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 ActivityBisindolylmaleimide II is a 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).
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Tocris products are intended for laboratory research use only, unless stated otherwise.
The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.
Toullec et al.
Chromaffin cell catecholamine secretion: bisindolylmaleimide compounds exhibit novel and potent antagonist effects at the nicotinic cholinergic receptor in pheochromocytoma cells.
Mahata et al.
Citations for Bisindolylmaleimide II
The citations listed below are publications that use Tocris products. Selected citations for Bisindolylmaleimide II include:
2 Citations: Showing 1 - 2
Selective modulation of tonically active GABAA receptor functional subgroups by G-proteins and protein kinase C.
Authors: O'Neill & Sylantyev
Exp Biol Med (Maywood) 2018;243:1046
Regulation of SHP-1 tyrosine phosphatase in human platelets by serine phosphorylation at its C terminus.
Authors: Jones Et al.
PLoS One 2004;279:40475
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Bisindolylmaleimide II (BII) was used to block PKC in hippocampal granule cells. Such a block enhances activity of GABA receptors and, as a sequence, increases effect of competitive antagonists of GABA on root mean square noise (RMS) amplitude of holding current in electrophysiological recording. Figure: changes of RMS after application of SR 95531 and SR 95531 + Picrotoxin. BII makes significant an effect of SR 95531 applied alone.