Sotrastaurin, pan-PKC inhibitor (ab219867)

Overview

  • Product name
    Sotrastaurin, pan-PKC inhibitor
  • Description
    Potent, selective pan-PKC inhibitor
  • Alternative names
    • 3-(1H-indol-3-yl)-4-(2-(4-methylpiperazin-1-yl)quinazolin-4-yl)-1H-pyrrole-2,5-dione
    • AEB071
    • NVP-AEB071
  • Biological description

    Potent, selective pan-PKC inhibitor (Ki values of 0.95, 0.64, 2.1, 3.2, 1.8, and 0.22 nM  for PKCα, βI, δ, ε, η, and θ respectively in a cell-free assay). Prevents the production of various cytokines by activated T cells, macrophages, and keratinocytes in vitro and has been shown to inhibit an acute allergic contact dermatitis response in rats when dosed orally at 30 mg. Displays potential immunosuppressive activity.

Properties

  • Molecular weight
    438.48
  • Chemical structure
    Chemical Structure
  • Molecular formula
    C25H22N6O2
  • CAS Number
    425637-18-9
  • Storage instructions
    Store at -20°C. Store under desiccating conditions.

References

This product has been referenced in:
  • de Weerd A  et al. The protein kinase C inhibitor sotrastaurin allows regulatory T cell function. Clin Exp Immunol 175:296-304 (2014). Read more (PubMed: 24131367) »
  • Vafadari R  et al. Tacrolimus inhibits NF-?B activation in peripheral human T cells. PLoS One 8:e60784 (2013). Read more (PubMed: 23573283) »
  • Naylor TL  et al. Protein kinase C inhibitor sotrastaurin selectively inhibits the growth of CD79 mutant diffuse large B-cell lymphomas. Cancer Res 71:2643-53 (2011). Read more (PubMed: 21324920) »
  • Weckbecker G  et al. Effects of the novel protein kinase C inhibitor AEB071 (Sotrastaurin) on rat cardiac allograft survival using single agent treatment or combination therapy with cyclosporine, everolimus or FTY720. Transpl Int 23:543-52 (2010). Read more (PubMed: 20003043) »
  • Evenou JP  et al. The potent protein kinase C-selective inhibitor AEB071 (sotrastaurin) represents a new class of immunosuppressive agents affecting early T-cell activation. J Pharmacol Exp Ther 330:792-801 (2009). Read more (PubMed: 19491325) »
  • Skvara H  et al. The PKC inhibitor AEB071 may be a therapeutic option for psoriasis. J Clin Invest : (2008). Read more (PubMed: 18688284) »

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Please note: All products are "FOR RESEARCH USE ONLY AND ARE NOT INTENDED FOR DIAGNOSTIC OR THERAPEUTIC USE, NOT FOR USE IN HUMANS"

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