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Bisindolylmaleimide I (GF 109203X) (CAS 133052-90-1)

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Solicitud:A highly selective inhibitor of all PKC isoforms and slight inhibitor of GSK-3
Número CAS:133052-90-1
Pureza:98%
Peso Molecular:412.5
Fórmula Molecular:C25H24N4O2
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Bisindolylmaleimide I (GF 109203X) sc-24003 10 mg $159
Bisindolylmaleimide I (GF 109203X) sc-24003A 1 mg $75
Descripción
Bisindolylmaleimide I (GF 109203X) is a staurosporine (sc-3510) inspired molecule, which has been shown to display equally potent inhibition, but with vastly superior selectivity for all of the known isoforms of PKC (IC50 = 8-20 nM). Inhibition is competitive with respect to ATP, which suggests that Bisindolylmaleimide I occupies the ATP binding domain of the PKC isoforms. Bisindolylmaleimide I (GF 109203X) has been used to selectively probe for PKC-mediated pathways for transduction of hormone, cytokine, and growth factor signals. Inhibits PKC within intact platelets and T cells, Fas-mediated apoptosis, and T cell-mediated autoimmune diseases. Also shown to inhibit GSK-3. See sc-24004 for water soluble form of Bisindolylmaleimide I.
Información Técnica
Apariencia:Red to orange
Estado Físico:Solid
Solubilidad:Soluble in DMSO (~1 mg/ml), DMF (10 mg/ml; warm to 40°C & vortex well), and 1:10 DMSO:PBS (pH 7.2) (~0.1 mg/ml). Insoluble in water.
Almacenamiento:Store at -20° C
Punto de Ebullición:685.64 °C at 760 mmHg (Predicted)
Densidad:1.31 g/cm3 (Predicted)
Índice de Refracción:n20D 1.69 (Predicted)
IC50:GSK-3: IC50 = 360 nM; GSK-3β: IC50 = 170 nM; Phosphorylase Kinase: IC50 = 700 nM; cAMP-Dependent Protein Kinase: IC50 = 2000 nM; Protein kinase C α isoforms: IC50 = 8.4 nM; Protein kinase C β1 isoforms: IC50 = 18 nM; Protein kinase C δ isoforms: IC50 = 210 nM; Protein kinase C ε isoforms: IC50 = 132 nM; Protein kinase C ζ isoforms: IC50 = 5.8 µM; MLCK: IC50 = 0.6 µM; PKG: IC50 = 4.6 µM; PKA: IC50 = 33 µM
Ki Data:PKA: Ki= 2 mM; 5-HT3 receptor: Ki= 29.5 nM; PKC: Ki= 14 nM
Seguridad e Información de Referencia
WGK Alemania:3
ID en PubChem:2396
Número MDL:MFCD00236428
SMILES:CN(C)CCCN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
References
1. Toullec, D., et al. 1991. J. Biol. Chem. 266: 15771-15781. PMID: 1874734
2. Martiny-Baron, G., et al. 1993. J. Biol. Chem. 268: 9194-9197. PMID: 8486620
3. Kiss, Z., et al. 1995. Biochim. Biophys. Acta. 1265: 93-95. PMID: 7857990
4. Zhou, T., et al. 1999. Nat. Med. 5: 42-48. PMID: 9883838
Bisindolylmaleimide I (GF 109203X) (CAS 133052-90-1) Menciones del Producto
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