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Key Documents

365250

Sigma-Aldrich

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

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About This Item

Formule empirique (notation de Hill):
C24H18N4O
Numéro CAS:
Poids moléculaire :
378.43
Numéro MDL:
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

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 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 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.
A 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.

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

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


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Learn tips and tricks for how to properly use inhibitors including how to select the right inhibitor and how to plan experiments with inhibitors.

Learn tips and tricks for how to properly use inhibitors including how to select the right inhibitor and how to plan experiments with inhibitors.

Learn tips and tricks for how to properly use inhibitors including how to select the right inhibitor and how to plan experiments with inhibitors.

Learn tips and tricks for how to properly use inhibitors including how to select the right inhibitor and how to plan experiments with inhibitors.

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