Bisindolylmaleimide I (hydrochloride) - CAS:176504-36-2

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Bisindolylmaleimide I (hydrochloride) (Synonyms:双吲哚基马来酰亚胺 I .盐酸盐；GF109203X hydrochloride; Go 6850 hydrochloride)

目录号 : KCM12004 CAS No. : 176504-36-2 纯度 : ≥98%

Data Sheet SDS 产品使用指南

Bisindolylmaleimide I (BIM I) is a highly selective, cell-permeable, and reversible PKC inhibitor (K = 14 nM) that is structurally similar to the poorly selective PKC inhibitor staurosporine . It acts as a competitive inhibitor for the ATP binding site of PKC and shows high selectivity for PKCα, β1, β2, γ, δ, and ε isozymes. BIM I directly inhibits glycogen synthase kinase 3 (GSK3) in primary adipocyte lysates (IC = 360 nM) and in GSK3β immunoprecipitates derived from rat epididymal adipocytes (IC = 170 nM). It also competitively antagonizes the serotonin (5-HT) receptor subtype 5-HT with a K value of 61 nM.

规格	价格	是否有货	数量
500μg		In-stock
1mg		In-stock
5mg		In-stock

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生物活性

Bisindolylmaleimide I (hydrochloride) is a cell-permeable and reversible PKC inhibitor (IC₅₀ of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I (hydrochloride) is also a GSK-3 inhibitor.

IC₅₀&Target

Bovine brain PKC PKC-βII PKC-βI

10 nM (IC₅₀) 16 nM (IC₅₀) 17 nM (IC₅₀)

体外研究

Bisindolylmaleimide I (hydrochloride) (5 μM) inhibits α - thrombin induced phosphorylation of P47.
Bisindolylmaleimide I (hydrochloride) (0-1 μM) inhibits DNA synthesis in resting state swiss 3T3 cells.
Bisindolylmaleimide I (hydrochloride) (5 μM) can reduce GSK-3 activity in adipocyte lysate to 25.1 ± 4.3%.
Bisindolylmaleimide I (hydrochloride) (10 μM, 24 hours) inhibits the release of extracellular vesicles and microbubbles (EMVs) from PC3 cells.
Bisindolylmaleimide I (hydrochloride) (10 μM, 24 hours) enhances the cytotoxicity of 5-fluorouracil.

体内研究

Bisindolylmaleimide I (hydrochloride) (0.02 mg/kg, intraperitoneal injection) ）Reduce the elevated levels of NLRP3, P-PKC α, and PKC α in the mechanical ventilation (MV) group of mice.
Bisindolylmaleimide I (hydrochloride) (0-20 mg/kg, intraperitoneal injection) reduced the average frequency of quinolone induced vomiting in shrews.

Animal Model:	Quinpirole-treated shrews
Dosage:	0-20 mg/kg
Administration:	i.p.
Result:	Reduced the mean frequency of Quinpirole-induced vomiting. Blocked Quinpirole-mediated ERK1/2 phosphorylation in shrew brainstems.

分子式

C₂₅H₂₄N₄O₂^.HCl

分子量

448.94

CAS号

176504-36-2

中文名称

双吲哚基马来酰亚胺 I .盐酸盐;3-[1-[3-(二甲基氨基)丙基]-1H-吲哚-3-基]-4-(1H-吲哚-3-基)-1H-吡咯-2,5-二酮单盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (139.22 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2275 mL	11.1373 mL	22.2747 mL
5 mM	0.4455 mL	2.2275 mL	4.4549 mL
10 mM	0.2227 mL	1.1137 mL	2.2275 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。-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 → 90% (20% SBE-β-CD in saline)

Solubility: 2.08 mg/mL (4.63 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.63 mM) 的均匀悬浊液，悬浊液可⽤于⼝服和腹腔注射。

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。

纯度： ≥98%

Data Sheet

SDS

产品使用指南

Hers I, et al. The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity. FEBS Lett. 1999 Nov 5;460(3):433-6.

Kosgodage US, et al. Chloramidine/Bisindolylmaleimide-I-Mediated Inhibition of Exosome and Microvesicle Release and Enhanced Efficacy of Cancer Chemotherapy. Int J Mol Sci. 2017 May 9;18(5):1007.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器