0741

Material Data Sheet

GF 109203X

Price: $185.00
Catalog #: 0741

GF 109203X

Price: 
$75 $159
Quantity: 
1 mg10 mg
Data Sheet: 

Product Information

MW: 
412.49
Purity: 
>98%
Solubility: 
Soluble to 25 mM in DMSO
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-HT3receptor (Ki = 29.5 nM). Anti-inflammatory in vivoAlso available as part of the Mixed Kinase Inhibitor Tocriset™.

Storage: 
Store at RT

Literature

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.