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CAS No.: 422513-13-1

Hesperadin Catalog No. CSN13761

Synonyms: Hesperadin

Hesperadin is a potent and ATP-competitive inhibitor of Aurora B kinase with IC50 of 250 nM.

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生物活性

实验方案

技术信息

生物活性

描述Hesperadin is an inhibitor of chromosome alignment and segregation. Hesperadin causes this phenotype by inhibiting the function of the mitotic kinase Aurora B. Mammalian cells treated with Hesperadin enter anaphase in the presence of numerous monooriented chromosomes, many of which may have both sister kinetochores attached to one spindle pole (syntelic attachment). Hesperadin also causes cells arrested by taxol or monastrol to enter anaphase within <1 h, whereas cells in nocodazole stay arrested for 3-5 h^[3]. Hesperadin, an inhibitor of human Aurora B, prevented the phosphorylation of substrate with IC(50) of 40 nM. Hesperadin blocked nuclear division and cytokinesis but not other aspects of the cell cycle. Hesperadin provides neuroprotection against ICH (intracerebral hemorrhage) by inhibiting the MST4/AKT signaling pathway^[4]. Hesperadin induces delayed transition from metaphase to anaphase, and early exit from mitosis after chromosome segregation. In addition, micronuclei were observed frequently and lagging chromosomes, caused by the delay and failure of sister chromatid separation, were observed at anaphase and telophase in Hesperadin-treated BY-2 cells^[5]. Hesperadin inhibits multiple human clinical isolates of influenza A and B viruses with single to submicromolar efficacy, including oseltamivir-resistant strains. Mechanistic studies revealed that hesperadin inhibits the early stage of viral replication by delaying the nuclear entry of viral ribonucleoprotein complex, thereby inhibiting viral RNA transcription and translation as well as viral protein synthesis. Moreover, a combination of hesperadin with oseltamivir shows synergistic antiviral activity^[6].
细胞研究
Cell Data
Cell Lines Concentration Assay Type Time Activity Description Data Sources
HepG2 cells - Cytotoxicity assay 48 h Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, TC50=0.2 μM 24910766
参考文献

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HepG2 cells	-	Cytotoxicity assay	48 h	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, TC50=0.2 μM	24910766

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9355 mL
- 9.6776 mL
- 19.3553 mL
- 5 mM
- 0.3871 mL
- 1.9355 mL
- 3.8711 mL
- 10 mM
- 0.1936 mL
- 0.9678 mL
- 1.9355 mL

技术信息

CAS号

422513-13-1

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H32N4O3S

运输

蓝冰

分子量

516.65

别名

Hesperadin

溶解度

DMSO	210.0 mg/mL (406.5 mM)
Water	insoluble

动物实验配方

5% DMSO+40%PEG300+5% tween80+50% water

2.5 mg/mL

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