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B-2464 Bisindolylmaleimide I, >99%
[GF 109203X] [Gö 6850] [2-[1-(3-Dimethylamino-propyl)indol-3-yl]-3-(1
H-indol-3-yl)maleimide]
[3-[1-(3-Dimethylaminopropyl)-1H-indol-3-yl]-4-(1 H-indol-3-yl)-1H-pyrrole-2,5-dione]
| M.W. 412.49 |
C25H24N4O2
|
[133052-90-1] |
Storage: Store at or below -20 ºC. Solubility:
Soluble in DMSO (1 mg/ml); store at -20 ºC. Appearance: Orange
solid. Disposal: A
 | A very potent inhibitor of A-group PKCs (IC50 =
8-20 nM); a less potent inhibitor of B-group PKCs (IC50
= 5.8 µM). Martiny-Baron, G. et al. "Selective inhibition of protein
kinase C isozymes by the indolocarbazole Gö 6976." J. Biol. Chem.
268: 9194-9197 (1993). (Please request Technical Note #2 for additional
information on PKC nomenclature.) |
| Kinase inhibitor with improved selectivity for PKC over several
serine/threonine and tyrosine kinases (PKA, IC50 = 2
µM; phosphorylase kinase, IC50 = 700 nM; EGFR-kinase,
IC50 >100 µM) as compared to staurosporine. Toullec,
D. et al. "The bisindolymaleimide GF 109203X is a potent and
selective inhibitor of protein kinase C." J. Biol. Chem. 266:
15771-15781 (1991). |
| CAUTIONARY NOTE: BIM I shows a Ki = 14 nM
on a cell-free, partially purified PKC mixture but potencies of 200-900 nM
in cellular assays. Inhibition shows competitive kinetics versus ATP; since
ATP levels are generally very high in cells, the potency of BIM I is
substantially reduced in whole-cell assays. |
| BIM I is one of the most widely used PKC inhibitors. See
Bisindolylmaleimide I, Hydrochloride, Cat. No. B-6191, for a water-soluble
form of this compound. |
| Please request Technical Note #9 for additional information. |
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