Cat. No. 4279
Chemical Name: (10R)-9,10,11,12-Tetrahydro-10-methyl-3-(6-methyl-3-pyridinyl)-8H-[1,4]diazepino[5',6':4,5]thieno[3,2-f]quinolin-8-one
Biological ActivityPotent, ATP-competitive inhibitor of mitogen-activated protein kinase (MAPK)-activated protein kinase-2 (MK2) (IC50 = 5.2 nM; Ki = 3 nM). Inhibits tumor necrosis factor α (TNFα) production in U937 monocytic cells and peripheral blood mononuclear cells (PBMCs) (IC50 = 160 nM); exhibits oral efficacy in acute and chronic inflammatory models.
Licensing InformationSold for research purposes under agreement from Pfizer Inc.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
Mourey et al (2010) A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor α production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation. J.Pharmacol.Exp.Ther. 333 797. PMID: 20237073.
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Keywords: PF 3644022, supplier, PF3644022, mapk, mitogen-activated, protein, kinase-activated, protein, kinase, 2, MK-2, MK2, potent, anti-inflammatory, inhibitors, inhibits, pfizer
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