GLPBio

Importazole

Catalog No.: GC19199Purity:>99.50%Synonyms: IPZ
COASDSData Sheet
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.

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Importazole
Cas No.: 662163-81-7
5mgIn Stock
$37.00
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10mgIn Stock
$50.00
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25mgIn Stock
$110.00
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50mgIn Stock
$200.00
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100mgIn Stock
$362.00
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Description

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.

Protocol

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:
[1] 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.
[2] He B, Li X, Yao M, et al. Blocking p85? nuclear translocation by importazole enhances Alpelisib efficacy against PIK3CA-helical-domain-mutant tumors. Biochem Biophys Res Commun. 2025 Feb 8;748:151324.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
662163-81-7
Synonyms
IPZ
SMILES
CC(NC1=C2C=CC=CC2=NC(N3CCCC3)=N1)C4=CC=CC=C4
Molecular Formula
C20H22N4
Molecular Weight
318.42
Solubility
DMSO : ≥ 33 mg/mL (103.64 mM)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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