p38 MAP Kinase Inhibitor X, BIRB 796 – CAS 285983-48-4 – Calbiochem

Descrição detalhada : A cell-permeable pyrazolo-napthalenyl urea compound that acts as a highly potent, slowly binding (IC50 = 8 and 97 nM, respectively, against human p38alpha, respectively, with or without 2 h preincubation), but high affinity (t1/2 of dissociation from human p38alpha = 23 h), p38-selective inhibitor by simultaneously targeting the ATP-binding site and an adjacent DFG-out conformation-specific allosteric cavity. It inhibits JNK2alpha2 and c-Raf-1 only at much higher concentrations (IC50 = 98 nM and 1.4 µM, respectively) and displays little or no activity toward 10 other kinases (IC50 >20 µM). Shown to inhibit LPS-induced TNF-alpha production in cultures in vitro (IC50 = 18 and 780 nM using THP-1 cells and in human whole blood, respectively) and in mice in vivo (by 84% and 63%, respectively, with oral dosage of 30 mg/kg and 10 mg/kg)., A cell-permeable pyrazolo-napthalenyl urea compound that acts as a highly potent, slowly binding (IC50 = 8 and 97 nM, respectively, against human p38alpha, respectively, with or without 2 h preincubation), but high affinity (t1/2 of dissociation from human p38alpha = 23 h), p38-selective inhibitor by simultaneously targeting the ATP-binding site and an adjacent DFG-out conformation-specific allosteric cavity. It inhibits JNK2alpha2 and c-Raf-1 only at much higher concentrations (IC50 = 98 nM and 1.4 µM, respectively) and displays little or no activity toward 10 other kinases (IC50 >20 µM). Shown to inhibit LPS-induced TNF-alpha production both in vitro (IC50 = 18 and 780 nM using THP-1 cells and in human whole blood, respectively) and in mice in vivo (by 84%; 30 mg/kg p.o.).
Sinónimos : p38 MAP Kinase Inhibitor X, BIRB 796 - CAS 285983-48-4 - Calbiochem; Doramapimod, BIRB796, 1-(5- tert-Butyl-2- p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naphthalen-1-yl]urea, JNK Inhibitor XVII; Doramapimod, BIRB796, 1-(5-tert-Butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naphthalen-1-yl]urea, JNK Inhibitor XVII
Fórmula molecula r: C31H37N5O3
Armazenamento : 2-8C; 2-8C; 2-8C
Embalagem : 1X10MG