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Hesperadin

现货
Catalog No.
A4118
Aurora B抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,050.00
现货
5mg
¥ 900.00
现货
10mg
¥ 1,550.00
现货
50mg
¥ 5,400.00
现货
200mg
¥ 14,900.00
Ship with 10-15 days

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Background

Hersperadin is an ATP-competitive small molecule inhibitor of Aurora B kinase, which is one of the three Aurora family kinases involved in the regulation of cell division, with half maximal inhibitory concentration IC50 of 250 nM, where the sulphonamide group of hersperadin inserts into the ATP-pocket in the catalytic cleft of Aurora B kinase and extends into the adjacent hydrophobic pocket. Hersperadin has been found to prevent the phosphorylation of Aurora B, where the Ser-10 phosphorylation of Aurora B in mitosis serves as a biomarker for mitotic progression, with IC50 of 40 nM leading to inhibition of chromosome alignment and segregation.

References:
[1]Jetton N1, Rothberg KG, Hubbard JG, Wise J, Li Y, Ball HL, Ruben L. 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. doi: 10.1111/j.1365-2958.2009.06657.x. Epub 2009 Mar 6.
[2]Hauf S1, 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. Epub 2003 Apr 21.

文献引用

1. Kaisari S, Shomer P, et al. "Role of Polo-like kinase 1 in the regulation of the action of p31(comet) in the disassembly of mitotic checkpoint complexes." Proc Natl Acad Sci U S A. 2019 Jun 11;116(24):11725-11730. PMID:31118282
2. Manuel Saldivia, Srinivasa P.S. Rao, et al. "Targeting the trypanosome kinetochore with CLK1 protein kinase inhibitors." bioRxiv. 2019 April 24.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt516.65
Cas No.422513-13-1
FormulaC29H32N4O3S
Solubility≥25.85 mg/mL in DMSO, ≥2.31 mg/mL in EtOH with ultrasonic and warming, <2.6 mg/mL in H2O
Chemical NameN-[(3Z)-2-oxo-3-[phenyl-[4-(piperidin-1-ylmethyl)anilino]methylidene]-1H-indol-5-yl]ethanesulfonamide
SDFDownload SDF
Canonical SMILESCCS(=O)(=O)NC1=CC2=C(C=C1)NC(=O)C2=C(C3=CC=CC=C3)NC4=CC=C(C=C4)CN5CCCCC5
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

体外实验 [1]:

激酶实验

Hesperadin是插入Aurora A和B的ATP结合口袋的抑制剂。它抑制Aurora B的IC50为250 nM,但对于Cdk1 /细胞周期蛋白B或Cdk2 / 细胞周期蛋白E的IC50值在1.2μM至> 10μM的范围内。在浓度为200nM的情况下,Hesperadin将免疫沉淀的激酶的活性降低到背景水平。

细胞实验[2]:

细胞系

HeLa细胞

溶解方法

该化合物在DMSO中的溶解度>25.9mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

50 nM; 2 h

应用

在HeLa细胞中,Hesperadin停止细胞增殖,但不停止生长,并且在6天的时间内,细胞直径增加了超过七倍(从20到150μm)。细胞获得与多倍体相关的扩大的裂核,在第3天达到32C DNA含量。Hesperadin引起有丝分裂和细胞分裂的缺陷。

References:

[1]Jetton N1, Rothberg KG, Hubbard JG, Wise J, Li Y, Ball HL, Ruben L. 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. doi: 10.1111/j.1365-2958.2009.06657.x. Epub 2009 Mar 6.

[2]Hauf S1, 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. Epub 2003 Apr 21.

生物活性

描述 Hesperadin是Aurora B有效的抑制剂,IC50值250 nM。
靶点 Aurora B (human) TbAUK1        
IC50 250 nM 40 nM        

质量控制

化学结构

Hesperadin

相关生物数据

Hesperadin

相关生物数据

Hesperadin

相关生物数据

Hesperadin

相关生物数据

Hesperadin