A water soluble p38 MAPK inhibitor
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].
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.
| 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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参考文献: [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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