SB 203580 hydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
SB203580 HCl是p38-MAPKs特异性抑制剂,其IC50值为0.6 μM[1]。
SB203580是p38-MAPKα和p38-MAPKβ的抑制剂。在新生肌细胞中,SB203580阻止p38-MAPK激活MAPKAPK2,其IC50值为70 nM。在KB细胞中,SB203580还通过IL-1、渗透压力或亚砷酸盐显著抑制MAPKAPK2活化。在KB细胞中,SB203580也抑制IL-1、化学物质或渗透压力诱导的HSP27磷酸化,其IC50值< 1 μM。在新生大鼠心肌细胞中,SB203580抑制JNK活化c-Jun,其IC50值为3 ~ 10 μM。此外,SB203580干预由MAPKAPK2引起的小分子热休克蛋白磷酸化[1,2]。
参考文献:
[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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 413.9 |
Cas No. | 869185-85-3 |
Formula | C21H17ClFN3OS |
Solubility | insoluble in EtOH; insoluble in H2O; ≥20.7 mg/mL in DMSO |
Chemical Name | 4-(4-(4-fluorophenyl)-2-(4-(methylsulfinyl)phenyl)-1H-imidazol-5-yl)pyridine hydrochloride |
SDF | Download SDF |
Canonical SMILES | FC(C=C1)=CC=C1C(N=C(C2=CC=C(S(C)=O)C=C2)N3)=C3C4=CC=NC=C4.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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. |
描述 | SB203580是p38-MAPKs特异性抑制剂。 | |||||
靶点 | p38MAPK | JNK | ||||
IC50 | 0.6 μM | 3-10 μM |
质量控制和MSDS
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