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Bisindolylmaleimide V

Catalog No.
B6066
negative control for protein kinase C (PKC)-inhibitory activity
Grouped product items
SizePriceStock Qty
1mg
$67.00
Ship with 5-10 days
5mg
$304.00
Ship with 5-10 days
10mg
$539.00
Ship with 5-10 days
25mg
$1,179.00
Ship with 5-10 days

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Background

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

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt341.36
Cas No.113963-68-1
FormulaC21H15N3O2
SolubilitySoluble in DMSO
Chemical Name3,4-di(1H-indol-3-yl)-1-methyl-1H-pyrrole-2,5-dione
SDFDownload SDF
Canonical SMILESCN1C(C(C2=CNC3=CC=CC=C23)=C(C1=O)C4=CNC5=CC=CC=C45)=O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

Bisindolylmaleimide V