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Bisindolylmaleimide IV蛋白激酶C(PKC)抑制剂

Bisindolylmaleimide IV

产品编号:C4316
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1mg ¥533.00 10-15 工作日发货
5mg ¥2,405.00 10-15 工作日发货
10mg ¥4,264.00 10-15 工作日发货
25mg ¥9,334.00 10-15 工作日发货

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Sample solution is provided at 25 µL, 10mM.

质量控制

质量控制和MSDS

批次:

化学结构

Bisindolylmaleimide IV

Bisindolylmaleimide IV Dilution Calculator

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Bisindolylmaleimide IV Molarity Calculator

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化学性质

CAS号 119139-23-0 SDF Download SDF
别名 Arcyriarubin A,BIM IV
化学名 3,4-di-1H-indol-3-yl-1H-pyrrole-2,5-dione
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
物理性状 A crystalline solid 运输条件 试用装:蓝冰运输。
其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

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.