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

557520
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₅H₂₃N₅O₂S · CH₄O₃S 138489-18-6

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      557520-500UG
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          Plastic ampoule 500 μg
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          Description
          OverviewA 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 Number557520
          Brand Family Calbiochem®
          Synonyms3-[1-[3-(Amidinothio)propyl-1H-indol-3-yl]-3-(1-methyl-1H-indol-3-yl)maleimide, Bisindolylmaleimide IX, Methanesulfonate
          References
          ReferencesTrapp, 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 number138489-18-6
          ATP CompetitiveY
          FormRed solid
          Hill FormulaC₂₅H₂₃N₅O₂S · CH₄O₃S
          Chemical formulaC₂₅H₂₃N₅O₂S · CH₄O₃S
          Hygroscopic Hygroscopic
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetPKC
          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 permeableY
          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
          Do not freeze Ok to freeze
          Special InstructionsFollowing 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

          Ro-31-8220 - CAS 138489-18-6 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          Ro-31-8220 - CAS 138489-18-6 - Calbiochem Certificates of Analysis

          TitleLot Number
          557520

          References

          Reference overview
          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.

          Brochure

          Title
          PKC Pathway Poster PDF ( 676 KB )

          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.

          Revision11-January-2010 RFH
          Synonyms3-[1-[3-(Amidinothio)propyl-1H-indol-3-yl]-3-(1-methyl-1H-indol-3-yl)maleimide, Bisindolylmaleimide IX, Methanesulfonate
          DescriptionA 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.
          FormRed solid
          CAS number138489-18-6
          Chemical formulaC₂₅H₂₃N₅O₂S · CH₄O₃S
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (100 mg/ml) or H₂O (1 mg/ml)
          Storage +2°C to +8°C
          Hygroscopic
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 4 months at -20°C.
          Toxicity Standard Handling
          ReferencesTrapp, 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,.