BIRB 796

Biological Activity
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). Cell permeable.

• M.Wt:
  527.66
• Formula:
  C₃₁H₃₇N₅O₃
• Solubility:
  Soluble to 100 mM in DMSO and to 50 mM in ethanol
• Purity:
  >99%
• Storage:
  Store at -20°C
• CAS No:
  285983-48-4

1. BIRB796 inhibits all p38 MAPK isoforms in vitro and in vivo.
   Kuma et al.
   J.Biol.Chem., 2005;280:19472
2. 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
3. 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
4. Selective p38α inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
   Goldstein et al.
   J.Med.Chem., 2010;53:2345