p38 MAP Kinase Inhibitor X, BIRB 796 (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)

Blue Ice

527, 7

Supplied as a white solid.

A cell-permeable pyrazolo-napthalenyl urea compound that acts as a highly potent, slowly binding (IC50=8 and 97nM, respectively, against human p38a, respectively, with or without 2h preincubation), but high affinity (t1/2 of dissociation from human p38a=23h), p38-selective inhibitor by simultaneously targeting the ATP-binding site and an adjacent DFG-out conformation-specific allosteric cavity. It inhibits JNK2a2 and c-Raf-1 only at much higher concentrations (IC50=98nM and 1.4uM, respectively) and displays little or no activity toward 10 other kinases (IC50>20uM). Shown to inhibit LPS-induced TNF-a production both in vitro (IC50=18 and 780nM using THP-1 cells and in human whole blood, respectively) and in mice in vivo (by 84%; 30mg/kg p.o.).

Synonyms: 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

CAS No:
285983-48-4

Molecular Formula:
C₃₁H₃₇N₅O₃

Molecular Weight:
527.7

Solubility:
DMSO

Appearance:
White solid.

Purity:
≥97% (HPLC)

Storage and Stability:
May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.