Reversine is a novel class of ATP-competitiveAurora kinaseinhibitor withIC₅₀s of 400, 500 and 400 nM forAurora A,Aurora BandAurora C, respectively.

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 IC₅₀of Reversine is determined on Aurora kinase A to be 400 nM, whereas Aurora kinase B and C IC₅₀are 500 and 400 nM, respectively. The IC₅₀is also determined on MEK1 is >1.5 μM and that the IC₅₀on muscle myosin (an analogue of nonmuscle myosin II) is 350 nM^[1].

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^[2].

393.49

Solid

C₂₁H₂₇N₇O

656820-32-5

逆转素

Room temperature in continental US; may vary elsewhere.

DMSO : 20 mg/mL(50.83 mM;Need ultrasonic)

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