Bisindolylmaleimide IV (Synonyms: Arcyriarubin A,BIM IV) |
رقم الكتالوجGC14716 |
Bisindolylmaleimide IV (Arcyriarubin A) هو مثبط قوي لبروتين كيناز C (PKC) ، مع IC50s تتراوح من 0.1 إلى 0.55 ميكرومتر
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Cas No.: 119139-23-0
Sample solution is provided at 25 µL, 10mM.
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.
Cas No. | 119139-23-0 | SDF | |
المرادفات | Arcyriarubin A,BIM IV | ||
Chemical Name | 3,4-di-1H-indol-3-yl-1H-pyrrole-2,5-dione | ||
Canonical SMILES | O=C1NC(=O)C(=C1c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 | ||
Formula | C20H13N3O2 | M.Wt | 327.3 |
الذوبان | ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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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 |
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Quality Control & SDS
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- Purity: >97.00%
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Average Rating: 5
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