Abstract
Analog 8, a 3-pyridinecarbonitrile with an (E)-2-[6-[(4-methylpiperazin-1-yl)methyl]pyridin-2-yl]vinyl group at C-5, had an IC(50) value of 1.1 nM for the inhibition of PKCtheta and potently blocked the production of IL-2 in both stimulated murine T cells (IC(50)=34 nM) and human whole blood (IC(50)=500 nM).
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MeSH terms
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Animals
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Humans
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Interleukin-2 / biosynthesis
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Isoenzymes / antagonists & inhibitors*
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Mice
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Microsomes, Liver / drug effects
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Microsomes, Liver / enzymology
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Nitriles / chemistry
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Nitriles / pharmacology*
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Protein Kinase C / antagonists & inhibitors*
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Protein Kinase C-theta
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Protein Kinase Inhibitors / chemistry
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Protein Kinase Inhibitors / pharmacology*
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T-Lymphocytes / drug effects
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T-Lymphocytes / metabolism
Substances
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Interleukin-2
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Isoenzymes
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Nitriles
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Protein Kinase Inhibitors
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Prkcq protein, mouse
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Protein Kinase C
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Protein Kinase C-theta