SB 239063

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、口服的 p38 MAPK 抑制剂，对 p38α 和 p38β 的 IC50 均为 44 nM。

A potent, selective, orally available p38 MAPK inhibitor with IC50 of 44 nM for both p38α and p38β; shows no activity (>100 μM) against the γ- and δ-kinase isoforms, and a panel of protein kinase; inhibits IL-1 and TNF-alpha production in LPS-stimulated human PBMCs (IC50= 0.12 and 0.35 uM); reduces inflammatory cytokine production, airways eosinophil infiltration and persistence in vivo.

Apoptosis Analysis Cell Line:Eosinophils (guinea pig BALs) Concentration:0.1μM, 1μM, 10μM Incubation Time:29 hours, 47 hours Result:Increased apoptosis of eosinophils in a dose-related in the presence of 10 pM IL-5 at every time point from 21 hours onwards.

Animal Model:Male BALB/c mice (18–20 g) Dosage:12 mg/kg Administration:Oral administration; 1 h before and 4 h after OA challenge; bis in die for 3 days Result:Significantly inhibited the resultant antigen-induced airway eosinophilia.

SB-239063 | SB239063

MAPK/ERK Signaling

p38 MAPK

p38α|p38β

Inflammation/Immunology

——

193551-21-2

368.4048

C20H21FN4O2

>98% (HPLC)

10 mM in DMSO

O[C@H]1CC[C@H](N2C(C3=NC(OC)=NC=C3)=C(C4=CC=C(F)C=C4)N=C2)CC1

Cyclohexanol, 4-[4-(4-fluorophenyl)-5-(2-methoxy-4-pyrimidinyl)-1H-imidazol-1-yl]-, trans-

(-20℃)

With Ice Pack

≥ 2 years