产品说明书

Hesperadin

Print
Chemical Structure| 422513-13-1 同义名 : -
CAS号 : 422513-13-1
货号 : A899555
分子式 : C29H32N4O3S
纯度 : 98%
分子量 : 516.654
MDL号 : MFCD18074526
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(203.23 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

5% DMSO+40%PEG300+5% tween80+50% water 2.5 mg/mL

生物活性
靶点

  • Aurora B

    Aurora B (human), IC50:250 nM
描述 Hesperadin is an inhibitor of chromosome alignment and segregation. Hesperadin causes this phenotype by inhibiting the function of the mitotic kinase Aurora B. 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[3]. Hesperadin, an inhibitor of human Aurora B, prevented the phosphorylation of substrate with IC(50) of 40 nM. Hesperadin blocked nuclear division and cytokinesis but not other aspects of the cell cycle. Hesperadin provides neuroprotection against ICH (intracerebral hemorrhage) by inhibiting the MST4/AKT signaling pathway[4]. Hesperadin induces delayed transition from metaphase to anaphase, and early exit from mitosis after chromosome segregation. In addition, micronuclei were observed frequently and lagging chromosomes, caused by the delay and failure of sister chromatid separation, were observed at anaphase and telophase in Hesperadin-treated BY-2 cells[5]. Hesperadin inhibits multiple human clinical isolates of influenza A and B viruses with single to submicromolar efficacy, including oseltamivir-resistant strains. Mechanistic studies revealed that hesperadin inhibits the early stage of viral replication by delaying the nuclear entry of viral ribonucleoprotein complex, thereby inhibiting viral RNA transcription and translation as well as viral protein synthesis. Moreover, a combination of hesperadin with oseltamivir shows synergistic antiviral activity[6].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
HepG2 cells Cytotoxicity assay 48 h Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, TC50=0.2 μM 24910766
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.94mL

0.39mL

0.19mL

9.68mL

1.94mL

0.97mL

19.36mL

3.87mL

1.94mL
参考文献

[1]Jetton N, Rothberg KG, et al. The cell cycle as a therapeutic target against Trypanosoma brucei: Hesperadin inhibits Aurora kinase-1 and blocks mitotic progression in bloodstream forms. Mol Microbiol. 2009 Apr;72(2):442-58.

[2]Hauf S, Cole RW, et al. The small molecule Hesperadin reveals a role for Aurora B in correcting kinetochore-microtubule attachment and in maintaining the spindle assembly checkpoint. J Cell Biol. 2003 Apr 28;161(2):281-94.

[3]Hauf S, Cole RW, LaTerra S, Zimmer C, Schnapp G, Walter R, Heckel A, van Meel J, Rieder CL, Peters JM. The small molecule Hesperadin reveals a role for Aurora B in correcting kinetochore-microtubule attachment and in maintaining the spindle assembly checkpoint. J Cell Biol. 2003 Apr 28;161(2):281-94

[4]Wu X, Wu J, Hu W, Wang Q, Liu H, Chu Z, Lv K, Xu Y. MST4 Kinase Inhibitor Hesperadin Attenuates Autophagy and Behavioral Disorder via the MST4/AKT Pathway in Intracerebral Hemorrhage Mice. Behav Neurol. 2020 Feb 3;2020:2476861

[5]Kurihara D, Matsunaga S, Kawabe A, Fujimoto S, Noda M, Uchiyama S, Fukui K. Aurora kinase is required for chromosome segregation in tobacco BY-2 cells. Plant J. 2006 Nov;48(4):572-80

[6]Hu Y, Zhang J, Musharrafieh R, Hau R, Ma C, Wang J. Chemical Genomics Approach Leads to the Identification of Hesperadin, an Aurora B Kinase Inhibitor, as a Broad-Spectrum Influenza Antiviral. Int J Mol Sci. 2017 Sep 8;18(9):1929