1. Epigenetics TGF-beta/Smad Apoptosis
  2. PKC Apoptosis
  3. Bisindolylmaleimide VIII

Bisindolylmaleimide VIII  (Synonyms: Ro 31-7549; Bis VIII)

目录号: HY-129624
产品使用指南

Bisindolylmaleimide VIII (Ro 31-7549) 是一种有效的选择性蛋白激酶 C (PKC) 抑制剂,对大鼠脑 PKCIC50 为 158 nM。Bisindolylmaleimide VIII 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 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。

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Bisindolylmaleimide VIII Chemical Structure

Bisindolylmaleimide VIII Chemical Structure

CAS No. : 125313-65-7

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Bisindolylmaleimide VIII 的其他形式现货产品:

Other Forms of Bisindolylmaleimide VIII:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Bisindolylmaleimide VIII (Ro 31-7549) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively[1]. Bisindolylmaleimide VIII facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases[1][2].

IC50 & Target

Rat Brain PKC

158 nM (IC50)

PKCα

53 nM (IC50)

PKC-βI

195 nM (IC50)

PKC-βII

163 nM (IC50)

PKCγ

213 nM (IC50)

PKCε

175 nM (IC50)

体外研究
(In Vitro)

Bisindolylmaleimide VIII (5 μM; 8, 12 hours) 显著增加 TRA-8 诱导的细胞死亡,呈时间依赖性和剂量依赖性[2]
Bisindolylmaleimide VIII (5 μM; 6 hours) 与 TRA-8 联合处理后,4 h procaspase-8 显著降低,6 h完全消失[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

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.

Apoptosis Analysis[2]

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.
体内研究
(In Vivo)

Bisindolylmaleimide VIII (100 μg;i.p;每隔一天服用三次),结合 toTRA-8,肿瘤几乎完全消退。单独使用 Bisindolylmaleimide VIII未引起肿瘤明显消退[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-8-week-old female NOD/SCID mice[2].
Dosage: 100 μg
Administration: i.p.; every other day for three doses
Result: Resulted in nearly complete tumor regression combined toTRA-8.
分子量

398.46

Formula

C24H22N4O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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