SB 203580 hydrochloride

目录号: GC13001纯度: >98.00%同义词: SB 203580 hydrochloride; RWJ 64809 hydrochloride
A water soluble p38 MAPK inhibitor

SB 203580 hydrochloride
Cas No.: 869185-85-3
规格价格库存数量操作
25mg¥483.00现货
1
50mg¥630.00现货
1
100mg¥1,124.00现货
1
250mg¥2,142.00现货
1
10mM (in 1mL DMSO)¥347.00现货
1

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产品描述 Description

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.

实验参考方法 Experimental Reference Method

Cell experiment: [1]

Cell lines

MG-63 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

10 μM, 24 hours

Applications

Cells were incubated for 60 min with various concentrations of SB203580 HCl (10, 5, and 1 μM) prior to stimulation with TNF-α (10 ng/mL) for 24 hrs. Interleukin-6 production by TNF-α was stimulated in MG-63 cells, in a time- and dose-dependent manner, while pre-incubation with the p38 MAPK inhibitor SB203580HCl caused a statistically significant decrease in TNF-α-induced IL-6 secretion.

Animal experiment: [2]

Animal models

Male ddY mice

Dosage form

Subcutaneous injection, 30 mg/kg

Applications

Twenty-five microliters of 1% carrageenan was injected into the right hind paw under light ether anesthesia. Paw volume was measured before and after carrageenan injection up to 6 h, using a plethysmograph. The inhibitor was injected s.c. at the back 1 h prior to carrageenan injection. It significantly inhibited the edema induced by carrageenan.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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.

产品文档 Product Documents

Purity:>98.00%

相关生物学数据Related Biological Data

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化学性质Chemical Properties

CAS 号
869185-85-3
同义词
SB 203580 hydrochloride; RWJ 64809 hydrochloride
化学名
4-(4-(4-fluorophenyl)-2-(4-(methylsulfinyl)phenyl)-1H-imidazol-5-yl)pyridine hydrochloride
SMILES
FC(C=C1)=CC=C1C(N=C(C2=CC=C(S(C)=O)C=C2)N3)=C3C4=CC=NC=C4.Cl
分子式
C21H17ClFN3OS
分子量
413.9 g/mol
溶解性
≥ 20.7mg/mL in DMSO
保存条件
Store at -20&deg;C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol