Cat No.
CEI-0169
Description
BIRB 796 (Doramapimod) can inhibit p38-alpha MAPK with IC50 of 0.1 nM.
CAS No.
285983-48-4
Targets
p38-alpha MAPK
Chemical Name
1-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)-3-(4-(2-morpholinoethoxy)naphthalen-1-yl)urea
M.Wt
527.66
Purity
>99%
Solubility
DMSO 106 mg/mL Water
Storage
2 years at -20centigrade Powder
In vitro
BIRB 796, a member of the N-pyrazole-N-naphthly urea class of p38MAPK inhibitors, binds to the kinase with both slow association and dissociation rates. Prior to binding, the kinase undergoes a reorganization of the activation loop exposing a critical binding domain. We demonstrate that, independent of the loop movement, association rates are governed by low energy conformations of the inhibitor and polar functionality on the tolyl ring. As anticipated, the dissociation rates of the inhibitors from the kinase are slowed by lipophilic and hydrogen bond interactions.
