4-isopropyl-1,4-diazepan-1-yl)-6-Methoxy-7-(3-(piperidin-1-yl)propoxy)quinazolin-4-aMine;UNC0646/UNC-0646;N-(1-Cyclohexyl-4-piperidinyl)-2-[hexahydro-4-(1-methylethyl)-1H-1,4-diazepin-1-yl]-6-methoxy-7-[3-(1-piperidinyl)propoxy]-4-quinazolinamine;N-(1-Cyclohexyl-4-piperidinyl)-2-(4-isopropyl-1,4-diazepan-1-yl)- 6-methoxy-7-[3-(1-piperidinyl)propoxy]-4-quinazolinamine;(1-CYCLOHEXYL-PIPERIDIN-4-YL)-[2-(4-ISOPROPYL-[1,4]DIAZEPAN-1-YL)-6-METHOXY-7-(3-PIPERIDIN-1-YL-PROPOXY)-QUINAZOLIN-4-YL]-AMINE;UNC 0646;UNC0646;UNC-0646;CS-792
沸点
754.6±70.0 °C(Predicted)
密度
1.128±0.06 g/cm3(Predicted)
储存条件
Keep in dark place,Sealed in dry,2-8°C
溶解度
DMSO: soluble2mg/mL, clear (warmed)
酸度系数(pKa)
9.34±0.70(Predicted)
生物活性
UNC0646是一种选择性的组蛋白赖氨酸甲基转移酶(HMTase)抑制剂，作用于G9a和GLP，IC50分别为6 nM和15 nM 。在多种细胞系中活性较强，也能有效的将功能性活性于细胞毒性区分。
靶点
Target Value
G9a
(Cell-free assay) 6 nM
GLP
(Cell-free assay) 15 nM
G9a
(Cell-free assay)
6 nM
GLP
(Cell-free assay)
15 nM
体外研究
UNC0646 (Compound 6) has high cellular potency and excellent separation of functional potency versus cell toxicity in a variety of cell lines. UNC0646 is highly potent in reducing H3K9me2 levels and has low cell toxicity. UNC0646 reduces H3K9me2 levels with ICW IC 50 values of 26 nM, 10 nM, 12 nM, 14 nM, 68 nM, 86 nM and 10 nM in MDA-MB-231, MCF7, PC3, 22RV1, HCT116 wt, HCT 116 p53 -/- and IMR90 cell lines, respectively.
