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B-6191 Bisindolylmaleimide I, Hydrochloride,
>99%
[GF 109203X, HCl Salt] [Gö 6850, HCl Salt] [2-[1-(3-Dimethylaminopropyl)-indol-3-yl]-3-(indol-3
-yl)maleimide, HCl Salt] [3-[1-(3-Dimethylaminopropyl)-1H-indol-3-yl]-4-(-1
H-indol-3-yl)-1H-pyrrole-2,5-dione, HCl Salt]
| M.W. 448.95 |
C25H24N4O2•HCl
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Storage: Store at or below -20 ºC in the dark.
Solubility: Soluble in water, DMSO, or methanol. Appearance:
Reddish-orange solid. Disposal: A
 | Water-soluble form of Bisindolylmaleimide I, Cat. No. B-2464. Kuchera,
S. et al. Agents Actions 39: C169 (1993). |
| BIM I is a very potent inhibitor of A-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 bisindolymaleimide 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. |
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