Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Target IC₅₀: 34 nM in vitro, 600 nM in cells against p38 MAPK; 50-100 nM Inhibiting IL-1 and TNF-α production from LPS-stimulated human monocytes and the human monocyte cell line THP-1; 0.2-1.0 µM inhibiting platelet aggregation by collagen

Cell permeable: yes

General description

A highly specific, cell-permeable inhibitor of p38 kinase (IC₅₀ = 34 nM in vitro, 600 nM in cells). Also known as reactivating kinase (RK) and CSBP (cytokine synthesis anti-inflammatory drug binding protein). Does not significantly inhibit JNK or p42 MAP kinase even at 100 µM. Inhibits IL-1 and TNF-α production from LPS-stimulated human monocytes and the human monocyte cell line THP-1 (IC₅₀ = 50-100 nM). SB 203580 has also been shown to be an effective inhibitor of inflammatory cytokine production in vivo in both mice and rats.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Powell, D.J., et al. 2003. Mol. Cell Biol.23, 7794.Davies, S.P., et al. 2000. Biochem. J.351, 95.Iwasaki, S., et al. 1999. J. Biol. Chem.274, 26503.Gallagher, T.F., et al. 1997. Bioorg. Med. Chem. 5, 49.LoGrasso, P.V., et al. 1997. Biochem. 36, 10422.Hazzalin, C.A., et al. 1996. Curr. Biol.6, 1028.Kramer, R.M., et al. 1996. J. Biol. Chem.271, 27723.Saklatvala, J., et al. 1996. J. Biol. Chem. 271, 6586.Cuenda, A., et al. 1995. FEBS Lett.364, 229.Gallagher, T.F., et al. 1995. Bioorg. Med. Chem. Lett. 5, 1171.Lee, J.C., et al. 1994. Nature 372, 739.

Packaging

Packaged under inert gas

1 ml in Plastic ampoule

Physical form

A 1 mg/ml solution of SB 203580 (Cat. No. 559389) in anhydrous DMSO.

Warning

Toxicity: Irritant (B)