557520 | Ro-31-8220 - CAS 138489-18-6 - Calbiochem

557520
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      Overview

      Replacement Information

      Tabla espec. clave

      Fórmula empírica Nº CAS
      C₂₅H₂₃N₅O₂S · CH₄O₃S138489-18-6

      Precios y disponibilidad

      Número de referenciaDisponiblidad Embalaje Cant./Env. Precio Cantidad
      557520-500UG
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      Disponibilidad a confirmar Disponibilidad a confirmar
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      Debe confirmarse disponibilidad
        Remaining : Will advise
          Se avisará

          500 μg
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          Descripción
          Visión de conjunto A cell-permeable, reversible, competitive, and selective inhibitor of protein kinase C (PKC; IC50 = 10 nM) over CaM kinase II (IC50 = 17 µM) and protein kinase A (IC50 = 900 nM). Potently inhibits GSK-3 in primary adipocytes (IC50 = 6.8 nM) and in GSK-3β immunoprecipitates (IC50 = 2.8 nM). An inhibitor of MAP kinase phosphatase-1 expression and an activator of JNK1. Inhibits the phosphorylation of Raf-1 and induces apoptosis, independent of its effects on PKC, in HL-60 cells. Also inhibits sirtuin in a NAD-competitive manner (IC50 = 3.5 µM and 0.8 µM for SIRT1 and SIRT2, respectively), and induces hyperacetylation of tubulin in A549 cells. A 5 mM (500 µg/181 µl) solution of Ro-31-8220 (Cat. No. 557521) in H2O is also available.
          Número de catálogo 557520
          Marca de familia Calbiochem®
          Sinónimos 3-[1-[3-(Amidinothio)propyl-1H-indol-3-yl]-3-(1-methyl-1H-indol-3-yl)maleimide, Bisindolylmaleimide IX, Methanesulfonate
          Referencias bibliográficas
          Referencias bibliográficas Trapp, J., et al. 2006. J. Med. Chem. In press.
          Powell, D.J., et al. 2003. Mol. Cell Biol. 23, 7794.
          Han, Z., et al. 2000. Cell Death Differ. 7, 521.
          Hers, I., et al. 1999. FEBS Lett. 460, 433.
          Beltman, J., et al. 1996. J. Biol. Chem. 271, 27018.
          Keller, H.U., and Niggli, V. 1993. Biochem. Biophys. Res. Commun. 194, 1111.
          McKenna, J.P., and Hanson, P.J. 1993. Biochem. Pharmacol. 46, 583.
          Davis, P.D., et al. 1992. J. Med. Chem. 35, 994.
          Información del producto
          Número de CAS 138489-18-6
          ATP Competitivo Y
          Formulario Red solid
          Fórmula Hill C₂₅H₂₃N₅O₂S · CH₄O₃S
          Fórmula química C₂₅H₂₃N₅O₂S · CH₄O₃S
          Molar Mass 553.7
          Higroscópico Hygroscopic
          Reversible Y
          Imagen fórmula estructural
          Aplicaciones
          Información biológica
          Objetivo principal PKC
          Objetivo principal IC50 10 nM, 17 µM, 900 nM against PKC, CaM kinase II, and protein kinase A, respectively; 6.8 nM against GSK-3 in primary adipocytes; 2.8 nM against GSK-3β immunoprecipitates)
          Pureza ≥95% by HPLC
          Información fisicoquímica
          Permeabilidad celular Y
          Solubilidad DMSO or H₂O
          Dimensiones
          Información de materiales
          Información toxicológica
          Información de seguridad según el GHS
          Información de seguridad
          Declaraciones de uso del producto
          Información de almacenamiento y transporte
          Código de envío Ambient Temperature Only
          Toxicidad Standard Handling
          Almacenamiento +2°C to +8°C
          Proteger de la luz Protect from light
          Higroscópico Hygroscopic
          No congelar No
          Instrucciones especiales Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 4 months at -20°C.
          Información sobre embalaje
          Información de transporte
          Información complementaria
          Especificaciones

          Documentation

          Ficha datos de seguridad (MSDS)

          Idiomas
          Australia Canadian English Canadian-French
          Colombia Danmark Deutschland
          Ellas English España
          France Italia Korea
          Magyarország Nederland  Norge
          Polska Portugal Suomi
          Sverige US Español Österreich
          България

          Certificados de análisis

          CargoNúmero de lote
          557520

          Referencias bibliográficas

          Visión general referencias
          Trapp, J., et al. 2006. J. Med. Chem. In press.
          Powell, D.J., et al. 2003. Mol. Cell Biol. 23, 7794.
          Han, Z., et al. 2000. Cell Death Differ. 7, 521.
          Hers, I., et al. 1999. FEBS Lett. 460, 433.
          Beltman, J., et al. 1996. J. Biol. Chem. 271, 27018.
          Keller, H.U., and Niggli, V. 1993. Biochem. Biophys. Res. Commun. 194, 1111.
          McKenna, J.P., and Hanson, P.J. 1993. Biochem. Pharmacol. 46, 583.
          Davis, P.D., et al. 1992. J. Med. Chem. 35, 994.

          Citas

          Título
        • Farahdiba Jafri, et al. (2006) Constitutive ERK1/2 activation by a chimeric neurokinin NK1 receptor-beta-arrestin1 fusion protein: Probing the composition and function of the G protein-coupled receptor 'signalsome'. Journal of Biological Chemistry in press,.
        • Ficha técnica

          Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

          Revisión 11-January-2010 RFH
          Sinónimos 3-[1-[3-(Amidinothio)propyl-1H-indol-3-yl]-3-(1-methyl-1H-indol-3-yl)maleimide, Bisindolylmaleimide IX, Methanesulfonate
          Descripción A cell-permeable, competitive, reversible, and selective inhibitor of protein kinase C (PKC; IC50 = 10 nM) over CaM kinase II (IC50 = 17 µM) and protein kinase A (IC50 = 900 nM). Potently inhibits GSK-3 in primary adipocytes (IC50 = 6.8 nM) and in GSK-3β immunoprecipitates (IC50 2.8 nM). An inhibitor of MAP kinase phosphatase-1 expression and an activator of JNK1. Inhibits the phosphorylation of Raf-1 and induces apoptosis, independent of its effects on PKC, in HL-60 cells. Also inhibits sirtuin in a NAD-competitive manner (IC50 = 3.5 µM and 0.8 µM for SIRT1 and SIRT2, respectively), and induces hyperacetylation of tubulin in A549 cells.
          Formulario Red solid
          Número de CAS 138489-18-6
          Masa molar 553.7
          Fórmula química C₂₅H₂₃N₅O₂S · CH₄O₃S
          Fórmula estructural
          Pureza ≥95% by HPLC
          Solubilidad DMSO (100 mg/ml) or H₂O (1 mg/ml)
          Almacenamiento +2°C to +8°C
          Protect from light
          Hygroscopic
          Do Not Freeze No
          Special Instructions Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 4 months at -20°C.
          Toxicidad Standard Handling
          Referencias bibliográficas Trapp, J., et al. 2006. J. Med. Chem. In press.
          Powell, D.J., et al. 2003. Mol. Cell Biol. 23, 7794.
          Han, Z., et al. 2000. Cell Death Differ. 7, 521.
          Hers, I., et al. 1999. FEBS Lett. 460, 433.
          Beltman, J., et al. 1996. J. Biol. Chem. 271, 27018.
          Keller, H.U., and Niggli, V. 1993. Biochem. Biophys. Res. Commun. 194, 1111.
          McKenna, J.P., and Hanson, P.J. 1993. Biochem. Pharmacol. 46, 583.
          Davis, P.D., et al. 1992. J. Med. Chem. 35, 994.
          Cita
        • Farahdiba Jafri, et al. (2006) Constitutive ERK1/2 activation by a chimeric neurokinin NK1 receptor-beta-arrestin1 fusion protein: Probing the composition and function of the G protein-coupled receptor 'signalsome'. Journal of Biological Chemistry in press,.