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

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Bisindolylmaleimide VIII acetate (Synonyms: Ro 31-7549 acetate; Bis VIII acetate) 纯度: 99.70%

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。

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

Bisindolylmaleimide VIII acetate Chemical Structure

CAS No. : 138516-31-1

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生物活性

Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate 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 acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases[2].

IC50 & Target

Rat Brain PKC

158 nM (IC50)

PKC-α

53 nM (IC50)

PKC-βI

195 nM (IC50)

PKC-βII

163 nM (IC50)

PKC-γ

213 nM (IC50)

PKC-ε

175 nM (IC50)

体外研究
(In Vitro)

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[2].
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[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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.

体内研究
(In Vivo)

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[2].

Shanghai Jinpan Biotech Co Ltd 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: IP; every other day for three doses
Result: Resulted in nearly complete tumor regression combined toTRA-8.

分子量

458.51

Formula

C26H26N4O4
CAS 号

138516-31-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (545.24 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1810 mL 10.9049 mL 21.8098 mL
5 mM 0.4362 mL 2.1810 mL 4.3620 mL
10 mM 0.2181 mL 1.0905 mL 2.1810 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.54 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.54 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Wilkinson SE, et al. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993 Sep 1;294 ( Pt 2):335-7.

    [2]. Ohtsuka T, et al. Bisindolylmaleimide VIII enhances DR5-mediated apoptosis through the MKK4/JNK/p38 kinase and the mitochondrial pathways. J Biol Chem. 2002 Aug 9;277(32):29294-303.

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