Bisindolylmaleimide XI hydrochloride, PKC inhibitor (ab143783)

Overview

  • Product name

    Bisindolylmaleimide XI hydrochloride, PKC inhibitor
  • Description

    Potent, selective, cell-permeable protein kinase C (PKC) inhibitor
  • Alternative names

    • BIM XI
    • Ro 32-0432
  • Biological description

    Selective, cell-permeable protein kinase C (PKC) inhibitor that displays 10-fold greater selectivity for PKCα (IC50 = 9 nM) and 4-fold greater selectivity for PKCβI (IC50 = 28 nM) over Ca2+-independent PKCε (IC50 = 108 nM). Enhances cardiac contractility and protection from heart failure. Prevents T-cell activation and proliferation (IC50s ranging from 30-150 nM) associated with chronic inflammatory responses in vivo. Also inhibits GRK2, GRK5, and GRK6 (IC50 values are 29, 3.6, and 16 µM, respectively).

  • Purity

    > 98%
  • CAS Number

    145333-02-4
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    3-[8-[(Dimethylamino)methyl]-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl]-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione hydrochloride
  • Molecular weight

    489.01
  • Molecular formula

    C28H28N4O2.HCl
  • PubChem identifier

    11605551
  • Storage instructions

    Shipped at Room Temperature. Store at -20°C. Store under desiccating conditions.
  • Solubility overview

    Soluble in DMSO to 10 mM (with warming)
  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=C5CC(CCN5C6=CC=CC=C64)CN(C)C.Cl
  • Source

    Synthetic

References

This product has been referenced in:

  • Liu Q  et al. Protein kinase C{alpha}, but not PKC{beta} or PKC{gamma}, regulates contractility and heart failure susceptibility: implications for ruboxistaurin as a novel therapeutic approach. Circ Res 105:194-200 (2009). Read more (PubMed: 19556521) »
  • Aiyar N  et al. Involvement of G protein-coupled receptor kinase-6 in desensitization of CGRP receptors. Eur J Pharmacol 403:1-7 (2000). Read more (PubMed: 10969137) »
  • Goekjian PG & Jirousek MR Protein kinase C in the treatment of disease: signal transduction pathways, inhibitors, and agents in development. Curr Med Chem 6:877-903 (1999). Read more (PubMed: 10495357) »
  • Birchall AM  et al. Ro 32-0432, a selective and orally active inhibitor of protein kinase C prevents T-cell activation. J Pharmacol Exp Ther 268:922-9 (1994). Read more (PubMed: 8114006) »
  • Wilkinson SE  et al. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J 294 ( Pt 2):335-7 (1993). Read more (PubMed: 8373348) »

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