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

365250
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
136194-77-9C₂₄H₁₈N₄O

Products

Catalogue NumberPackaging Qty/Pack
365250-1MGCN Plastic ampoule 1 mg
365250-500UGCN Plastic ampoule 500 μg
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
Catalogue Number GTIN
365250-1MGCN 04055977192018
365250-500UGCN 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.

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.