信号转导通路: HDAC-HSP-Aurora >> Aurora Kinase >> Aurora Kinase YZ剂 >> Hesperadin
http://selleck.cn/hesperadin-S1529.html
技术数据:
分子量(MW): 516.65
化学式:
C29H32N4O3S
溶解度: DMSO ≥103mg/mL Water <1mg/mL Ethanol ≥3mg/mL
纯度: >99%
稳定性: at -20℃ 2 years
CAS号: 422513-13-1
生物活性
Hesperadin is a human Aurora B inhibitor with an IC50 of 40 nM for the prevention of the phosphorylation of substrate. Growth of cultured bloodstream forms (BF) was also sensitive to Hesperadin with an IC50 of 50 nM. It blocked nuclear division and cytokinesis, but not other aspects of the cell cycle. Mammalian cells treated with Hesperadin enter anaphase in the presence of numerous monooriented chromosomes, many of which may have both sister kinetochores attached to one spindle pole (syntelic attachment). Hesperadin also causes cells arrested by taxol or monastrol to enter anaphase within <1 h, whereas cells in nocodazole stay arrested for 3-5 h. [1][2][3]
参考文献
The cell cycle as a therapeutic target against Trypanosoma brucei: Hesperadin inhibits Aurora kinase-1 and blocks mitotic progression in bloodstream forms Neal Jetton, Karen G. Rothberg,et al. Mol Microbiol 2009 April;72(2): 442–458
The small molecule Hesperadin reveals a role for Aurora B in correcting kinetochore–microtubule attachment and in maintaining the spindle assembly checkpoint Silke Hauf,Richard W. Cole,et al. The Journal of Cell Biology 2003;161:281–294
Mechanism of Aurora B Activation by INCENP and Inhibition by Hesperadin Fabio Sessa,Marina Mapelli,et al. Molecular Cell April 29, 2005;18:379–391
客户反馈数据
Western blot analysis of p-histone and histone. 0-10μM Hesperadin was added.
HeLa cells treated with nocodazole containing DMSO or Hesperadin (100 nM) for 2h and stained with the indicated antibodies.
Time-lapse analysis of duration of mitotic arrest in U2OScells treated with Hec1 siRNA and indicated inhibitors in cells non-induced or induced to express LAP–Mis12–Mps1Δ200. Data indicate cumulative percentage of cells (from 50 cells per treatment) that exit mitosis (scored as cell flattening) at the indicated times after NEB, and are representative of three independent experiments.
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