BIRB 796

Biological Activity

BIRB 796 is a high affinity and selective p38 kinase inhibitor (K_d = 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). BIRB 796 can be used in protocols for the chemical reprogramming of somatic cells to iPSCs. Cell permeable.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. 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.
   J.Med.Chem., 2008;51:4122
2. 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.
   J.Med.Chem., 2003;46:4676
3. Selective p38α inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
   Goldstein et al.
   J.Med.Chem., 2010;53:2345

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