Importazole
Based on 16 publication(s) in Google Scholar
Importazole is a small molecule inhibitor of the nuclear transport receptor importin-β.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.89%
- CAS No.: 662163-81-7
- Formule: C20H22N4
- Masse moléculaire:318.42
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) Importazole
More- Nature. 2025 Jan;637(8044):215-223. [Abstract]
- Nature. 2018 Nov;563(7729):131-136. [Abstract]
- Cell Death Discov. 2024 Oct 26;10(1):453. [Abstract]
- Proc Natl Acad Sci U S A. 2026 Feb 24;123(8):e2528243123. [Abstract]
- Cell Rep. 2026 Jan 22;45(2):116858. [Abstract]
- EMBO Rep. 2019 Jun;20(6):e47283. [Abstract]
- J Cell Mol Med. 2022 Apr;26(7):2089-2103. [Abstract]
- PLoS One. 2020 Nov 12;15(11):e0242312. [Abstract]
- Onco Targets Ther. 2019 Dec 2:12:10455-10467. [Abstract]
- Genes Cells. 2024 Oct;29(10):820-837. [Abstract]
- Technical University of Munich. 2025.
- bioRxiv. 2025 Aug 15.
- bioRxiv. 2025 March 19.
- bioRxiv. 2025 January 14.
- Heliyon. 2024 Jun 28;10(13):e33904. [Abstract]
- SSRN. 5 Dec 2022.
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Activité biologique
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 662163-81-7
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Appearance Solid
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Masse moléculaire 318.42
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Formule C20H22N4
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Color White to off-white
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SMILES
CC(NC1=C2C=CC=CC2=NC(N3CCCC3)=N1)C4=CC=CC=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (16)
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Journal Impact Factor
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Most Recent
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Nature
2025 Jan;637(8044):215-223. PMID: 39567688 -
Nature
2018 Nov;563(7729):131-136. PMID: 30356214
Importazole purchased from MedChemExpress. Usage Cited in: Nature. 2018 Nov;563(7729):131-136. [Abstract]
The inhibition of importin-β by Importazole significantly reduces the nuclear translocation of cGAS induced by DNA damage.
Importazole purchased from MedChemExpress. Usage Cited in: Nature. 2018 Nov;563(7729):131-136. [Abstract]
The inhibition of importin-β by Importazole significantly reduces the nuclear translocation of cGAS induced by DNA damage.
Importazole purchased from MedChemExpress. Usage Cited in: Nature. 2018 Nov;563(7729):131-136. [Abstract]
The inhibition of importin-β by Importazole significantly reduces the nuclear translocation of cGAS induced by DNA damage.
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Cell Death Discov
CDK4/6 inhibition initiates cell cycle arrest by nuclear translocation of RB and induces a multistep molecular response. [Abstract]2024 Oct 26;10(1):453. PMID: 39461947 -
Proc Natl Acad Sci U S A
2026 Feb 24;123(8):e2528243123. PMID: 41712636 -
Cell Rep
Extracellular matrix stiffness drives post-mitotic nuclear pore complex assembly to promote neuroblastoma pathogenesis. [Abstract]2026 Jan 22;45(2):116858. PMID: 41575851 -
EMBO Rep
The nucleoporin ELYS regulates nuclear size by controlling NPC number and nuclear import capacity. [Abstract]2019 Jun;20(6):e47283. PMID: 31085625 -
J Cell Mol Med
CD44/ERM/F-actin complex mediates targeted nuclear degranulation and excessive neutrophil extracellular trap formation during sepsis. [Abstract]2022 Apr;26(7):2089-2103. PMID: 35146909 -
PLoS One
Identification of a non-classical three-dimensional nuclear localization signal in the intestinal fatty acid binding protein. [Abstract]2020 Nov 12;15(11):e0242312. PMID: 33180886 -
Onco Targets Ther
Inhibition of KPNB1 Inhibits Proliferation and Promotes Apoptosis of Chronic Myeloid Leukemia Cells Through Regulation of E2F1. [Abstract]2019 Dec 2:12:10455-10467. PMID: 31819526
Importazole purchased from MedChemExpress. Usage Cited in: Onco Targets Ther. 2019 Dec 2:12:10455-10467. [Abstract]
Western analysis of the expressions of KPNB1 and KPNA2 in K562 and K562R cells with the treatment of Importazole (IM: 10μM) for 48 hrs.
Western analysis of the expressions of KPNB1 and KPNA2 in 293T cells which transfected with pAdTrack-Bcr-Abl with the treatment of Importazole (IM: 10μM) for 48 hrs. -
Genes Cells
Reconstruction of artificial nuclei with nuclear import activity in living mouse oocytes. [Abstract]2024 Oct;29(10):820-837. PMID: 39140385 -
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Heliyon
Astragaloside Ⅳ mediates the effect and mechanism of KPNB1 on biological behavior and tumor growth in prostate cancer. [Abstract]2024 Jun 28;10(13):e33904. PMID: 39027542 -
Solvant et solubilité
DMSO : ≥ 33 mg/mL (103.64 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.85 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1405 mL | 15.7025 mL | 31.4051 mL | 78.5127 mL |
| 5 mM | 0.6281 mL | 3.1405 mL | 6.2810 mL | 15.7025 mL | |
| 10 mM | 0.3141 mL | 1.5703 mL | 3.1405 mL | 7.8513 mL | |
| 15 mM | 0.2094 mL | 1.0468 mL | 2.0937 mL | 5.2342 mL | |
| 20 mM | 0.1570 mL | 0.7851 mL | 1.5703 mL | 3.9256 mL | |
| 25 mM | 0.1256 mL | 0.6281 mL | 1.2562 mL | 3.1405 mL | |
| 30 mM | 0.1047 mL | 0.5234 mL | 1.0468 mL | 2.6171 mL | |
| 40 mM | 0.0785 mL | 0.3926 mL | 0.7851 mL | 1.9628 mL | |
| 50 mM | 0.0628 mL | 0.3141 mL | 0.6281 mL | 1.5703 mL | |
| 60 mM | 0.0523 mL | 0.2617 mL | 0.5234 mL | 1.3085 mL | |
| 80 mM | 0.0393 mL | 0.1963 mL | 0.3926 mL | 0.9814 mL | |
| 100 mM | 0.0314 mL | 0.1570 mL | 0.3141 mL | 0.7851 mL |
Importazole Related Classifications
HY-101091 Related Classifications
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