Importazole

Catalog No.S8446 Batch:S844601

Technical Data

Formula	C₂₀H₂₂N₄
Molecular Weight	318.42	CAS No.	662163-81-7
Solubility (25°C)*	In vitro	DMSO	63 mg/mL (197.85 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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].

Protocol (from reference)

Cell Assay:^{^[1]}	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.

Cell Assay:^{^[1]}

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.

References

Customer Product Validation

: Data from [Data independently produced by , , Cell, 2018, 174(5):1200-1215]

Selleck's Importazole has been cited by 11 publications

Nuclear translocation of cGAS orchestrates VEGF-A-mediated angiogenesis [ Cell Reports, 2023, 112328]	PubMed: None
Nuclear translocation of cGAS orchestrates VEGF-A-mediated angiogenesis [ Cell Rep, 2023, 42(4):112328]	PubMed: 37027305
Nucleocytoplasmic transport rates are regulated by cellular processes that modulate GTP availability [ bioRxiv, 2023, 2023.12.29.573651]	PubMed: 38234722
The transcriptional coactivator RUVBL2 regulates Pol II clustering with diverse transcription factors [ Nat Commun, 2022, 13(1):5703]	PubMed: 36171202
ORAI1-Regulated Gene Expression in Breast Cancer Cells: Roles for STIM1 Binding, Calcium Influx and Transcription Factor Translocation [ Int J Mol Sci, 2022, 23(11)5867]	PubMed: 35682546
Effects of Ran-GTP/importin β inhibition on the meiotic division of porcine oocytes [ Histochem Cell Biol, 2022, 10.1007/s00418-022-02134-9]	PubMed: 35930054
Nucleocytoplasmic Shuttling of Porcine Parvovirus NS1 Protein Mediated by the CRM1 Nuclear Export Pathway and the Importin α/β Nuclear Import Pathway [ J Virol, 2021, JVI0148121]	PubMed: 34643426
Inhibition of Karyopherin beta 1 suppresses prostate cancer growth [ Oncogene, 2019, 38(24):4700-4714]	PubMed: 30742095
C9orf72-generated poly-GR and poly-PR do not directly interfere with nucleocytoplasmic transport [ Sci Rep, 2019, 9(1):15728]	PubMed: 31673013
Nuclear Pores Promote Lethal Prostate Cancer by Increasing POM121-Driven E2F1, MYC, and AR Nuclear Import [Rodriguez-Bravo V, et al. Cell, 2018, 174(5):1200-1215]	PubMed: 30100187

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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