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 CAS#: 138516-31-1

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

中文名称	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
中文同义词	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;BISINDOLYLMALEIMIDE VIII醋酸盐;化合物BISINDOLYLMALEIMIDE VIII ACETATE;RO 31-7549 ACETATE; BIS VIII ACETATE;3-(1-(3-氨基丙基)-1H-吲哚-3-基)-4-(1-甲基-1H-吲哚-3-基)-1H-吡咯-2,5-二酮乙酸盐
英文名称	Bisindolylmaleimide VIII acetate salt
英文同义词	BisindolylMaleiMide VIII . AcOH [Ro 31-7549];BISINDOLYLMALEIMIDE VIII ACETATE SALT;RO 31-7549 ACETATE;3-[1-(3-Aminopropyl)-1H-indol-3-yl]-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione monoacetate;Bis VIII acetate;1H-Pyrrole-2,5-dione, 3-[1-(3-aminopropyl)-1H-indol-3-yl]-4-(1-methyl-1H-indol-3-yl)-, acetate (1:1);protein,Bisindolylmaleimide VIII acetate,Ro 31-7549,Inhibitor,inhibit,Fas,Bis VIII,Apoptosis,autoimmune,Protein kinase C,diseases,kinase,cell-mediated,Bisindolylmaleimide VIII,PKC;3-(1-(3-Aminopropyl)-1H-indol-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione acetate
CAS号	138516-31-1
分子式	C24H22N4O2
分子量	398.464
EINECS号
相关类别	对照品;inhibitor
Mol文件	138516-31-1.mol
结构式

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

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.

安全信息

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