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SB 202190

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Chemical Structure| 152121-30-7 同义名 : FHPI
CAS号 : 152121-30-7
货号 : A277214
分子式 : C20H14FN3O
纯度 : 99%+
分子量 : 331.343
MDL号 : MFCD00941964
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(316.89 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+40%PEG300+5%Tween80+50%water 8 mg/mL

生物活性
靶点

  • p38β

    p38β, IC50:100 nM

  • p38α

    p38α, IC50:50 nM
描述 Mitogen-activated protein kinase (MAPK) cascades regulate signal transduction involved in cell proliferation and death. SB-202190 is a potent cell-permeable inhibitor of p38 MAPK that inhibits p38 and p38β with IC50 values of 50 nM and 100 nM, respectively[3]. SB-202190 at 5 μM inhibited the activation of p38 in HaCaT cells. The protein expression of COX-2 was almost completely blocked by 5 μM SB-202190 at 8 and 12 h post the exposure to UVB irradiation (250 J/m2). SB-202190 at the same concentration also significantly abrogated UVB induced cox-2mRNA in HaCaT cells. The inhibitory effect of SB-202190 on PGE2 production after UVB was observed in HaCaT cells treated by 5 μM SB-202190 for one hour[4]. Bull serum albumin induced the gene expression of the inflammation marker MCP-1 more than 30-fold in renal tubular cells, while pre-incubation with 10 μM SB-202190 decreased the gene expression to the basal level. In HK-2 cells, 10 μM SB202190 treatment significantly reduced TGF-β1-induced gene expression[5]. Two doses of SB-202190 (6.25 μg/dose, i.d. administered) prevented the development of blisters and a positive Nikolsky’s skin induced by PV IgG injection (1.5 mg of IgG/g body weight) in neonatal mice. The PV IgG-mediated activation of phospho-p38MAPK immunoreactivity in the skin was abrogated in SB-202190-treated mice[6].
作用机制 SB-202190 is a pyridinyl imidazole that inhibits p38 MAPK via competing with ATP[7].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
A 549 50 μM Function Assay 1 h decreases the level of IL-8  24179688
A549 0.3/3/30 μM Function Assay 1 h significantly attenuates ATPγS-mediated COX-2 protein and mRNA expression and promoter activity  23680674
A549 10 μM  Function Assay 0-30 min inhibits ATPγS induced p42/p44 MAPK and p38 MAPK phosphorylation 23680674
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.02mL

0.60mL

0.30mL

15.09mL

3.02mL

1.51mL

30.18mL

6.04mL

3.02mL
参考文献

[1]351(Pt 1):95-105.

[2]20(29):3921-6.

[3]Davies SP, Reddy H, Caivano M, Cohen P. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.

[4]Chen W, Tang Q, Gonzales MS, Bowden GT. Role of p38 MAP kinases and ERK in mediating ultraviolet-B induced cyclooxygenase-2 gene expression in human keratinocytes. Oncogene. 2001 Jun 28;20(29):3921-6.

[5]Prakash J, Sandovici M, Saluja V, Lacombe M, Schaapveld RQ, de Borst MH, van Goor H, Henning RH, Proost JH, Moolenaar F, Këri G, Meijer DK, Poelstra K, Kok RJ. Intracellular delivery of the p38 mitogen-activated protein kinase inhibitor SB202190 [4-(4-fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)1H-imidazole] in renal tubular cells: a novel strategy to treat renal fibrosis. J Pharmacol Exp Ther. 2006 Oct;319(1):8-19.