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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 2024/12/24 22:28:46
138516-31-1 結(jié)構(gòu)式 138516-31-1 結(jié)構(gòu)式

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(xué)性質(zhì)

儲(chǔ)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(guān)編碼2925199590

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(duì)大鼠腦 PKC 的 IC50 為 158 nM。Bisindolylmaleimide VIII acetate 對(duì) 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(jìn) Fas 介導(dǎo)的細(xì)胞凋亡 (apoptosis),并抑制 T 細(xì)胞介導(dǎo)的自身免疫性疾病。
靶點(diǎn)

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(nèi)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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