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,138516-31-1,结构式](https://www.chemicalbook.com/CAS/GIF/138516-31-1.gif)
- CAS号:138516-31-1
- 英文名:Bisindolylmaleimide VIII acetate salt
- 中文名: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
- CBNumber:CB32130296
- 分子式:C24H22N4O2
- 分子量:398.464
- MOL File:138516-31-1.mol
- 储存条件 :-20°C
- 溶解度 :Soluble in DMSO
- 形态 :Red powder.
- 颜色 :Brown to reddish brown
- 海关编码 :2925199590
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、用途与生产工艺
- 生物活性 Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) 是一种有效的选择性蛋白激酶 C (PKC) 抑制剂，对大鼠脑 PKC 的 IC50 为 158 nM。Bisindolylmaleimide VIII acetate 对 PKC-α，PKC-βI，PKC-βII，PKC-γ，PKC-ε 的 IC50 分别为 53、195、163、213 和 175 nM。Bisindolylmaleimide VIII acetate 促进 Fas 介导的细胞凋亡 (apoptosis)，并抑制 T 细胞介导的自身免疫性疾病。
-
靶点
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 )
-
体外研究
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. -
体内研究
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.
- 公司名称：APOLLO-NMR
- 联系电话：--
- 电子邮件：sales@apolloscientific.co.uk
- 国家：英国
- 产品数：6084
- 优势度：88
- 公司名称：Glentham Life Sciences
- 联系电话：--
- 电子邮件：info@glenthamls.com
- 国家：英国
- 产品数：1429
- 优势度：0
