3-[1-(3-氨基丙基)-1H-吲哚-3-基]-4-(1-甲基-1H-吲哚-3-基)-1H-吡咯-2,5-二酮单乙酸盐
3-[1-(3-氨基丙基)-1H-吲哚-3-基]-4-(1-甲基-1H-吲哚-3-基)-1H-吡咯-2,5-二酮单乙酸盐
![3-[1-(3-氨基丙基)-1H-吲哚-3-基]-4-(1-甲基-1H-吲哚-3-基)-1H-吡咯-2,5-二酮单乙酸盐 结构式](https://img.chemicalbook.com/CAS/GIF/138516-31-1.gif)
3-[1-(3-氨基丙基)-1H-吲哚-3-基]-4-(1-甲基-1H-吲哚-3-基)-1H-吡咯-2,5-二酮单乙酸盐 性质
| 储存条件 | -20°C |
|---|---|
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 红色粉末。 |
| 颜色 | 棕至红棕色 |
3-[1-(3-氨基丙基)-1H-吲哚-3-基]-4-(1-甲基-1H-吲哚-3-基)-1H-吡咯-2,5-二酮单乙酸盐 用途与合成方法
|
Rat Brain PKC 158 nM (IC 50 ) |
PKC-α 53 nM (IC 50 ) |
PKC-βI 195 nM (IC 50 ) |
PKC-βII 163 nM (IC 50 ) |
PKC-γ 213 nM (IC 50 ) |
PKC-ε 175 nM (IC 50 ) |
Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate; 5 μM; 8, 12 hours) dramatically increases TRA-8-induced cell death in time-dependent and TRA-8 dose-dependent manners.
Bisindolylmaleimide VIII acetate (5 μM; 6 hours) significantly decreases procaspase-8 at 4 h and completely disappeares at 6 h after the combined treatment with TRA-8.
Apoptosis Analysis
| Cell Line: | 1321N1 cells |
| Concentration: | 5 μM |
| Incubation Time: | 8, 12 hours |
| Result: | Dramatically increased TRA-8-induced cell death in time-dependent and TRA-8 dose-dependent manners. |
Western Blot Analysis
| Cell Line: | 1321N1 cells |
| Concentration: | 5 μM |
| Incubation Time: | 6 hours |
| Result: | Significantly decreased procaspase-8 at 4 h and completely disappeared at 6 h. |
Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate; 100 μg; IP; every other day for three doses) results in nearly complete tumor regression combined toTRA-8. The treatment with Bisindolylmaleimide VIII acetate alone does not induce significant tumor regression.
| Animal Model: |
6-8-week-old female NOD/SCID mice.
|
| Dosage: | 100 μg |
| Administration: | IP; every other day for three doses |
| Result: | Resulted in nearly complete tumor regression combined toTRA-8. |
