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説明

Hesperadin is a multi-kinase inhibitor. It inhibits human Aurora kinase B (IC₅₀ = 250 nM) and its T. brucei homolog Aurora kinase-1 (IC₅₀ = 40 nM) in in vitro kinase assays. Hesperadin (1 μM) inhibits AMPK, LCK, MKK1, MAPKAP-K1, CHK1, and PHK in a panel of 25 kinases. It also inhibits MEKK2 in ATPase and transphosphorylation assays with IC₅₀s of 60 and 34 nM, respectively. Hesperadin (50-100 nM) induces polyploidy and defects in cytokinesis and spindle assembly as well as inhibits proliferation of HeLa cells and overrides mitotic arrest induced by paclitaxel or monastrol . Hesperadin also induces toxicity in HepG2 cells with a toxic concentration (TC₅₀) value of less than 0.2 μM. It inhibits replication of clinical isolates of influenza A and B viruses with EC₅₀s ranging from 0.22 to 2.21 μM in a plaque formation assay. Hesperadin inhibits the growth of T. brucei, L. major promastigotes and amastigotes, and P. falciparum with EC₅₀ values ranging from 0.01 to 2.37 μM, but has less activity against T. cruzi (EC₅₀ = 39 μM).