Hesperadin hydrochloride

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Hesperadin hydrochloride 

Hesperadin hydrochloride 是 Aurora A 和 B 的 ATP 竞争性吲哚酮抑制剂。Hesperadin hydrochloride 以 250 nM 的 IC50 抑制 Aurora B。

Hesperadin hydrochloride

Hesperadin hydrochloride Chemical Structure

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Hesperadin hydrochloride 的其他形式现货产品:

Hesperadin

生物活性

Hesperadin hydrochloride is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin hydrochloride inhibits Aurora B with an IC50 of 250 nM[1].

IC50 & Target[1]

Aurora B

250 nM (IC50)

体外研究
(In Vitro)

Hesperadin (10-100 nM) inhibits the Aurora kinase-1 (TbAUK1)-mediated phosphoryation of trypanosome histone H3 (TbH3) in a dose dependent manner, with an IC50 of 40 nM[1].
Hesperadin (0.01-10 μM; 24 or 48 hours) inhibits growth of bloodstream forms (BF) and procyclic forms (PF) cultures[1].
Hesperadin (100-200 nM; 24-72 hours) alters cell morphology and inhibits cell cycle progression similar to the RNAi knockdown of TbAUK1[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: M110 cells
Concentration: 0.01, 0.1, 1, 10 μM
Incubation Time: 24 hours or 48 hours
Result: Inhibiting growth of BF cultures with an IC50 of 50 nM, while the inhibition of PF growth required approximately 11-fold more Hesperadin, with an IC50 of 550 nM.

Cell Cycle Analysis[1]

Cell Line: M110 cells
Concentration: 100, 200 nM
Incubation Time: 24, 48, 72 hours
Result: Had a strong effect on cell growth and mitotic progression at 100-200 nM.

体内研究
(In Vivo)

Hesperadin (20 mg/kg/d; i.v.) prolongs the survival of xenograft mice via synergistic effect with Temozolomide (TMZ)[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-week-old female nude mice injected GBM cells[2]
Dosage: 20 mg/kg/d
Administration: I.v. injection
Result: Increased the survival of xenograft mice models.

分子量

553.12

Formula

C29H33ClN4O3S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Neal J, 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]. Wahafu A, et, al. Targeting Aurora kinase B attenuates chemoresistance in glioblastoma via a synergistic manner with temozolomide. Pathol Res Pract. 2019 Nov; 215(11): 152617.

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