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Reversine

CAS No. : 656820-32-5

MCE 国际站：Reversine

产品活性：Reversine 是一种ATP-竞争性的 Aurora kinase 抑制剂，作用于 Aurora A，Aurora B 和 Aurora C，IC₅₀ 分别为 400，500 和 400 nM。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics  |  Autophagy

作用靶点：Aurora Kinase  |  Autophagy

In Vitro: Reversine, a novel Aurora kinases inhibitor, inhibits colony formation of human acute myeloid leukemia cells. Reversine is a potent inhibitor of Aurora A and B and is also an inhibitor of Aurora C kinase. Aurora A and B activities are inhibited by 80% and Aurora kinase C by 55%, already at a concentration of 0.5 μM, whereas no inhibition or only modest inhibition is observed on others kinases tested. In a second round of experiments, the IC₅₀ of Reversine is determined on Aurora kinase A to be 400 nM, whereas Aurora kinase B and C IC₅₀ are 500 and 400 nM, respectively. The IC₅₀ is also determined on MEK1 is >1.5 μM and that the IC₅₀ on muscle myosin (an analogue of nonmuscle myosin II) is 350 nM.

In Vivo: The combination of Reversine and Aspirin can more efficiently induce cell cycle arrest and apoptosis. To evaluate the anti-tumor effect of this combination, a xenograft nude mouse model is established by s.c. injection. Mice inoculated with cervical cancer cells have lost about 10 % of their initial body weight by about 16 days after tumor inoculation. However, tumor growth (tumor weight) is reduced and the mice survive longer in the combination group.

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