Importazole (Synonyms: IPZ) |
Catalog No.GC19199
One-Click Copy Product Info
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Importazole, a small molecule inhibitor of the transport receptor importin-β, can be used to assess the function of the importin-β/RanGTP pathway at specific stages of the cell cycle.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 662163-81-7
Sample solution is provided at 25 µL, 10mM.
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Importazole, a small molecule inhibitor of the transport receptor importin-β, can be used to assess the function of the importin-β/RanGTP pathway at specific stages of the cell cycle[1].
In vitro, Importazole (10μM; 24h) treatment reduced the nuclear localization of IRF1 in Ca9-22 cells[2]. Blocking p85β nuclear translocation by Importazole enhances Alpelisib efficacy against PIK3CA-helical-domain-mutant tumors[3]. Inhibition of the nuclear transport protein Importin-β with Importazole (40µM; 4h) in MAC-T cells reduces ribotoxin-induced nuclear localization of IGFBP-3[4].
In vivo, Combination of Importazole (6.25mg/kg; 3 weeks; i.p.) and Alpelisib (p110α-specific inhibitor) significantly inhibited the growth of DLD1 cells, DLD1 xenograft tumors, and two patient-derived xenograft tumors harboring a PIK3CA E545K mutation[3]. Pharmacological inhibition of KPNB1 using the specific inhibitor Importazole (20mg/kg/3 times a week; 2 weeks; i.p.) significantly reduced tumor burden and prolonged survival in MLL-AF9-induced Acute myeloid leukemia (AML) mice[5].
References:
[1] Soderholm JF, Bird SL, Kalab P, et al. Importazole, a small molecule inhibitor of the transport receptor importin-β. ACS Chem Biol. 2011 Jul 15;6(7):700-8.
[2] Yoshino H, Sato Y, Nakano M. KPNB1 Inhibitor Importazole Reduces Ionizing Radiation-Increased Cell Surface PD-L1 Expression by Modulating Expression and Nuclear Import of IRF1. Curr Issues Mol Biol. 2021 May 19;43(1):153-162.
[3] He B, Li X, Yao M, et al. Blocking p85β nuclear translocation by importazole enhances Alpelisib efficacy against PIK3CA-helical-domain-mutant tumors. Biochem Biophys Res Commun. 2025 Feb 8;748:151324.
[4] Agostini-Dreyer A, Jetzt AE, Skorupa J, et al. IGFBP-3 Induced by Ribotoxic Stress Traffics From the Endoplasmic Reticulum to the Nucleus in Mammary Epithelial Cells. J Endocr Soc. 2018 Dec 24;3(3):517-536.
[5] Xie Y, Zhao R, Zheng Y, et al. Targeting KPNB1 suppresses AML cells by inhibiting HMGB2 nuclear import. Oncogene. 2025 Jun;44(21):1646-1661. doi: 10.1038/s41388-025-03340-0. Epub 2025 Mar 13.
| Cell experiment [1]: | |
Cell lines | Human HNSCC Ca9-22 cells |
Preparation Method | Cells were seeded onto glass slides, incubated for 6h, and then treated with Importazole (10μM; 24h) and/or X-ray irradiation (X-ray irradiation was performed at 1h after Importazole administration). The treated cells were fixed for 15min with 4% paraformaldehyde in Ca2+ and Mg2+-free PBS and then blocked with blocking buffer (3% bovine serum albumin (BSA)/0.3% Triton X-100 in PBS) for 60min at room temperature. The coverslips were then incubated overnight with IRF1 primary antibody diluted to 1:300 with antibody dilution buffer (1% BSA/0.3% Triton X-100 in PBS). After incubation, the samples were washed 3 times and incubated with AlexaFluor 488®-conjugated anti-rabbit IgG secondary antibody diluted to 1:400 with antibody dilution buffer for 1h at room temperature in the dark. After washing 3 times, the samples were mounted using Mounting Medium with DAPI and examined under an LSM 710 laser-scanning microscope. |
Reaction Conditions | 10μM; 24h |
Applications | Importazole treatment reduced the nuclear localization of IRF1 in Ca9-22 cells. |
| Animal experiment [2]: | |
Animal models | 6- weeks old female NON SCID mice |
Preparation Method | For xenograft animal models, Importazole was dissolved in the solvent solution containing 5% DMSO, 40% PEG-400, 5% Tween-80, and 50% H2O. Subcutaneous tumors were generated bilaterally with DLD1 cells or small pieces of PDX tumors (2×2 mm3). Once tumor sizes reached 100-150mm3, mice were randomly assigned into four groups (5 mice per group), including vehicle group, Alpelisib group (BYL719, 12.5mg/kg, oral gavage), Importazole group (IPZ, 6.25mg/kg, intraperitoneal injection), Alpelisib plus Importazole group. Mice were treated five times per week for 3 weeks. |
Dosage form | 6.25mg/kg; 3 weeks; i.p. |
Applications | Combination of Importazole and Alpelisib (p110α-specific inhibitor) significantly inhibited the growth of DLD1 cells, DLD1 xenograft tumors, and two patient-derived xenograft tumors harboring a PIK3CA E545K mutation. |
References: | |
| Cas No. | 662163-81-7 | SDF | |
| Synonyms | IPZ | ||
| Canonical SMILES | CC(NC1=C2C=CC=CC2=NC(N3CCCC3)=N1)C4=CC=CC=C4 | ||
| Formula | C20H22N4 | M.Wt | 318.42 |
| Solubility | DMSO : ≥ 33 mg/mL (103.64 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1405 mL | 15.7025 mL | 31.4051 mL |
| 5 mM | 628.1 μL | 3.1405 mL | 6.281 mL |
| 10 mM | 314.1 μL | 1.5703 mL | 3.1405 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)