标签归档：hesperadin

Hesperadin hydrochloride

发表于由

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

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Hesperadin

发表于由

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  纯度: ≥98.0%

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

Hesperadin

Hesperadin Chemical Structure

CAS No. : 422513-13-1

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥909 In-stock
5 mg ￥800 In-stock
10 mg ￥1500 In-stock
50 mg ￥5400 In-stock
100 mg ￥9200 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Hesperadin 相关产品

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生物活性

Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC50 of 250 nM. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral[1][2][3].

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].

上海金畔生物科技有限公司 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 IC50 of 50 nM, while the inhibition of PF growth required approximately 11-fold more Hesperadin, with 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].

上海金畔生物科技有限公司 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

516.65

Formula

C29H32N4O3S
CAS 号

422513-13-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (193.55 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9355 mL 9.6777 mL 19.3555 mL
5 mM 0.3871 mL 1.9355 mL 3.8711 mL
10 mM 0.1936 mL 0.9678 mL 1.9355 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.84 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.84 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

    [3]. Hu Y, et, al. Chemical Genomics Approach Leads to the Identification of Hesperadin, an Aurora B Kinase Inhibitor, as a Broad-Spectrum Influenza Antiviral. Int J Mol Sci. 2017 Sep 8;18(9):1929.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务