Bisindolylmaleimide II

Cat. No. 4128

Bisindolylmaleimide II C27H26N4O2 [137592-45-1]

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Chemical Name: 3-(1H-Indol-3-yl)-4-[1-[2-(1-methyl-2-pyrrolidinyl)ethyl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione

Biological Activity

Potent, ATP-competitive protein kinase C (PKC) inhibitor (IC50 = 0.01 μM). Displays selectivity for PKC over protein kinase A (PKA) and phosphorylase kinase (PK) (IC50 values are 0.75 and 2μM for PK and PKA respectively). Also displays potent, noncompetitive antagonism at nicotinic cholinergic receptors (IC50 ~ 0.03 μM for inhibition of catecholamine secretion in nicotine-stimulated PC-12 cells).

Technical Data

M.Wt:
438.52
Formula:
C27H26N4O2
Solubility:
Soluble to 100 mM in DMSO
Purity:
>97 %
Storage:
Store at -20°C
CAS No:
137592-45-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Mahata et al (2002) Chromaffin cell catecholamine secretion: bisindolylmaleimide compounds exhibit novel and potent antagonist effects at the nicotinic cholinergic receptor in pheochromocytoma cells. Mol.Pharmacol. 61 1340. PMID: 12021395.

Toullec et al (1991) The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J.Biol.Chem. 266 15771. PMID: 1874734.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for Bisindolylmaleimide II include:

Jones et al (2004) Regulation of SHP-1 tyrosine phosphatase in human platelets by serine phosphorylation at its C terminus. PLoS One 279 40475. PMID: 15269224.

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Keywords: Bisindolylmaleimide II, supplier, protein, kinase, C, PKC, inhibits, inhibitors, nicotinic, cholinergic, acetylcholine, nAChRs, antagonists, antagonism, catecholamines, potent, Tocris Bioscience, Protein Kinase C Inhibitor products

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