Bisindolylmaleimide II

Catalog #: 4128
4 Citations Datasheet

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Bisindolylmaleimide II | CAS No. 137592-45-1 | Protein Kinase C Inhibitors

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Description: Potent PKC inhibitor; also potent nAChR antagonist

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

Purity: ≥97%

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Product Details

Citations (4)

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Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

Bisindolylmaleimide 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).

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.
Toullec et al.
J.Biol.Chem., 1991;266:15771
Chromaffin cell catecholamine secretion: bisindolylmaleimide compounds exhibit novel and potent antagonist effects at the nicotinic cholinergic receptor in pheochromocytoma cells.
Mahata et al.
Mol.Pharmacol., 2002;61:1340

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Citations for Bisindolylmaleimide II

The citations listed below are publications that use Tocris products. Selected citations for Bisindolylmaleimide II include:

4 Citations: Showing 1 - 4

Contributing mechanisms underlying desensitization of cholecystokinin-induced activation of primary nodose ganglia neurons.
Authors: James H Et al.
Am J Physiol Cell Physiol 2020;318:C787-C796
Small Molecule Inhibitor Screen Reveals Calcium Channel Signaling as a Mechanistic Mediator of Clostridium difficile TcdB-Induced Necrosis.
Authors: John Et al.
ACS Chem Biol 2020;15:1212-1221
Selective modulation of tonically active GABA_A 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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