Importazole is a small molecule inhibitor of the nuclear transport receptor importin-β.
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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] |
Dose | Mice: 100 mg/kg[3] (i.p.) |
Administration | i.p. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 662163-81-7 |
分子式 | C20H22N4 |
分子量 | 318.416 |
别名 | IPZ |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,2-8°C |
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 |