Bisindolylmaleimide VIII acetate Ro 31-7549 acetate; Bis VIII acetate|cas:138516-31-1|西域试剂

Bisindolylmaleimide VIII acetate Ro 31-7549 acetate; Bis VIII acetate,99.70%

产品编号：Bellancom-129624A| CAS NO：138516-31-1| 分子式：C₂₆H₂₆N₄O₄| 分子量：458.51

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货号	价格	库存与货期
Bellancom-129624A	￥1900.00	杭州北京（现货）
Bellancom-129624A	￥3000.00	杭州北京（现货）
Bellancom-129624A	￥6300.00	杭州北京（现货）
Bellancom-129624A	￥10100.00	杭州北京（现货）

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Bisindolylmaleimide VIII acetate Ro 31-7549 acetate; Bis VIII acetate

产品介绍

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-β_I，PKC-β_II，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。

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-β_I, PKC-β_II, PKC-γ, PKC-ε, respectively. Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.

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.

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

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
(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.

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

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.

体内研究

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

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.

体内研究

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

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.

性状

Solid

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