Cat. No. 5989
Alternative Name: Doramapimod
Chemical Name: N-[3-(1,1-Dimethylethyl)-1-(4-methy
Biological ActivityHigh affinity and selective p38 kinase inhibitor (Kd = 50-100 pM). Exhibits no significant inhibition on a panel of related kinases. Inhibits LPS-induced TNFα production in human PBMCs and whole blood (IC50 values are 21 and 960 nM, respectively). Also inhibits JNK2α2 and c-Raf-1 (IC50 values are 98 nM and 1.4 μM, respectively). Cell permeable.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Goldstein et al (2010) Selective p38α inhibitors clinically evaluated for the treatment of chronic inflammatory disorders. J.Med.Chem. 53 2345. PMID: 19950901.
Laufer et al (2008) Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. J.Med.Chem. 51 4122. PMID: 18578517.
Kuma et al (2005) BIRB796 inhibits all p38 MAPK isoforms in vitro and in vivo. J.Biol.Chem. 280 19472. PMID: 15755732.
Regan et al (2003) Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796). J.Med.Chem. 46 4676. PMID: 14561087.
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