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p38 MAP Kinase Inhibitor X, BIRB 796
JNK Inhibitor XVII, 1-(5-tert-Butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naphthalen-1-yl]urea, Doramapimod, BIRB796
A cell-permeable pyrazolo-napthalenyl urea compound that acts as a highly potent, slowly binding (IC50 = 8 and 97 nM, respectively, against human p38α, respectively, with or without 2 h preincubation), but high affinity (t1/2 of dissociation from human p38α = 23 h), p38-selective inhibitor by simultaneously targeting the ATP-binding site and an adjacent DFG-out conformation-specific allosteric cavity. It inhibits JNK2α2 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-α 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.).
产品信息
Form White solid
Molar mass 527.7
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥99% by HPLC
Solubility DMSO
Chemical formula C31H37N5O3
CAS number 285983-48-4
商店和运输信息
Storage +2°C to +8°C
Ship Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Regulatory Review |