GF 109203X (Bisindolylmaleimide i) (ab144264)

Overview

  • Product name
    GF 109203X (Bisindolylmaleimide i)
  • Description
    Potent, selective PKC inhibitor. Potent GSK-3 inhibitor. Potent 5-HT3 antagonist.
  • Alternative names
    • Bisindolylmaleimide I
  • Biological description
    Potent, selective PKC inhibitor (IC50 values are 0.0084, 0.0180, 0.210, 0.132, and 5.8 μM for α, β1, δ, ε and ζ isoforms respectively). Potent GSK-3 inhibitor (IC50 = 360 nM). Potent 5-HT3 antagonist (Ki = 29.5 nM). Shows anti-inflammatory effects in vivo.
  • Purity
    > 98%

Properties

Images

  • 1.5 x 10e7 THP-1 cells were incubated with 100 nM GF 109203X (ab144264) or Ro 31-8220 mesylate (ab120374) for 30 minutes prior to activation with 10 µg x mL-1 PMA (Sigma) for 4 hours. Control cells were left without inhibitors or PMA. Cells were lysed in 1 mL of lysis buffer, and 30 µL were tested for PKC activity (duplicates; +/- SD).

References

This product has been referenced in:
  • Tsao HK  et al. PKC-dependent ERK phosphorylation is essential for P2X7 receptor-mediated neuronal differentiation of neural progenitor cells. Cell Death Dis 4:e751 (2013). Read more (PubMed: 23907465) »
  • Hers I  et al. The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity. FEBS Lett 460:433-6 (1999). Read more (PubMed: 10556511) »
  • Toullec D  et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem 266:15771-81 (1991). Read more (PubMed: 1874734) »

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