365250 Gö 6976 - CAS 136194-77-9 - Calbiochem

365250
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Key Spec Table

Empirical FormulaCAS #
C₂₄H₁₈N₄O136194-77-9

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365250-1MGCN
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      Plastic ampoule 1 mg
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      Description
      OverviewA cell-permeable, reversible, and ATP-competitive inhibitor of protein kinase C (PKC; IC50 = 7.9 nM for rat brain). Selectively inhibits Ca2+-dependent PKC α-isozyme (IC50 = 2.3 nM) and PKCβI (IC50 = 6.2 nM). Does not affect the kinase activity of the Ca2+-independent PKC δ-, ε-, and ζ-isozymes even at micromolar levels. Reported to inhibit PKCµ at higher concentrations (IC50 = 20 nM). A 500 µg/ml solution of Gö 6976 (Cat. No. 365253) in anhydrous DMSO is also available.
      Catalogue Number365250
      Brand Family Calbiochem®
      SynonymsGo 6976, 12-(2-Cyanoethyl)-6,7,12,13-tetrahydro-13-methyl-5-oxo-5H-indolo(2,3-a)pyrrolo(3,4-c)-carbazole
      References
      ReferencesGschwendt, M., et al. 1996. FEBS Lett. 392, 77.
      Wenzel-Seifert, K., et al. 1994. Biochem. Biophys. Res. Commun. 200, 1536.
      Martiny-Baron, G.M., et al. 1993. J. Biol. Chem. 268, 9194.
      Qatsha, K.A., et al. 1993. Proc. Natl. Acad. Sci. USA 90, 4674.
      Product Information
      CAS number136194-77-9
      ATP CompetitiveY
      FormOff-white solid
      Hill FormulaC₂₄H₁₈N₄O
      Chemical formulaC₂₄H₁₈N₄O
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetPKC
      Primary Target IC<sub>50</sub>7.9 nM against rat brain PKC; 2.3 nM, 6.2 nM against Ca2+-dependent PKC α-isozyme and PKCβI, respectively
      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
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 4 months at -20°C.
      Packaging Information
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Gö 6976 - CAS 136194-77-9 - Calbiochem Certificates of Analysis

      TitleLot Number
      365250

      References

      Reference overview
      Gschwendt, M., et al. 1996. FEBS Lett. 392, 77.
      Wenzel-Seifert, K., et al. 1994. Biochem. Biophys. Res. Commun. 200, 1536.
      Martiny-Baron, G.M., et al. 1993. J. Biol. Chem. 268, 9194.
      Qatsha, K.A., et al. 1993. Proc. Natl. Acad. Sci. USA 90, 4674.

      Citations

      Title
    • Elizabeth A. Johnson, et al. (2006) Agonist-selective mechanisms of µ-opioid receptor desensitization in human embryonic kidney 293 cells. Molecular Pharmacology 70, 676-685.
    • Ying Zhang, Mingjuan Liao and Maria L. Dufau. (2006) Phosphatidylinositol 3-kinase/protein kinase Cγ-induced phosphorylation of Sp1 and p107 repressor release have a critical role in histone deacetylase inhibitor-mediated depression of transcription of the luteinizing hormone receptor gene. Molecular and Cellular Biology 26, 6748-6761.
    • Justin C. Mason, et al. (2004) Decay-accelerating actor induction on vascular endothelium by vascular endothelial growth factor (VEGF) is mediated via a VEGF receptor-2 (VEGF-R2)- and protein kinase C-α/ε (PKCα/ε)-dependent cytoprotective signaling pathway a. Journal of Biological Chemistry 279, 41611-41618.
    • 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.

      Revision08-January-2010 RFH
      SynonymsGo 6976, 12-(2-Cyanoethyl)-6,7,12,13-tetrahydro-13-methyl-5-oxo-5H-indolo(2,3-a)pyrrolo(3,4-c)-carbazole
      DescriptionA cell-permeable, reversible, and ATP-competitive inhibitor of protein kinase C (PKC; IC50 = 7.9 nM for rat brain). Selectively inhibits Ca2+-dependent PKCα-isozyme (IC50 = 2.3 nM) and PKCβI (IC50 = 6.2 nM). Does not affect the kinase activity of the Ca2+-independent PKC δ-, ε-, and ζ-isoenzymes even at micromolar levels. A potent antagonist of HIV-1 induction.
      FormOff-white solid
      CAS number136194-77-9
      Chemical formulaC₂₄H₁₈N₄O
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (5 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 4 months at -20°C.
      Toxicity Standard Handling
      ReferencesGschwendt, M., et al. 1996. FEBS Lett. 392, 77.
      Wenzel-Seifert, K., et al. 1994. Biochem. Biophys. Res. Commun. 200, 1536.
      Martiny-Baron, G.M., et al. 1993. J. Biol. Chem. 268, 9194.
      Qatsha, K.A., et al. 1993. Proc. Natl. Acad. Sci. USA 90, 4674.
      Citation
    • Elizabeth A. Johnson, et al. (2006) Agonist-selective mechanisms of µ-opioid receptor desensitization in human embryonic kidney 293 cells. Molecular Pharmacology 70, 676-685.
    • Ying Zhang, Mingjuan Liao and Maria L. Dufau. (2006) Phosphatidylinositol 3-kinase/protein kinase Cγ-induced phosphorylation of Sp1 and p107 repressor release have a critical role in histone deacetylase inhibitor-mediated depression of transcription of the luteinizing hormone receptor gene. Molecular and Cellular Biology 26, 6748-6761.
    • Justin C. Mason, et al. (2004) Decay-accelerating actor induction on vascular endothelium by vascular endothelial growth factor (VEGF) is mediated via a VEGF receptor-2 (VEGF-R2)- and protein kinase C-α/ε (PKCα/ε)-dependent cytoprotective signaling pathway a. Journal of Biological Chemistry 279, 41611-41618.