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

557520
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      Overview

      Key Spec Table

      Empirical FormulaCAS #
      C₂₅H₂₃N₅O₂S · CH₄O₃S138489-18-6

      Pricing & Availability

      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      557520-500UG
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      There is a newer version of this product
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          500 μg
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          Description
          Overview 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.
          Catalogue Number 557520
          Brand Family Calbiochem®
          Synonyms 3-[1-[3-(Amidinothio)propyl-1H-indol-3-yl]-3-(1-methyl-1H-indol-3-yl)maleimide, Bisindolylmaleimide IX, Methanesulfonate
          References
          References 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.
          Product Information
          CAS number 138489-18-6
          ATP Competitive Y
          Form Red solid
          Hill Formula C₂₅H₂₃N₅O₂S · CH₄O₃S
          Chemical formula C₂₅H₂₃N₅O₂S · CH₄O₃S
          Molar Mass 553.7
          Hygroscopic Hygroscopic
          Reversible Y
          Structure formula Image
          Applications
          Application 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).
          Biological Information
          Primary Target PKC
          Primary Target IC<sub>50</sub> 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)
          Purity ≥95% by HPLC
          Physicochemical Information
          Cell permeable Y
          Solubility DMSO or H₂O
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Ambient Temperature Only
          Toxicity Standard Handling
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Hygroscopic Hygroscopic
          Special Instructions Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 4 months at -20°C.
          Packaging Information
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          MSDS

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          Certificates of Analysis

          TitleLot Number
          557520

          Citations

          Title
        • 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,.
        • Data Sheet

          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.

          Revision 11-January-2010 RFH
          Synonyms 3-[1-[3-(Amidinothio)propyl-1H-indol-3-yl]-3-(1-methyl-1H-indol-3-yl)maleimide, Bisindolylmaleimide IX, Methanesulfonate
          Description 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.
          Form Red solid
          CAS number 138489-18-6
          Molar mass 553.7
          Chemical formula C₂₅H₂₃N₅O₂S · CH₄O₃S
          Structure formula
          Purity ≥95% by HPLC
          Solubility DMSO (100 mg/ml) or H₂O (1 mg/ml)
          Storage +2°C to +8°C
          Protect from light
          Hygroscopic
          Special Instructions Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 4 months at -20°C.
          Toxicity Standard Handling
          References 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.
          Citation
        • 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,.