Toggle Nav

SB 203580 hydrochloride

In stock
Catalog No.
B1285
Specific p38-MAPKs inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$50.00
In stock
25mg
$63.00
In stock
50mg
$84.00
In stock
100mg
$146.00
In stock
250mg
$282.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

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
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
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

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.

Biological Activity

Description SB203580 is a specific inhibitor of p38MAPK.
Targets p38MAPK JNK        
IC50 0.6 μM 3-10 μM        

Quality Control