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DA-E 5090 is an orally effective inhibitor of IL-1 production that can be converted into a pharmacologically active deacetylated form (DA-E5090) in vivo. In this study, the effects of DA-E5090 on IL-1 production in vitro were examined by LPS-stimulated human monocytes. The results showed that DA-E5090 could dose-dependently inhibit the production of IL-1α and IL-1β (1-10 μM) by LPS-stimulated human monocytes, as determined by LAF assay and ELISA. Northern blotting analysis showed that DA-E5090 inhibited the transcription of IL-1α and IL-1β mRNA.