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经验公式(希尔记法):
C24H18N4O
化学文摘社编号:
分子量:
378.43
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
Gö 6976, InSolution, ≥95%, Inhibitor of protein kinase C
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
liquid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
solubility
DMSO: 5 mg/mL
shipped in
wet ice
storage temp.
−20°C
Quality Level
Biochem/physiol Actions
Target IC50: 7.9 nM, 2.3 nM, and 6.2 nM, for rat brain PKC, Ca2+-dependent PKC α-isozyme, and PKCβI, respectively
Cell permeable: yes
Primary Target
PKC
PKC
Product competes with ATP.
Reversible: yes
Disclaimer
Toxicity: Irritant (B)
General description
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.
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., et al. 1993. J. Biol. Chem.268, 9194.
Qatsha, K.A., et al. 1993. Proc. Natl. Acad. Sci. USA90, 674.
Wenzel-Seifert, K., et al. 1994. Biochem. Biophys. Res. Commun.200, 1536.
Martiny-Baron, G., et al. 1993. J. Biol. Chem.268, 9194.
Qatsha, K.A., et al. 1993. Proc. Natl. Acad. Sci. USA90, 674.
Packaging
Packaged under inert gas
Physical form
A 500 µg/ml solution of Gö 6976 (Cat. No. 365250) in anhydrous DMSO.
Preparation Note
Following initial thaw, aliquot and freeze (-20°C).
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
10 - Combustible liquids
wgk
WGK 1
flash_point_f
188.6 °F - closed cup - (Dimethylsulfoxide)
flash_point_c
87 °C - closed cup - (Dimethylsulfoxide)
An-Angela N Van et al.
The Journal of biological chemistry, 296, 100445-100445 (2021-02-23)
Within the AGC kinase superfamily, gene fusions resulting from chromosomal rearrangements have been most frequently described for protein kinase C (PKC), with gene fragments encoding either the C-terminal catalytic domain or the N-terminal regulatory moiety fused to other genes. Kinase
Li-Mei Chen et al.
Bioscience reports, 41(7) (2021-07-10)
The serine protease prostasin is a negative regulator of lipopolysaccharide-induced inflammation and has a role in the regulation of cellular immunity. Prostasin expression in cancer cells inhibits migration and metastasis, and reduces epithelial-mesenchymal transition. Programmed death-ligand 1 (PD-L1) is a
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