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

365250
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₄H₁₈N₄O 136194-77-9

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      365250-1MG
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          Plastic ampoule 1 mg
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          365250-500UG
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              Plastic ampoule 500 μg
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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
              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

              SDS

              Title

              Safety Data Sheet (SDS) 

              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.