CAY10571

Pyridinylimidazoles, often termed CSAIDs, are a class of anti-inflammatory compounds that inhibit eicosanoid production and suppress the synthesis of cytokines in human monocytes.¹ Because of its high specificity, one predominant pyridinylimidazole, SB203580, is frequently used to inhibit p38 MAPK, the tyrosine kinase activated by environmental stresses and inflammatory cytokines.² CAY10571 is an analog of SB203580. It inhibits IL-1 production in the human monocytic cell line THP with an IC₅₀ value of 0.20 µM and binds CSAID binding protein, a serine/threonine kinase homologous to p38, inhibiting its kinase activity with an IC₅₀ value of 0.03 µM.^3,4 CAY105571 also inhibits 5-lipoxygenase production in RBL-1 cells with an IC₅₀ value of 24 µM.³

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1. Lee, J.C., Laydon, J.T., McDonnell, P.C., et al. A protein kinase involved in the regulation of inflammatory cytokine biosynthesis. Nature 372(6508), 739-746 (1994).

2. 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 Lett. 364(2), 229-233 (1995).

3. Gallagher, T.F., Fier-Thompson, S.M., Garigipati, R.S., et al. 2,4,5-triarylimidazole inhibitors of IL-1 biosynthesis. Bioorg. Med. Chem. Lett. 5(11), 1171-1176 (1995).

4. Gallagher, T.F., Seibel, G.L., Kassis, S., et al. Regulation of stress-induced cytokine production by pyridinylimidazoles; Inhibition of CSBP kinase. Bioorg. Med. Chem. 5(1), 49-64 (1997).