GLPBio

Importazole

Catalog No.: GC19199Purity:>99.50%Synonyms: IPZ
COASDSData Sheet
Importazol ist ein niedermolekularer Inhibitor des Kerntransportrezeptors Importin-β.

Die Produkte sind ausschließlich für Forschungszwecke bestimmt. Nicht zur Anwendung am Menschen. Wir verkaufen nicht an Patienten.

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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Beschreibung (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.

Protokoll (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.

Produktdokumente (Product Documents)

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
662163-81-7
Synonyme
IPZ
SMILES
CC(NC1=C2C=CC=CC2=NC(N3CCCC3)=N1)C4=CC=CC=C4
Summenformel
C20H22N4
Molekulargewicht
318.42
Löslichkeit
DMSO : ≥ 33 mg/mL (103.64 mM)
Lagerung
Store at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

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