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SB203580, 1 mg  

SB203580, 1 mg

4-[5-(4-Fluorophenyl)-2-[4-(methylsulfonyl)phenyl]-1H-imidazol-4-yl]pyridine

Synonyms: SB 203580, SB-203580
cell permeable inhibitor of p38 MAP kinase

More details

PKI-SB203-001

Availability: on stock

100,00 €

Background: SB203580 is a highly selective and cell permeable inhibitor of p38 mitogen-activated protein kinase with IC50 values of 50 and 500 nM for p38/SAPK2a and p38/SAPK2b respectively. Also inhibits the phosphoinositide-dependent protein kinase 1 (PDK1) at 10-fold higher concentrations (IC50 ~3-5 µM).  Displays 100-500-fold selectivity over Lck, GSK3b and Akt/PKB. Shown to inhibit interleukin-2-induced T-cell proliferation, cyclooxygenase-1 and -2 and thromboxane synthase.

Chemical formula: C21H16N3FOS
Molecular weight: 377.4 g/mol
Purity: >99%
Solubility: soluble in DMSO
CAS Number: 152121-47-6

Also available predissolved at 10 mM in our MAP kinase Inhibitor Set.

BIAFFIN SERVICES:

Use the p38 MAPK - SPR Binding Assay of BIAFFIN for comprehensive kinetic characterization of your small molecule kinase inhibitors. 

P38a_SB203580.png 

Figure: Real-time kinetic analysis of kinase inhibitor SB203580 binding to p38α using surface plasmon resonance.

We provide our Kinascreen services to kinetically characterize small molecule kinase inhibitors for all p38 isoforms (p38α, p38β, p38γ and p38δ) in their phosphorylated (activated) and unphosphorylated (non-activated) state. 

 

Product specific literature:

Cuenda A, Rouse J, Doza YN, Meier R, Cohen P, Gallagher TF, Young PR, Lee JC. (1995) "SB 203580 is a specific inhibitor of a MAP kinase homologue which is stimulated by cellular stresses and interleukin-1." FEBS Lett. 364(2):229-33

Ward SG, Parry RV, Matthews J, O\'Neill L. (1997) "A p38 MAP kinase inhibitor SB203580 inhibits CD28-dependent T cell proliferation and IL-2 production." Biochem. Soc. Trans. (2):304S

Borsch-Haubold AG, Pasquet S, Watson SP (1998) "Direct inhibition of cyclooxygenase-1 and -2 by the kinase inhibitors SB 203580 and PD 98059. SB 203580 also inhibits thromboxane synthase." J. Biol. Chem. 273(44):28766-72

Kankaanranta H, De Souza PM, Barnes PJ, Salmon M, Giembycz MA, Lindsay MA. (1999) "SB 203580, an inhibitor of p38 mitogen-activated protein kinase, enhances constitutive apoptosis of cytokine-deprived human eosinophils." J. Pharmacol. Exp. Ther. 290(2):621-8.

Lahti A, Kankaanranta H, Moilanen E. (2002) "P38 mitogen-activated protein kinase inhibitor SB203580 has a bi-directional effect on iNOS expression and NO production." Eur. J. Pharmacol. 454(2-3):115-23

Product Citations:

Cui S, Wienhoefer N, Bilitewski U. (2014) "Genistein induces morphology change and G2/M cell cycle arrest by inducing p38 MAPK activation in macrophages." Int Immunopharmacol. 18(1):142-50.

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.