Bisindolylmaleimide VIII (acetate) (Synonyms: BIM VIII,Ro 31-7549) |
| رقم الكتالوجGC13226 |
Bisindolylmaleimide VIII (acetate) (Ro 31-7549 acetate) هو مثبط قوي وانتقائي للبروتين كيناز C (PKC) مع IC 50 من 158 نانومتر لدماغ الفئران PKC.
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Cas No.: 138516-31-1
Sample solution is provided at 25 µL, 10mM.
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IC50: 158 nM for rat brain PKC
Bisindolylmaleimide VIII is a protein kinase C (PKC) inhibitor.
The protein kinase C (PKC) consists of a family of closely related isoenzymes mediating various signal transduction processes. The ten isoenzymes that have been currently identified can be divided into three families on the basis of their different requirements for activation. Members of the conventional PKC family are Ca2+ and phospholipid-dependent and are activated by diacylglycerols and phorbol esters.
In vitro: Previous study found that bisindolylmaleimides carrying a straight-chain alkyl side-chain bearing a cationic substituent, such as Ro 31-7549 (bisindolylmaleimide VIII) and Ro 31-8220, showed a significant improvement in potency over the simple bisindolylmaleimides. For bisindolylmaleimide VIII, a further improvement in potency was obtained by restricting the position of the amine substituent. Moreove, unlike the indolocarbazole, staurosporine, which displayed 2-fold selectivity for PKC-β over the other examined isoenzymes, bisindolylmaleimide VIII exhibited a slight selectivity for PKC-α over the other isoenzymes. Compounds such as bisindolylmaleimide VIII carrying a straight-chain alkyl side-chain with the cationic substituent were found to be equipotent as inhibitors of PKC-β, PKC-γ and PKC-ε [1].
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 [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Wilkinson, S. E.,Parker, P.J. and Nixon, J.S. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochemistry Journal 294, 335-337 (1993).
[2] 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. | 138516-31-1 | SDF | |
| المرادفات | BIM VIII,Ro 31-7549 | ||
| Chemical Name | 3-[1-(3-aminopropyl)-1H-indol-3-yl]-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione, acetate | ||
| Canonical SMILES | O=C(N1[H])C(C2=CN(C)C3=C2C=CC=C3)=C(C4=CN(CCCN)C5=C4C=CC=C5)C1=O.CC(O)=O | ||
| Formula | C24H22N4O2 • C2H4O2 | M.Wt | 458.5 |
| الذوبان | 5mg/mL in DMSO, 5mg/mL in DMF | 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 | 2.181 mL | 10.9051 mL | 21.8103 mL |
| 5 mM | 0.4362 mL | 2.181 mL | 4.3621 mL |
| 10 mM | 0.2181 mL | 1.0905 mL | 2.181 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)
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