High 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 JNK2α
2 and c-Raf-1 (IC50
values are 98 nM and 1.4 μ
M, respectively). Cell permeable.
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All Tocris products are intended for laboratory research use only.
BIRB796 inhibits all p38 MAPK isoforms in vitro and in vivo.
Kuma et al.
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.
Laufer et al.
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).
Regan et al.
Selective p38α inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
Goldstein et al.