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Merck

365250

Gö 6976

≥95% (HPLC), protein kinase C inhibitor, solid

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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A propos de cet article

Formule empirique (notation de Hill) :
C24H18N4O
Numéro CAS:
136194-77-9
Poids moléculaire :
378.43
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD00236434

Principaux documents

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Nom du produit

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).

SMILES string

[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)

InChI key

VWVYILCFSYNJHF-UHFFFAOYSA-N

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

Catégories apparentées

Biochem/physiol Actions

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

Disclaimer

Toxicity: Standard Handling (A)

General description

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.

Other Notes

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.

Preparation Note

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

Legal Information

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

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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