Bisindolylmaleimide II

(HB0135)

Product overview

  • Name
    Bisindolylmaleimide II
  • Short 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).
  • Biological action
    Inhibitor
  • Purity
    >97%
  • Citations

Properties

  • 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
    Bisindolylmaleimide II [137592-45-1]
  • 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

Storing and Using Your Product

  • 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.

References for Bisindolylmaleimide II

  • PKC inhibition results in a Kv 1.5 + Kv β1.3 pharmacology closer to Kv 1.5 channels.

    Macías A et al (2014) Br J Pharmacol :
    PubMedID: 24946104
  • 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.
    PubMedID: 12021395
  • 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.
    PubMedID: 1874734

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