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CAS No.: 193551-21-2

SB 239063 Catalog No. CSN12897

Synonyms: SB-239063

SB 239063 is a potent, selective and oral active p38 MAPK inhibitor with IC50 of 44 nM for recombinant purified p38α.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The family members of the mitogen-activated protein kinase (MAPK) mediate a wide variety of cellular behaviors in response to extracellular stimuli. One of the four main sub-groups, the p38 group of MAP kinases, serve as a nexus for signal transduction and play a vital role in numerous biological processes^[3]. SB-239063 is a potent, selective and orally active p38 MAPK inhibitor, exhibits an IC₅₀ of 44 nM for recombinant purified human p38α, with equipotent inhibitory activity against p38α and p38β. It has no effect on p38γ or p38δ^[4]. In lipopolysaccharide-stimulated human peripheral blood monocytes, SB-239063 inhibited interleukin-1 and tumor necrosis factor-alpha production with IC₅₀ values of 0.12 and 0.35 μM, respectively^[4]. SB-239063 provided substantial protection against cell death induced by either oxygen glucose deprivation (OGD) or magnesium deprivation in cultured neurons^[5]. In oxygen-glucose-deprived hippocampal slice cultures, SB-239063 strikingly reduces the levels of the pro-inflammatory cytokine IL-1β, causes cell death after oxygen-glucose deprivation and significantly diminishes microglia activation^[6]. In human corneal endothelial cell, SB-239063 inhibits TGF-β (2) and FGF-2-induced cell migration^[7]. In both guinea pigs and mice, SB-239063 (10 mg/kg, p.o.) reduces antigen-induced airway eosinophilia, SB-239063 (12 mg/kg; p.o.) almost abolishes ovalbumin (OA)-induced airway eosinophilia (~ 93% inhibition) by inhalation^[4].
细胞研究
Cell Data
Cell Lines Concentration Assay Type Time Activity Description Data Sources
THP1 cells - Function assay - Inhibition of LPS-stimulated TNFalpha production in human THP1 cells, IC50=0.12 μM 18077363
动物研究
剂量
Rat: 3 mg/kg - 30 mg/kg^[3] (p.o.)

给药途径
p.o.
参考文献

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
THP1 cells	-	Function assay	-	Inhibition of LPS-stimulated TNFalpha production in human THP1 cells, IC50=0.12 μM	18077363

动物研究
剂量	Rat: 3 mg/kg - 30 mg/kg^[3] (p.o.)
给药途径	p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7144 mL
- 13.5720 mL
- 27.1441 mL
- 5 mM
- 0.5429 mL
- 2.7144 mL
- 5.4288 mL
- 10 mM
- 0.2714 mL
- 1.3572 mL
- 2.7144 mL

技术信息

CAS号

193551-21-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H21FN4O2

运输

蓝冰

分子量

368.40

别名

SB-239063

溶解度

DMSO	107.0 mg/mL (290.4 mM) warming
Water	90.0 mg/mL (244.3 mM) warming

动物实验配方

5% DMSO+30% PEG 300+water

4 mg/mL

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