Importazole is a small molecule inhibitor of the nuclear transport receptor importin-β.

Importazole specifically blocks importin-β-mediated nuclear import both in Xenopus egg extracts and cultured cells, without disrupting transportin-mediated nuclear import or CRM1-mediated nuclear export. Importazole impairs the release of an importin-β cargo FRET probe and causes both predicted and novel defects in spindle assembly^[1]. Importazole displays an IC₅₀ of approximately 15 μM for inhibition of NFAT-GFP import. Importazole has an IC₅₀ of approximately 22.5 μM in HeLa cells following treatment over a 24-hour period^[1]. Importazole induces a dose-and time-dependent inhibition of myeloma cells growth. And the IC₅₀ values of importazole on RPMI 8226 and NCI-H929 after 48 hours incubation are (4.43±0.41) and (4.78±0.35) μmol/L, respectively. Treatment of RPMI 8226 and NCI-H929 cells with 8 μmol/L importazole for 24 h could inhibit NF-κB import to nucleus and reduce its DNA binding activity^[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.

318.42

C₂₀H₂₂N₄

662163-81-7

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : ≥ 33 mg/mL (103.64 mM)

* “≥” means soluble, but saturation unknown.

*

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• 1.

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

  Solubility: ≥ 2.5 mg/mL (7.85 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.85 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。

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• 2.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (7.85 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.85 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。

• [1]. Soderholm JF, 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 WQ, et al. Effect of nuclear receptor inhibitor importazole on the proliferation and apoptosis of multiple myeloma cells. Zhonghua Xue Ye Xue Za Zhi. 2013 Apr;34(4):323-6.

HEK 293 cells stably expressing NFAT-GFP are grown on glass coverslips to approximately 50% confluency prior to drug treatment. In all cases, importazole is used at 40 μM and leptomycin B is used at 10 ng/mL. For controls, DMSO is used at a concentration of 0.4%. Ionomycin is added at 1.25 μM. Importazole and leptomycin B treatments are all for 1 hour. In all experiments cells are fixed with 4% formaldehyde prior to fluorescence microscopy. DNA is visualized with 1 μg/mL Hoechst dye. For quantification, 100 cells from each condition are analyzed and the percentage that shows nuclear accumulation of NFAT-GFP are calculated^[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.

• [1]. Soderholm JF, 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 WQ, et al. Effect of nuclear receptor inhibitor importazole on the proliferation and apoptosis of multiple myeloma cells. Zhonghua Xue Ye Xue Za Zhi. 2013 Apr;34(4):323-6.