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B-2464 Bisindolylmaleimide I, >99%

[GF 109203X] [Gö 6850] [BIM I] [Go 6850]

M.W. 412.49

C25H24N4O2

[133052-90-1]

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO (1 mg/ml).  Appearance:  Orange solid.  Disposal:  A

View the MSDS for this product

• A very potent inhibitor of A-group PKCs (IC50 = 8-20 nM); a less potent inhibitor of B-group PKCs (IC50 = 210-700 nM); and a much less potent inhibitor of a C-group PKC (PKCζ, 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 bisindolylmaleimide 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.

• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.