SB 202190

Biochem/physiol Actions

Target IC₅₀: 350 nM against the kinase activity of p38β; 280 nM against p38 phosphorylation of activating transcription factor 2 (ATF-2)

Primary Targetp38β

Reversible: yes

Product competes with ATP.

Cell permeable: yes

General description

A potent, reversible, competitive, and cell-permeable inhibitor of p38 MAP kinase. Inhibits p38 phosphorylation of myelin basic protein (MBP) with no effect on the activity of the ERK or JNK MAP kinase subgroups. Also inhibits the kinase activity of p38β (K_i = 16 nM; IC₅₀ = 350 nM) and p38 phosphorylation of activating transcription factor 2 (ATF-2; IC₅₀ = 280 nM). Blocks LPS-induced TNF-α and interleukin biosynthesis. Reported to induce LDL receptor expression in Hep52 cells. A 1 mg/ml solution of SB 202190 (Cat. No. 559397) in anhydrous DMSO is also available.

A potent, reversible, competitive, and cell-permeable inhibitor of p38 MAP kinase. Inhibits p38 phosphorylation of myelin basic protein (MBP) with no effect on the activity of the ERK or JNK MAP kinase subgroups. Also inhibits the kinase activity of p38β (K_i = 16 nM; IC₅₀ = 350 nM) and p38 phosphorylation of activating transcription factor 2 (ATF-2; IC₅₀ = 280 nM). Blocks LPS-induced TNF-α and interleukin biosynthesis. Reported to induce LDL receptor expression in Hep52 cells.

Legal Information

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

Other Notes

Davies, S.P., et al. 2000. Biochem. J.351, 95.Ajizian, S.J., et al. 1999. J. Infect. Dis.179, 939.Singh, R.P., et al. 1999. J. Biol. Chem.274, 19593.Wang, S.W., et al. 1999. Inflamm. Res.48, 533. Gallagher, T.F., et al. 1997. Bioorg. Med. Chem. 5, 49.LoGrasso, P.V., et al. 1997. Biochem. 36, 10422.Jiang, Y., et al. 1996. J. Biol. Chem. 271, 17920.Kramer, R.M., et al. 1996. J. Biol. Chem.271, 27723.Li, Z., et al. 1996. Biochem. Biophys. Res.Commun. 228, 334.Lee, J.C., et al. 1994. Nature 372, 739.

Packaging

1 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)