138516-31-1

中文名稱 3-[1-(3-氨基丙基)-1H-吲哚-3-基]-4-(1-甲基-1H-吲哚-3-基)-1H-吡咯-2,5-二酮單乙酸鹽

英文名稱 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 2026/05/17 14:25:31

138516-31-1 結構式

基本信息物理化學性質安全數(shù)據(jù) 圖譜信息常見問題列表

基本信息

中文別名

3-[1-(3-氨基丙基)-1H-吲哚-3-基]-4-(1-甲基-1H-吲哚-3-基)-1H-吡咯-2,5-二酮單乙酸鹽

英文別名

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

物理化學性質

儲存條件-20°C

溶解度溶于二甲基亞砜

形態(tài)紅色粉末。

顏色Brown to reddish brown

安全數(shù)據(jù)

海關編碼2925199590

圖譜信息

3-[1-(3-氨基丙基)-1H-吲哚-3-基]-4-(1-甲基-1H-吲哚-3-基)-1H-吡咯-2,5-二酮單乙酸鹽(138516-31-1)核磁圖(¹HNMR)

常見問題列表

生物活性

Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) 是一種有效的選擇性蛋白激酶 C (PKC) 抑制劑，對大鼠腦 PKC 的 IC50 為 158 nM。Bisindolylmaleimide VIII acetate 對 PKC-α，PKC-βI，PKC-βII，PKC-γ，PKC-ε 的 IC50 分別為 53、195、163、213 和 175 nM。Bisindolylmaleimide VIII acetate 促進 Fas 介導的細胞凋亡 (apoptosis)，并抑制 T 細胞介導的自身免疫性疾病。

靶點

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 )

體外研究

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.

體內研究

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.