Importazole

Importazole is a small molecule inhibitor of the transport receptor importin-β (Karyopherin beta) specifically blocking importin-β-mediated nuclear import. Importazole induces apoptosis and inhibits tumor growth.

Importazole Chemical Structure

Importazole Chemical Structure

CAS No. 662163-81-7

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Importazole Related Products

Biological Activity

Description Importazole is a small molecule inhibitor of the transport receptor importin-β (Karyopherin beta) specifically blocking importin-β-mediated nuclear import. Importazole induces apoptosis and inhibits tumor growth.
Targets
importin-β [1]
In vitro
In vitro Importazole is an effective inhibitor of the Ran/importin-β interaction in vitro. 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. When added during mitosis, importazole impairs the release of an importin-β cargo FRET probe and causes both predicted and novel defects in spindle assembly[1]. It also inhibits proliferation and induces apoptosis of multiple myeloma cells by blocking the NF-κB signal pathway in vitro[2].
Cell Research Cell lines HEK 293 cells
Concentrations 40 μM
Incubation Time 1 h
Method For all import and export experiments, 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 calculated.
Experimental Result Images Methods Biomarkers Images PMID
Western blot Cyclin B1 / CDK1 / p-RCC1 / Cyclin D1 c-Myc 30742095

Chemical Information & Solubility

Molecular Weight 318.42 Formula

C20H22N4

CAS No. 662163-81-7 SDF Download Importazole SDF
Smiles CC(C1=CC=CC=C1)NC2=NC(=NC3=CC=CC=C32)N4CCCC4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 63 mg/mL ( (197.85 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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