REVERSINE

Reversine是一种强效human A3 adenosine receptor拮抗剂，K_i为0.66 μM，也是一种泛aurora A/B/C kinase抑制剂，IC50分别为12 nM/13 nM/20 nM。也用于干细胞分化。 Reversine induces myogenic lineage-committed cells to become multipotent mesenchymal progenitor cells, which proliferates and redifferentiates into bone and fat cells. Reversine, as an A3 adenosine receptor antagonist, competitively inhibits forskolin-stimulated cAMP production in stably transfected Chinese hamster ovary (CHO) cells. Reversine inhibits the phosphorylation of a well-known Aurora target, histone H3 in HCT116 cells. Moreover, Reversine potently blocks proliferation of multiple tumor cell types, and induces cell death. In primary human tumor samples, Reversine also inhibits colony formation of leukemic cells. When treated in combination, reversine and aspirin synergistically inhibit growth of cervical cancer cells and induce cell apoptosis. In mice inoculated with U14 tumors, Reversine (10 mg/kg i.p.) and aspirin cause more reduced tumor weight and tumor volume when compared with the control agents.