1320288-17-2
中文名稱
N-(1-環(huán)己基-4-哌啶基)-2-[六氫-4-異丙基-1H-1,4-二氮雜卓-1-基]-6-甲氧基-7-[3-(1-哌啶基)丙氧基]-4-喹唑啉胺
英文名稱
UNC0646
CAS
1320288-17-2
分子式
C36H59N7O2
分子量
621.9
MOL 文件
1320288-17-2.mol
更新日期
2024/12/23 17:39:05
1320288-17-2 結(jié)構(gòu)式
基本信息
中文別名
G9A抑制劑(UNC0646)N-(1-環(huán)己基-4-哌啶基)-2-[六氫-4-異丙基-1H-1,4-二氮雜卓-1-基]-6-甲氧基-7-[3-(1-哌啶基)丙氧基]-4-喹唑啉胺
英文別名
CS-792UNC0646
UNC0646/UNC-0646
UNC 0646
UNC0646
UNC-0646
N-(1-cyclohexylpiperidin-4-yl)-2-(4-isopropyl-1,4-diazepan-1-yl)-6-Methoxy-7-(3-(piperidin-1-yl)propoxy)quinazolin-4-aMine
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
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
4-Quinazolinamine, N-(1-cyclohexyl-4-piperidinyl)-2-[hexahydro-4-(1-methylethyl)-1H-1,4-diazepin-1-yl]-6-methoxy-7-[3-(1-piperidinyl)propoxy]-
所屬類別
生物化工：激動劑抑制劑物理化學(xué)性質(zhì)
沸點(diǎn)754.6±70.0 °C(Predicted)
密度1.128±0.06 g/cm3(Predicted)
儲存條件Keep in dark place,Sealed in dry,2-8°C
溶解度DMSO：可溶，2mg/mL，澄清（加熱）
酸度系數(shù)(pKa)9.34±0.70(Predicted)
形態(tài)粉末
顏色白色至米色
常見問題列表
生物活性
UNC0646是一種選擇性的組蛋白賴氨酸甲基轉(zhuǎn)移酶(HMTase)抑制劑，作用于G9a和GLP，IC50分別為6 nM和15 nM 。在多種細(xì)胞系中活性較強(qiáng)，也能有效的將功能性活性于細(xì)胞毒性區(qū)分。靶點(diǎn)
| Target | Value |
|
G9a
(Cell-free assay) | 6 nM |
|
GLP
(Cell-free assay) | 15 nM |
體外研究
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.