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Bisindolylmaleimide V

目录号 GC17239

negative control for protein kinase C (PKC)-inhibitory activity

规格 价格 库存 购买数量
1mg
¥784.00
现货
5mg
¥3,486.00
现货
10mg
¥6,188.00
现货
25mg
¥13,510.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

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.

Chemical Properties

Cas No. 113963-68-1 SDF
化学名 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
分子式 C21H15N3O2 分子量 341.36
溶解度 DMF: 20 mg/ml,DMF:PBS (pH 7.2) (1:9): 0.1 mg/ml,DMSO: 20 mg/ml,Ethanol: 20 mg/ml 储存条件 Store at -20°C
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

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