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

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).

Ro-31-8220 - CAS 138489-18-6 - Calbiochem: のSDS（安全データシート）、CoA（試験成績書）およびCoQ（品質証明書）、カタログなど製品関連の技術資料を入手いただけます。

同義語: 3-[1-[3-(Amidinothio)propyl-1H-indol-3-yl]-3-(1-methyl-1H-indol-3-yl)maleimide, Bisindolylmaleimide IX, Methanesulfonate

Primary Target: PKC
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557520
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概要

Replacement Information

主要スペック表

CAS #Empirical Formula
138489-18-6C₂₅H₂₃N₅O₂S · CH₄O₃S

価格＆在庫状況

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557520-500UGCN
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      		 樹脂ｱﾝﾌﾟﾙ 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
      Quality LevelMQ100
      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
      Global Trade Item Number
      カタログ番号 GTIN
      557520-500UGCN 07790788051518

      Documentation

      Ro-31-8220 - CAS 138489-18-6 - Calbiochem (M)SDS

      タイトル

      英語版製品安全データシート（(M)SDS） 

      Ro-31-8220 - CAS 138489-18-6 - Calbiochem 試験成績書（CoA）

      タイトルロット番号
      557520

      参考資料

      参考資料の概要
      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.

      Posters

      タイトル
      Human Kinome & InhibitorSelect™ Libraries

      引用

      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,.
      		•
      データシート

      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 Protect from light
      +2°C to +8°C
      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.
      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,.
      		•