Bisindolylmaleimide V (Synonyms: BIM V, Ro 316045) |
رقم الكتالوجGC17239 |
Bisindolylmaleimide V هو عنصر تحكم سلبي منفذ للخلايا لدراسات تثبيط بروتين كيناز C بقيمة IC تزيد عن 100 ميكرومتريمنع Bisindolylmaleimide V تنشيط بروتين كيناز المحفز بالميتوجين p70s6k / p85s6k (S6K) في الجسم الحي باستخدام IC50 من 8 ميكرومتر
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Cas No.: 113963-68-1
Sample solution is provided at 25 µL, 10mM.
Bisindolylmaleimide V (BIM V, Ro 31-6045) is a negative control for protein kinase C (PKC)-inhibitory activity with Kd value of 100 ?M [1]. Ro 31-6045 also inhibited S6K activity with IC50 value of 8 ?M [4].
Protein kinase C plays an important role in the transduction of signals from a variety of mediators across the cell membrane. PKC regulates cell proliferation, secretion, and gene expression. Inhibition of PKC may provide therapy for diseases such as rheumatoid arthritis, cancer and AIDS [2][3].
Bisindolylmaleimide V is the inactive analogue of the protein kinase C inhibitor Ro 31-8220. Bisindolylmaleimide IV was very weak and inhibited [3H] N-methyl scopolamine binding only at the highest concentration used [1]. Ro 31-6045 also inhibited mitogen-stimulated protein kinase p70s6k/p85s6k (S6K) activity. In fibroblasts, Ro 31-6045 inhibited S6K with IC50 value of 8 ?M [4].
References:
Lazareno S, Popham A, Birdsall NJ. Muscarinic interactions of bisindolylmaleimide analogues. Eur J Pharmacol. 1998 Nov 6;360(2-3):281-4.
Toullec D, Pianetti P, Coste H, et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem. 1991 Aug 25;266(24):15771-81.
Davis PD, Hill CH, Lawton G, et al. Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. J Med Chem. 1992 Jan;35(1):177-84.
Marmy-Conus N, Hannan KM, Pearson RB. Ro 31-6045, the inactive analogue of the protein kinase C inhibitor Ro 31-8220, blocks in vivo activation of p70(s6k)/p85(s6k): implications for the analysis of S6K signalling. FEBS Lett. 2002 May 22;519(1-3):135-40.
Cas No. | 113963-68-1 | SDF | |
المرادفات | BIM V, Ro 316045 | ||
Chemical Name | 3,4-di(1H-indol-3-yl)-1-methyl-1H-pyrrole-2,5-dione | ||
Canonical SMILES | CN1C(C(C2=CNC3=CC=CC=C23)=C(C1=O)C4=CNC5=CC=CC=C45)=O | ||
Formula | C21H15N3O2 | M.Wt | 341.36 |
الذوبان | DMF: 20 mg/ml,DMF:PBS (pH 7.2) (1:9): 0.1 mg/ml,DMSO: 20 mg/ml,Ethanol: 20 mg/ml | 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 | 2.9295 mL | 14.6473 mL | 29.2946 mL |
5 mM | 0.5859 mL | 2.9295 mL | 5.8589 mL |
10 mM | 0.2929 mL | 1.4647 mL | 2.9295 mL |
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- Purity: >98.00%
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