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B-8777 Bisindolylmaleimide XI, Hydrochloride Salt,
>99%
[Ro 32-0432] [2-{8-[(Dimethylamino)methyl]-6,7,8,9-tetrahydropyrido[1,2-
a]indol-3-yl}-3-(1-methylindol-3-yl)maleimide, HCl Salt] [3-{8-[(Dimethylamino)methyl]-6,7,8,9-tetrahydropyrido[1,2-
a]indol-10-yl}-4-(1-methylindol-3-yl)-1H -pyrrole-2,5-dione, HCl
Salt]
| M.W. 489.02 |
C28H28N4
O2 •HCl |
Storage: Store at or below -20 ºC. Solubility:
Soluble in DMSO. Disposal: A
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Orally active, potent and selective inhibitor
of PKC; IC50 = 21 nM for rat brain PKC. Slightly
less potent for the inhibition of PKCε (IC50 = 108
nM) than for the group A PKCs (IC50 = 9-37 nM).
Wilkenson, S.E. et al. Biochem. J. 294: 335-337
(1993). (Please request Technical Note #2.) |
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Other kinases are inhibited at much higher
concentrations, e.g., PKA (IC50 = 8.6 µM),
phosphorylase kinase (IC50 = 1.1 µM) and myosin light
chain kinase (IC50 = 17.8 µM). Bit, R.A. et al.
J. Med. Chem. 36: 21-29 (1993). |
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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. |
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