365250

Gö 6976

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).

• Synonyme(s) : Gö 6976, Go 6976, 12-(2-Cyanoethyl)-6,7,12,13-tetrahydro-13-methyl-5-oxo-5H-indolo(2,3-a)pyrrolo(3,4-c)-carbazole
• Formule empirique (notation de Hill): C₂₄H₁₈N₄O
• Numéro CAS: 136194-77-9
• Poids moléculaire : 378.43
• Numéro MDL: MFCD00236434
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: off-white
• Solubilité: DMSO: 5 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• InChI: 1S/C24H18N4O/c1-27-17-9-4-2-7-14(17)20-21-16(13-26-24(21)29)19-15-8-3-5-10-18(15)28(12-6-11-25)23(19)22(20)27/h2-5,7-10H,6,12-13H2,1H3,(H,26,29)
• Clé InChI: VWVYILCFSYNJHF-UHFFFAOYSA-N

Description

Description générale

A 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 PKC_βI (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 PKC_µ at higher concentrations (IC₅₀ = 20 nM). A 500 µg/ml solution of Gö 6976 (Cat. No. 365253) in anhydrous DMSO is also available.

A 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 PKC_βI (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.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
PKC

Product competes with ATP.

Reversible: yes

Target IC₅₀: 7.9 nM against rat brain PKC; 2.3 nM, 6.2 nM against Ca2+-dependent PKC α-isozyme and PKCβI, respectively

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 4 months at -20°C.

Autres remarques

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. USA90, 4674.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable