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Hesperadin

CAS号

422513-13-1

分子式

C29H32N4O3S

主要靶点

Parasite|Autophagy|Aurora Kinase|Influenza Virus

仅限科研使用

Cat No : CM03081

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Synonyms

bloodstream|Autophagy|Aurora|AuroraKinase|Aurora Kinase|Aurora B (human)|forms|Hesperadin|Influenza Virus|InfluenzaVirus|Parasite|procyclic|Inhibitor|inhibit|TbAUK1

验证数据展示

  • CAS No.: 422513-13-1

    Hesperadin
    CAS#: 422513-13-1

产品信息

CAS号 422513-13-1
分子式 C29H32N4O3S
主要靶点 Parasite|Autophagy|Aurora Kinase|Influenza Virus
主要通路 微生物学|微生物学|表观遗传|细胞周期|自噬
分子量 516.65
纯度 99.44%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 bloodstream|Autophagy|Aurora|AuroraKinase|Aurora Kinase|Aurora B (human)|forms|Hesperadin|Influenza Virus|InfluenzaVirus|Parasite|procyclic|Inhibitor|inhibit|TbAUK1

靶点活性

Aurora B:250 nM

体外活性

在HeLa细胞中，Hesperadin通过抑制Aurora B的功能，干扰染色体连接，造成有丝分裂和细胞质分裂缺陷，导致细胞增殖停止和多倍体化。Hesperadin在20-100 nM浓度作用下，导致有丝分裂活化组蛋白H3在Ser10位点的磷酸化丢失。当Hesperadin浓度达到1 μM时，其他激酶（AMPK, Lck, MKK1, MAPKAP-K1, CHK1, 和 PHK）活性显著降低。在体外激酶测定中，Hesperadin（IC50 = 40 nM）阻断了来自病原性锥虫（Trypanosoma brucei）的TbAUK1（T. brucei Aurora kinase-1）对重组色质组蛋白H3的磷酸化。Hesperadin（IC50 = 48 nM）显著抑制了培养的传染性血液形式（BF）细胞的生长，而以IC50 = 550 nM的浓度弱抑制了昆虫循环阶段（PF）细胞的生长。

溶解度

DMSO:55.3 mg/mL (107.04 mM);Ethanol:27.7 mg/mL (53.61 mM)

细胞实验

HeLa cells and PtK1 cells are added Hesperadin 500 nM for 24 and 48 hours.

参考文献

1.Hauf S, et al. J Cell Biol, 2003, 161(2), 281-294.
2.Jetton N, et al. Mol Microbiol, 2009, 72(2), 442-458.
3.Wang J, Yan X, Chen H, et al. Enhanced UV-B radiation affects AUR1 regulation of mitotic spindle morphology leading to aberrant mitosis[J]. Plant Physiology and Biochemistry. 159: 160-170.

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