SB 203580 hydrochloride
(Synonyms: SB 203580 hydrochloride; RWJ 64809 hydrochloride) 目录号 : GC13001
A water soluble p38 MAPK inhibitor
Cas No.:869185-85-3
Sample solution is provided at 25 µL, 10mM.
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.
| Cell experiment: [1] | |
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Cell lines |
MG-63 cells |
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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. |
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Reaction Conditions |
10 μM, 24 hours |
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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] | |
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Animal models |
Male ddY mice |
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Dosage form |
Subcutaneous injection, 30 mg/kg |
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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. |
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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. |
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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. |
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| Cas No. | 869185-85-3 | SDF | |
| 别名 | SB 203580 hydrochloride; RWJ 64809 hydrochloride | ||
| 化学名 | 4-(4-(4-fluorophenyl)-2-(4-(methylsulfinyl)phenyl)-1H-imidazol-5-yl)pyridine hydrochloride | ||
| Canonical 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 |
| 溶解度 | ≥ 20.7mg/mL in DMSO | 储存条件 | Store at -20°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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.416 mL | 12.0802 mL | 24.1604 mL |
| 5 mM | 0.4832 mL | 2.416 mL | 4.8321 mL |
| 10 mM | 0.2416 mL | 1.208 mL | 2.416 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet