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Bisindolylmaleimide V Sale

(Synonyms: 双吲哚马来酰亚胺,BIM V) 目录号 : GC17239

A S6K inhibitor

Bisindolylmaleimide V Chemical Structure

Cas No.:113963-68-1

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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
别名 双吲哚马来酰亚胺,BIM V
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
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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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