Importazole

製品コードS8446 バッチS844602

印刷

化学情報

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

61 mg/mL (191.57 mM)

Ethanol

7 mg/mL (21.98 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (15.70mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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.

溶剤液（一定の濃度）を調合する

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. This compound 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, this chemical 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].

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. This compound 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, this chemical 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. This compound 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.

参考

https://pubmed.ncbi.nlm.nih.gov/21469738/
https://pubmed.ncbi.nlm.nih.gov/23668205/

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：

Sphingosine simultaneously inhibits nuclear import and activates PP2A by binding importins and PPP2R1A [ EMBO J, 2025, 44(16):4473-4498]	PubMed: 40588551
N4BP1 is a nucleocytoplasmic shuttling protein and recognizes aggregates of the ubiquitin-like protein NEDD8 to protect cells under heat shock [ J Biol Chem, 2025, 301(9):110511]	PubMed: 40701250
Avermectins Inhibit Replication of Parvovirus B19 by Disrupting the Interaction Between Importin α and Non-Structural Protein 1 [ Viruses, 2025, 17(2)220]	PubMed: 40006975
Nuclear Lactate Dehydrogenase A Resists Cardiomyocyte Cell Cycle Arrest Induced by Oxidative Stress [ J Cardiovasc Dev Dis, 2025, 12(7)278]	PubMed: 40710803
Palmitoylated Importin α Regulates Mitotic Spindle Orientation Through Interaction with NuMA [ bioRxiv, 2025, 2024.10.25.620315]	PubMed: 39484393
Nucleocytoplasmic transport rates are regulated by cellular processes that modulate GTP availability [ J Cell Biol, 2024, 223(7)e202308152]	PubMed: 38683248
Ibetazol, a novel inhibitor of importin β1-mediated nuclear import [ Commun Biol, 2024, 7(1):1560]	PubMed: 39580542
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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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