SB 239063 是一种选择性、可口服的p38 MAPK抑制剂,对重组纯化的人 p38α 的IC50值为 44 nM,具有抗哮喘作用,还被用于增强因衰老或疾病受损的记忆,如阿尔茨海默病。
产品描述
SB239063 is a potent and selective p38 MAPKα/β inhibitor with IC50 of 44 nM, showing no activity against the γ- and δ-kinase isoforms.
体外活性
SB 239063 potently inhibits IL-1 and TNF-α production in LPS-stimulated human peripheral blood monocytes with IC50 of 120 and 350 nM, respectively. [1] In oxygen-glucose-deprived hippocampal slice cultures, SB239063 strikingly reduces the levels of the pro-inflammatory cytokine IL-1beta, causes cell death after oxygen-glucose deprivation and significantly diminishes microglia activation. [2] In human corneal endothelial cell, SB 239063 inhibits TGF-β(2) and FGF-2-induced cell migration. [4]
体内活性
In both guinea pigs and mice, SB 239063 (10 mg/kg, p.o.) reduces antigen-induced airway eosinophilia. [1] In air- and ozone-exposed C57/BL6 and MKP-1(-/-) mice, SB239063 inhibits bronchial contraction. [3]
Cas No.
193551-21-2
分子式
C20H21FN4O2
分子量
368.412
别名
SB239063
储存和溶解度
DMSO:3.7 mg/mL (10 mM)),with gentle warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years