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Importazole

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Chemical Structure| 662163-81-7 同义名 : IPZ
CAS号 : 662163-81-7
货号 : A528010
分子式 : C20H22N4
纯度 : 99%+
分子量 : 318.416
MDL号 : MFCD04077630
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(109.92 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The transport receptor importin-β carries cargoes into the nucleus during interphase. Importazole is a selective Importin-β inhibitor. Importazole at concentration of 50μM specifically binds to importin-β, but not RanQ69L, transportin and CRM1. Importazole at concentration of 100μM could inhibit importin-β NLS (importin-β import substrate)-mediated nuclear import without effect on transportin M9-mediated import. Importazole impaired spindle assembly and disrupted mitotic cargo release and mitotic spindles. Treatment with 12μM Importazole could decrease TNF-α-induced p65 nuclear import and suppressed the expression of NF-κB target gene BCL2, c-IAP1 and XIAP in NCI-H929 and RPMI-8226 cells.
作用机制 Importazole specifically binds to importin-β and alters its interaction with RanGTP.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.14mL

0.63mL

0.31mL

15.70mL

3.14mL

1.57mL

31.41mL

6.28mL

3.14mL
参考文献

[1]Soderholm JF, Bird SL, et al. Importazole, a small molecule inhibitor of the transport receptor importin-β. ACS Chem Biol. 2011 Jul 15;6(7):700-8.

[2]Yan W, Li R, et al. Importin β1 mediates nuclear factor-κB signal transduction into the nuclei of myeloma cells and affects their proliferation and apoptosis. Cell Signal. 2015 Apr;27(4):851-9.