Product overview

Name Bisindolylmaleimide II
Description Potent PKC inhibitor
Biological description Potent protein kinase C (PKC) inhibitor (IC50 = 0.10 µM). Displays less activity at protein kinase A (PKA) and pyruvate kinase (PK) (IC50 values are 2.0 and 0.70 µM respectively).Also β1.3 subunit of Kv 1.5 channel inhibitor (IC50 = 12.4 µM) and non-competitive nicotonic cholinergic receptor antagonist (approx IC50 = 0.031 µM).
Purity >97%
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Solubility & Handling

Storage instructions -20°C
Solubility overview Soluble in DMSO (100mM)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

Calculators

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Chemical Data

Chemical name 3-(1H-Indol-3-yl)-4-[1-[2-(1-methyl -2-pyrrolidinyl)ethyl]-1H-indol-3-yl]-1H-pyrrole-2 ,5-dione
Molecular Weight 438.52
Chemical structure Product image
Molecular Formula C27H26N4O2
CAS Number 137592-45-1
PubChem identifier 2397
SMILES CN1CCCC1CCN2C=C(C3=CC=CC=C32)C4=C(C(=O)NC4=O)C5=CNC6=CC=CC=C65
InChiKey LBFDERUQORUFIN-UHFFFAOYSA-N

References for Bisindolylmaleimide II

References are publications that support the biological activity of the product
  • PKC inhibition results in a K<sub>v</sub> 1.5 + K<sub>v</sub> β1.3 pharmacology closer to K<sub>v</sub> 1.5 channels.

    Macías A et al (2014) Br J Pharmacol :
  • Chromaffin cell catecholamine secretion: bisindolylmaleimide compounds exhibit novel and potent antagonist effects at the nicotinic cholinergic receptor in pheochromocytoma cells.

    Mahata M et al (2002) Mol Pharmacol 61(6) : 1340-7.
  • The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.

    Toullec D et al (1991) J Biol Chem 266(24) : 15771-81.