Importazole

製品コードS8446 バッチS844603

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H22N4
分子量 318.42 CAS No. 662163-81-7
Solubility (25°C)* 体外 DMSO 64 mg/mL (200.99 mM)
Ethanol 16 mg/mL (50.24 mM)
Water 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.

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生物活性

製品説明 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.
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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HEK 293 cells
濃度 40 μM
反応時間 1 h
実験の流れ 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.

カスタマーフィードバック

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

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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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