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138516-31-1

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
英文名称 Bisindolylmaleimide VIII acetate salt
CAS 138516-31-1
分子式 C24H22N4O2
分子量 398.464
MOL 文件 138516-31-1.mol
更新日期 2024/09/04 11:44:07
138516-31-1 结构式 138516-31-1 结构式

基本信息

中文别名
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
英文别名
Bis VIII acetate
RO 31-7549 ACETATE
BISINDOLYLMALEIMIDE VIII ACETATE SALT
BisindolylMaleiMide VIII . AcOH [Ro 31-7549]
3-[1-(3-Aminopropyl)-1H-indol-3-yl]-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione monoacetate

物理化学性质

储存条件-20°C
溶解度溶于二甲基亚砜
形态红色粉末。
颜色Brown to reddish brown

安全数据

海关编码2925199590

常见问题列表

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.
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