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).

• Sinónimos: 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
• Fórmula empírica (notación de Hill): C₂₄H₁₈N₄O
• Número de CAS: 136194-77-9
• Peso molecular: 378.43
• Número MDL: MFCD00236434
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Ensayo: ≥95% (HPLC)
• Formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: off-white
• solubilidad: DMSO: 5 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: 2-8°C
• cadena SMILES: [n]1(c2c3[n](c4c(c3c5c(c2c6c1cccc6)CNC5=O)cccc4)C)CCC#N
• 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)
• Clave InChI: VWVYILCFSYNJHF-UHFFFAOYSA-N

Descripción

Descripción general

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.

Acciones bioquímicas o fisiológicas

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

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

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

Otras notas

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.

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable