"目录号: HY-14711
Cell Cycle/DNA DamageEpigenetics-
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。
Aurora Kinase
相关产品
Alisertib-Tozasertib-AMG 900-Danusertib-AT9283-AZD1152-HQPA-Hesperadin-MK-5108-MLN8054-ZM-447439-AZD1152-TAK-901-GSK-1070916-JNJ-7706621-PF-03814735-
生物活性
Description
Reversine is a novel class of ATP-competitiveAurora kinaseinhibitor withIC50s of 400, 500 and 400 nM forAurora A,Aurora BandAurora C, respectively.
IC50& Target
IC50: 400 nM (Aurora Kinase A), 500 nM (Aurora Kinase B), 400 nM (Aurora Kinase C)[1]
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 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].
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[2].
References
[1].D'Alise AM, et al. Reversine, a novel Aurora kinases inhibitor, inhibits colony formation of human acute myeloid leukemia cells. Mol Cancer Ther. 2008 May;7(5):1140-9.
[2].Qin HX, et al. Synergistic antitumor activity of reversine combined with aspirin in cervical carcinoma in vitro and in vivo. Cytotechnology. 2013 Aug;65(4):643-53.