1227098-15-8
中文名稱
(1E,6E)-1,7-雙(3,4-二甲氧基苯基)-4-(4-羥基-3-甲氧基亞芐基)庚-1,6-二烯-3,5-二酮
英文名稱
1,6-Heptadiene-3,5-dione, 1,7-bis(3,4-dimethoxyphenyl)-4-[(4-hydroxy-3-methoxyphenyl)methylene]-, (1E,6E)-
CAS
1227098-15-8
分子式
C31H30O8
分子量
530.57
MOL 文件
1227098-15-8.mol
1227098-15-8 結(jié)構(gòu)式
基本信息
中文別名
化合物NF-ΚB-IN-1(1E,6E)-1,7-雙(3,4-二甲氧基苯基)-4-(4-羥基-3-甲氧基亞芐基)庚-1,6-二烯-3,5-二酮
英文別名
NF-κB-IN-1AC17 NF-κB-IN-1
NF-kB-IN-1(AC17)
(1E,6E)-1,7-Bis(3,4-dimethoxyphenyl)-4-(4-hydroxy-3-methoxybenzylidene)hepta-1,6-diene-3,5-dione
1,6-Heptadiene-3,5-dione, 1,7-bis(3,4-dimethoxyphenyl)-4-[(4-hydroxy-3-methoxyphenyl)methylene]-, (1E,6E)-
物理化學性質(zhì)
沸點732.0±60.0 °C(Predicted)
密度1.233±0.06 g/cm3(Predicted)
酸度系數(shù)(pKa)9.27±0.31(Predicted)
形態(tài)Solid
顏色Light yellow to yellow
常見問題列表
生物活性
NF-κB-IN-1，一種 4-亞芳基姜黃素類似物，是有效的 NF-κB 信號通路抑制劑。NF-κB-IN-1 直接抑制 IKK 來阻斷 NF-κB 的激活。NF-κB-IN-1 可有效抑制肺癌細胞的活力并減弱 A549 細胞的克隆活性。靶點
IKK
體外研究
NF-κB-IN-1 (compound 17) (0.001-100 μM; 72 h) inhibits the growth of A549, H1944, H460 and H157 cells, with GI
50
s of 0.72, 0.07, 0.13, and 0.16 μM, respectively.
NF-κB-IN-1 (0.5-25 μM; pretreated for 30 min or 4 h) potently blocks the IκB phosphorylation and degradation in A549 cells.
NF-κB-IN-1 (0.1-100 μM; pretreated for 30 min) dose-dependently inhibits the TNFα-induced nuclear translocation of NF-κB in A549 cells, with an IC
50
s of 1.0 μM.
NF-κB-IN-1 (0.1-0.4 μM; 9 d) inhibits lung cancer clonogenic activity.
Cell Viability Assay
| Cell Line: | A549, H1944, H460 and H157 cells |
| Concentration: | 0.001, 0.01, 0.1, 1, 10, 100 μM |
| Incubation Time: | 72 hours |
| Result: | Decreased viability of lung adenocarcinoma cells A549 and H1944, quamous cell carcinoma cells H157, and large cell carcinoma cells H460 in a dose-dependent manner. |
Western Blot Analysis
| Cell Line: | A549 cells |
| Concentration: | 0.5, 1.0, 2.5, 5.0, 10.0, 25.0 μM |
| Incubation Time: | Pretreated for 30 min or 4 h |
| Result: |
Blocked IκB phosphorylation, with an IC
50
of 2.8 μM.
Blocked IκB degradation in a dose-dependent manner. |