产品说明书

SB 239063

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Chemical Structure| 193551-21-2 同义名 : -
CAS号 : 193551-21-2
货号 : A577018
分子式 : C20H21FN4O2
纯度 : 99%+
分子量 : 368.405
MDL号 : MFCD03792786
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(95 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

5% DMSO+30% PEG 300+water 4 mg/mL

生物活性
靶点

  • p38β

    p38β, IC50:44 nM

  • p38α

    p38α, IC50:44 nM
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
细胞系 浓度 检测类型 检测时间 活动说明 数据源
THP1 cells Function assay Inhibition of LPS-stimulated TNFalpha production in human THP1 cells, IC50=0.12 μM 18077363
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.57mL

2.71mL

1.36mL

27.14mL

5.43mL

2.71mL
参考文献

[1]Strassburger M, Braun H, et al. Anti-inflammatory treatment with the p38 mitogen-activated protein kinase inhibitor SB239063 is neuroprotective, decreases the number of activated microglia and facilitates neurogenesis in oxygen-glucose-deprived hippocampal slice cultures. Eur J Pharmacol. 2008 Sep 11;592(1-3):55-61.

[2]Underwood DC, Osborn RR, et al. SB 239063, a potent p38 MAP kinase inhibitor, reduces inflammatory cytokine production, airways eosinophil infiltration, and persistence. J Pharmacol Exp Ther. 2000 Apr;293(1):281-8.

[3]Zarubin T, Han J. Activation and signaling of the p38 MAP kinase pathway. Cell Res. 2005 Jan;15(1):11-8. doi: 10.1038/sj.cr.7290257. PMID: 15686620.

[4]Underwood DC, Osborn RR, Kotzer CJ, Adams JL, Lee JC, Webb EF, Carpenter DC, Bochnowicz S, Thomas HC, Hay DW, Griswold DE. SB 239063, a potent p38 MAP kinase inhibitor, reduces inflammatory cytokine production, airways eosinophil infiltration, and persistence. J Pharmacol Exp Ther. 2000 Apr;293(1):281-8. PMID: 10734180.

[5]Legos JJ, McLaughlin B, Skaper SD, Strijbos PJ, Parsons AA, Aizenman E, Herin GA, Barone FC, Erhardt JA. The selective p38 inhibitor SB-239063 protects primary neurons from mild to moderate excitotoxic injury. Eur J Pharmacol. 2002 Jun 28;447(1):37-42. doi: 10.1016/s0014-2999(02)01890-3. PMID: 12106800.

[6]Strassburger M, Braun H, Reymann KG. Anti-inflammatory treatment with the p38 mitogen-activated protein kinase inhibitor SB239063 is neuroprotective, decreases the number of activated microglia and facilitates neurogenesis in oxygen-glucose-deprived hippocampal slice cultures. Eur J Pharmacol. 2008 Sep 11;592(1-3):55-61. doi: 10.1016/j.ejphar.2008.06.099. Epub 2008 Jul 3. PMID: 18638472.

[7]Joko T, Shiraishi A, Akune Y, Tokumaru S, Kobayashi T, Miyata K, Ohashi Y. Involvement of P38MAPK in human corneal endothelial cell migration induced by TGF-β(2). Exp Eye Res. 2013 Mar;108:23-32. doi: 10.1016/j.exer.2012.11.018. Epub 2012 Dec 17. PMID: 23257207.