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Hesperadin

Hesperadin 是 Aurora A 和 B 的 ATP 竞争性吲哚酮抑制剂，抑制 Aurora B 的 IC50值为250nM。它通过阻断核分裂和胞质分裂而抑制布鲁氏锥虫的生长。它也是一种广谱流感抗病毒剂。

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

验证数据展示

  • CAS No.: 422513-13-1

    Hesperadin
    CAS#: 422513-13-1

产品信息

Hesperadin(IC50=250 nM) effectively inhibits Aurora B. It potently reduces the activity of AMPK, MAPKAP-K1, MKK1, Lck, CHK1 and PHK, but it could not inhibit MKK1 activity in vivo.

CAS号 422513-13-1
分子式 C29H32N4O3S
主要靶点 Parasite|Autophagy|Aurora Kinase|Influenza Virus
主要通路 表观遗传|微生物学|自噬|细胞周期
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
别名

靶点活性

Aurora B:250 nM

体外活性

In HeLa cells, Hesperadin causing defects in mitosis and cytoplasmic division, leading to cell proliferation and polyploidization stopped, because of Aurora B function inhibition during chromosome connection. Addition of 20-100 nM Hesperadin leading to loss of phosphorylation of the mitogenic histone H3 at the Ser10 site. When Hesperadin concentration was 1 μM, other kinases (AMPK, Lck, MKK1, MAPKAP-K1, CHK1, and PHK) activity were significantly reduced.In an in vitro kinase assay, Hesperadin (IC50 = 40 nM) blocked recombinant trypton histone H3 phosphorylation by T. brucei Aurora kinase-1 (TbAUK1) from the pathogenic Trypanosoma brucei. Hesperadin (IC50 = 48 nM) significantly inhibited the growth of cultured infectious blood form (BF) cells, while Hesperadin (IC50 = 550 nM) and weakly inhibited the growth of insect circulation stage (PF) cells.

溶解度

Ethanol:27.7 mg/mL (50 mM),DMSO:55.3 mg/mL (100 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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