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

Gö 6976, CAS 136194-77-9, is a cell-permeable, reversible, and ATP-competitive inhibitor of PKC (IC₅₀ = 7.9 nM for rat brain). Exhibits selectively for PKCα (IC₅₀ = 2.3 nM) and βI (IC₅₀ = 6.2 nM).

Gö 6976 - CAS 136194-77-9 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Go 6976, 12-(2-Cyanoethyl)-6,7,12,13-tetrahydro-13-methyl-5-oxo-5H-indolo(2,3-a)pyrrolo(3,4-c)-carbazole

Primary Target: PKC
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
136194-77-9C₂₄H₁₈N₄O

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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
          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
          Global Trade Item Number
          Catalog Number GTIN
          365250-1MG 04055977192018
          365250-500UG 07790788049614

          Documentation

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

          Title

          Safety Data Sheet (SDS) 

          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.

          Brochure

          Title
          PKC Pathway Poster PDF ( 676 KB )

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