Home>>Signaling Pathways>> Microbiology & Virology>> CMV>>Bisindolylmaleimide IV

Bisindolylmaleimide IV Sale

(Synonyms: 双吲哚马来酰亚胺IV,Arcyriarubin A,BIM IV) 目录号 : GC14716

A PKC inhibitor

Bisindolylmaleimide IV Chemical Structure

Cas No.:119139-23-0

规格 价格 库存 购买数量
1mg
¥228.00
现货
5mg
¥997.00
现货
10mg
¥1,761.00
现货
25mg
¥3,523.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

产品描述

IC50: from 0.10 to 0.55 μM

Bisindolylmaleimide IV is a protein kinase C (PKC) inhibitor.

The enzyme family protein kinase C2 (PKC) occupies a central role in the transduction of signals from a variety of mediators across the cell membrane.3 Receptor occupation by a number of hormones, cytokines, neurotransmitters, and growth factors results in activation of PKC via activation of phospholipase C through either a G protein mechanism or a tyrosine kinase mechanism. PKC then propagates the signal by phosphorylation of proteins on serine or threonine, with ATP as cosubstrate, resulting in modification of the properties of these proteins. Thus PKC appears to regulate mechanisms of cell proliferation, secretion, and gene expression.

In vitro: Bisindolylmaleimide IV was identified as a cell permeable inhibitor of protein kinase C (PKC) with IC50 values from 0.10 to 0.55 μM. Bisindolylmaleimide IV was designed to be more discriminative than its parent compound staurosporine, the non-selective PKC inhibitor. In addition, Bisindolylmaleimide IV also found to be able to inhibit protein kinase A with IC50 values ranging from 2 to 11.8 μM [1, 2].

In vivo: Animal study found that, in neonatal rats, high glucose levels could induce the hypertrophy of cardiomyocytes. Ro-31-8220, a analog of bisindolylmaleimide VIII, was able to reverse the effect of high glucose on the cardiac myocytes, which might be through PKC/NF-κB/c-Fos pathway [3].

Clinical trial: So far, no clinical study has been conducted.

References:
[1] Davis, P. D.,Hill, C.H.,Lawton, G., et al. Inhibitors of protein kinase C. 1.1 2,3-bisarylmaleimides. Journal of Medicinal Chemistry 35, 177-184 (1992).
[2] Toullec, D. ,Pianetti, P.,Coste, H., et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. The Journal of Biological Chemisty 266(24), 15771-15781 (1991).
[3] Zhang, W.  B. et al. Reverse effect of protein kinase C inhibitor Ro-31-8220 on the hypertrophy of cardiomyocytes of neonatal rats induced by high glucose levels. Chinese Journal of Pathophysiology. 2009-08.

Chemical Properties

Cas No. 119139-23-0 SDF
别名 双吲哚马来酰亚胺IV,Arcyriarubin A,BIM IV
化学名 3,4-di-1H-indol-3-yl-1H-pyrrole-2,5-dione
Canonical SMILES O=C1NC(=O)C(=C1c1c[nH]c2ccccc12)c1c[nH]c2ccccc12
分子式 C20H13N3O2 分子量 327.3
溶解度 ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide 储存条件 Store at -20°C
General tips 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 3.0553 mL 15.2765 mL 30.553 mL
5 mM 0.6111 mL 3.0553 mL 6.1106 mL
10 mM 0.3055 mL 1.5277 mL 3.0553 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

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 g 每只动物给药体积 ul 动物数量
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GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置