GF 109203X

Cat. No. 0741

GF 109203X C25H24N4O2 [133052-90-1]

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Alternative Names: Gö 6850, Bisindolylmaleimide I

Chemical Name: 2-[1-(3-Dimethylaminopropyl)indol-3-yl]-3-(indol-3-yl) maleimide

Biological Activity

Very potent and selective inhibitor of protein kinase C, selective for the α and β1 isoforms (IC50 values are 0.0084, 0.0180, 0.210, 0.132, and 5.8 μM for α, β1, δ, ε and ζ isoforms respectively). Selective over MLCK, PKG and PKA (IC50 values are 0.6, 4.6, and 33 μM respectively). Potent antagonist at the 5-HT3 receptor (Ki = 29.5 nM). Anti-inflammatory in vivo.

Technical Data

M.Wt:
412.49
Formula:
C25H24N4O2
Solubility:
Soluble to 25 mM in DMSO
Purity:
>98 %
Storage:
Store at RT
CAS No:
133052-90-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

Toullec et al (1991) The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J.Biol.Chem. 266 15771. PMID: 1874734.

Martiny-Baron et al (1993) Selective inhibition of protein kinase C isozymes by the indolocarbazole Go 6976. J.Biol.Chem. 268 9194. PMID: 8486620.

Jacobson et al (1995) Anti-inflammatory properties of Go 6850: a selective inhibitor of protein kinase C. J.Pharmacol.Exp.Ther. 275 995. PMID: 7473193.

Coultrap et al (1999) Competitive antagonism of the mouse 5-hydroxytryptamine3 receptor by bisindolylmaleimide I, a "selective" protein kinase C inhibitor. J.Pharmacol.Exp.Ther. 290 76. PMID: 10381762.

Jiang et al (2011) Heat shock protein 90-mediated inactivation of nuclear factor-κB switches autophagy to apoptosis through becn1 transcriptional inhibition in selenite-induced NB4 cells. Mol.Biol.Cell. 22 1167. PMID: 21346199.

If you know of a relevant citation for this product please let us know.

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Keywords: GF 109203X, supplier, Protein, kinase, C, inhibitors, PKC, PKM, Kinase, Kinases, alpha, beta, α, β, GF109203X, Go6850, Go, 6850, Tocris Bioscience, Protein Kinase C Inhibitors

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