Hesperadin
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Hersperadin是Aurora B的ATP竞争性小分子抑制剂，是与细胞分裂有关的三个Aurora激酶家族成员之一，IC50值250 nM，Hersperadin的磺胺群插入到Aurora B催化位点的ATP结合处并延伸到邻近的疏水腔里。已发现Hersperadin可阻止AuroraB的磷酸化，Aurora B的Ser-10磷酸化在有丝分裂过程中作为一个生物标志物，Hersperadin抑制染色体联合和分离的IC50值为40 nM。
参考文献：
[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.
- 1. Maik Schuler, Lindsay Tomlinson, et al. "Experiments in the EpiDerm 3D Skin In Vitro Model and Minipigs In Vivo Indicate Comparatively Lower In Vivo Skin Sensitivity of Topically Applied Aneugenic Compounds." Toxicol Sci. 2021 Feb 26;180(1):103-121. PMID:33481035
- 2. 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
- 3. Manuel Saldivia, Srinivasa P.S. Rao, et al. "Targeting the trypanosome kinetochore with CLK1 protein kinase inhibitors." bioRxiv. 2019 April 24.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 516.65 |
| Cas No. | 422513-13-1 |
| Formula | C29H32N4O3S |
| Solubility | ≥25.85 mg/mL in DMSO; insoluble in H2O; ≥2.31 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | N-[(3Z)-2-oxo-3-[phenyl-[4-(piperidin-1-ylmethyl)anilino]methylidene]-1H-indol-5-yl]ethanesulfonamide |
| SDF | Download SDF |
| Canonical SMILES | CCS(=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 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。溶液形式一般不宜长期储存，请尽快用完。 |
| 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. |
|
| 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 | ||||
质量控制和MSDS
- 批次:
化学结构
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