化學(xué)名

4-[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)imidazol-1-yl]cyclohexan-1-ol

簡稱

SB239063

別名

SB 239063, SB-239063

中文名

N/A

化學(xué)式

C₂₀H₂₁FN₄O₂

分子量

368.4

CAS號

193551-21-2

純度

98%

溶劑/溶解度

Water<1mg/ml; DMSO60mg/ml; Ethanol7mg/ml warming

溶液配制

5mg加入1.36ml DMSO，或者每3.68mg加入1ml DMSO，配制成10mM溶液。SD5937-10mM用DMSO配制。

產(chǎn)品描述

SB239063是一種有效的選擇性p38 MAPKα/β抑制劑，IC50為44nM，對γ-和δ-激酶亞型沒有活性。

信號通路

MAPK

靶點(diǎn)

p38α

p38β

－

－

－

IC50

44nM

44nM

－

－

－

體外研究

SB 239063 potently inhibits IL-1 and TNF-α production in LPS-stimulated human peripheral blood monocytes with IC50 of 120 and 350nM, respectively. 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. In human corneal endothelial cell, SB 239063 inhibits TGF-β(2) and FGF-2-induced cell migration.

體內(nèi)研究

In both guinea pigs and mice, SB 239063 (10mg/kg, p.o.) reduces antigen-induced airway eosinophilia. In air- and ozone-exposed C57/BL6 and MKP-1(-/-) mice, SB239063 inhibits bronchial contraction.

臨床實(shí)驗(yàn)

N/A

特征

N/A

酶活性檢測實(shí)驗(yàn)

方法

Yeast-expressed, activated, and purified p38α (3.55nM) is added to the reaction mixture (30μl) containing 25mM HEPES, pH 7.5; 10mM MgCl2; 0.2mM sodium orthovanadate; 1mM dithiothreitol; 0.1% BSA; 10% (w/v) glycerol; 0.17mM/2.5 μCi of [γ-32P]ATP; 0.67mM the endothelial growth factor receptor-derived T669 peptide as the substrate in the presence or absence of SB 239063. Incubation is for 25 min at 37℃ in 96-well plates, the reactions are stopped by adding 10μl of 0.3M phosphoric acid, and phosphorylated peptide is isolated from the reaction mixture on phosphocellulose (p81) filters. Filters are washed three times with 75mM phosphoric acid, followed by three times with H2O, and counted for bound 32P. The inhibitor is preincubated with the reaction mixture on ice for 30 min before starting the reactions with [γ-32P]ATP.

細(xì)胞實(shí)驗(yàn)

細(xì)胞系

N/A

濃度

N/A

處理時間

N/A

方法

N/A

動物實(shí)驗(yàn)

動物模型

Guinea pigs

配制

Acidified 0.5% Tragacanth

劑量

~30mg/kg

給藥方式

p.o.

產(chǎn)品編號

產(chǎn)品名稱

包裝

SD5937-10mM

SB239063 (p38 MAPK抑制劑)

10mM×0.2ml

SD5937-5mg

SB239063 (p38 MAPK抑制劑)

5mg

SD5937-25mg

SB239063 (p38 MAPK抑制劑)

25mg

—

說明書

1份