Background: Benzothiazole and its derivatives have been extensive studied due to their versatile biological properties and pharmaceutical applications. We recently found that the BMP326 (1-(1,3-benzothiazol-2-yl)-3-(2-methoxyphenyl)-1H-pyrazol-5-ol), a novel benzothiazole derivative, have anti-inflammatory properties in lipopolysaccharide(LPS)-induced RAW264.7 macrophages and there were no relevant reports previously. Methods and Results: Treatment with BMP326(5, 10 and 20 μM) can significantly inhibit nitric oxide production and down-regulate mRNA expression of nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) but did not cause significant cytotoxicity on RAW264.7 macrophages. It is also observed BMP326 can inhibit LPS-stimulated interleukin (IL)-6, interleukin(IL)-1β, tumor necrosis factor (TNF)-α production depending on its dosage. The gene transcription levels of IL-6, IL-1β and TNF-α were reduced under BMP326 exposure in LPS-treated RAW264.7 cells. In addition, we explored the inhibitory mechanisms of BMP326 on the production of pro-inflammatory mediators. The results showed that BMP326 inhibited nuclear factor kappa B (NF-κB) activation by reducing the phosphorylation of p65 and IκBα. Moreover, the phosphorylation of p38 MAPK (p38), extracellular signal-regulated kinases 1/2 (ERK1/2), and c-Jun N-terminal kinase (JNK) in RAW264.7 cells which are stimulated with LPS were suppressed in a dose-dependent manner. Conclusions: In summary, these results suggest that BMP326 exerts anti-inflammatory properties via suppression of the NF-κB and MAPKs signaling pathways.