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SB 203580 hydrochloride

现货
Catalog No.
B1285
p38-MAPK特异性抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 500.00
现货
25mg
¥ 630.00
现货
50mg
¥ 840.00
现货
100mg
¥ 1,460.00
现货
250mg
¥ 2,820.00
现货

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Background

SB203580 HCl is a specific inhibitor of p38-MAPKs with IC50 value of 0.6 μM [1].

SB203580 is an inhibitor of p38-MAPKα and p38-MAPKβ. In neonatal myocytes, SB203580 prevented p38-MAPK from activating MAPKAPK2 with IC50 value of 70 nM. It also significantly suppressed MAPKAPK2 activation in by IL-1, osmotic stress or arsenite in KB cells. In neonatal rat ventricular myocytes, SB203580 inhibited JNK activity of activating c-Jun with IC50 value of 3-10 μM. Besides that, SB203580 affected the phosphorylation of small heat shock proteins caused by MAPKAPK2. It inhibited the IL-1-, chemical- or osmotic stress-stimulated HSP27 phosphorylation with IC50 value of < 1μM in KB cells [1, 2].

References:
[1] Cuenda A, Rouse J, Doza Y N, et al. SB 203580 is a specific inhibitor of a MAP kinase homologue which is stimulated by cellular stresses and interleukin-1. FEBS letters, 1995, 364(2): 229-233.
[2] Clerk A, Sugden P H. The p38-MAPK inhibitor, SB203580, inhibits cardiac stress-activated protein kinases/c-Jun N-terminal kinases (SAPKs/JNKs). FEBS letters, 1998, 426(1): 93-96.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt413.9
Cas No.869185-85-3
FormulaC21H17ClFN3OS
Solubility≥20.7mg/mL in DMSO, <2.1 mg/mL in EtOH, <2.13 mg/mL in H2O
Chemical Name4-(4-(4-fluorophenyl)-2-(4-(methylsulfinyl)phenyl)-1H-imidazol-5-yl)pyridine hydrochloride
SDFDownload SDF
Canonical SMILESFC(C=C1)=CC=C1C(N=C(C2=CC=C(S(C)=O)C=C2)N3)=C3C4=CC=NC=C4.Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验: [1]

细胞系

MG-63细胞

制备方法

该化合物在DMSO中的溶解度大于10 mM,若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

10 μM,24小时

实验结果

在用10 ng/mL的TNF-α刺激24小时之前,将细胞与各种浓度的SB203580 HCl(10、5和1 μM)温育60分钟。在MG-63细胞中,TNF-α以时间和剂量依赖性方式刺激白细胞介素-6的生成,而p38 MAPK抑制剂SB203580 HCl预孵育导致TNF-α诱导的IL-6的分泌统计学显著降低。

动物实验: [2]

动物模型

雄性ddY小鼠

给药剂量

皮下注射,30 mg/kg

实验结果

在轻乙醚麻醉下,将25微升的1%carrageenan注入右后爪。使用体积描记器测量carrageenan注射前后6小时的爪体积。在carrageenan注射前1小时皮下注射抑制剂,它显著抑制carrageenan诱导的水肿。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1] Webb S J, McPherson J R, Pahan K, et al. Regulation of TNF-α-induced IL-6 production in MG-63 human osteoblast-like cells. Journal of dental research, 2002, 81(1): 17-22.

[2] Nishikori T, Irie K, Suganuma T, et al. Anti-inflammatory potency of FR167653, a p38 mitogen-activated protein kinase inhibitor, in mouse models of acute inflammation. European journal of pharmacology, 2002, 451(3): 327-333.

生物活性

描述 SB203580是p38-MAPKs特异性抑制剂。
靶点 p38MAPK JNK        
IC50 0.6 μM 3-10 μM        

质量控制