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B-6191 Bisindolylmaleimide I, Hydrochloride Salt, >99%

[GF 109203X, HCl Salt] [Gö 6850, HCl Salt] [BIM I, HCl] [Go 6850, HCl Salt]

M.W. 448.95

C25H24N4O2•HCl

[176504-36-2]

Storage:  Store at or below -20 ºC in the dark.  Solubility:  Soluble in water, DMSO, or methanol.  Appearance:  Reddish-orange solid.  Disposal:  A

View the MSDS for this product

• Water-soluble form of Bisindolylmaleimide I, Cat. No. B-2464.  Kuchera, S. et al.  "Anti-inflammatory properties of the protein kinase C inhibitor, 3-[1-[3-(dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H- pyrrole-2,5-dione monohydrochloride (GF109203X) in the PMA-mouse ear edema model."  Agents Actions 39:  C169-C173 (1993).

• BIM I is 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).

• See the product description for Bisindolylmaleimide I, Cat. No. B-2464, for a cautionary note regarding the effects of ATP concentrations on apparent inhibitory potencies.

• Please request Technical Note #9 for additional information.

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