NF-κB-IN-1, a 4-arylidene crucumin analogue, is a potent NF-κB signaling pathway inhibitor. NF-κB-IN-1 directly inhibits IKK to block NF-κB activation. NF-κB-IN-1 effectively inhibits the viability of lung cancer cells and attenuates the clonogenic activity of A549 cells.
IC50&Target
IKK
体外研究
NF-κB-IN-1 (compound 17) (0.001-100 μM; 72 h) inhibits the growth of A549, H1944, H460 and H157 cells, with GI50s 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 IC50s 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 IC50 of 2.8 μM.
Blocked IκB degradation in a dose-dependent manner.
分子式
C31H30O8
分子量
530.57
CAS号
1227098-15-8
运输条件
Room temperature in continental US; may vary elsewhere.