| CAS NO: | 119139-23-0 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Cas No. | 119139-23-0 |
| 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℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 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: |
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