R&D Systems Inc. Tocris Bioscience Boston Biochem

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.

Resources

Other Information

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
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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-indeced NB4 cells. Mol.Biol.Cell. 22 1167. PMID: 21346199.

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

View Related Products by Target

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

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