2. Apoptosis
  3. Apoptosis
  4. Importazole

Importazole is a small molecule inhibitor of the nuclear transport receptor importin-β.

For research use only. We do not sell to patients.

Importazole Chemical Structure

Importazole Chemical Structure

CAS No. : 662163-81-7

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10 mM * 1 mL in DMSO
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Customer Review

Based on 12 publication(s) in Google Scholar

Importazole Related Antibodies

Top Publications Citing Use of Products

    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.

    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.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Importazole is a small molecule inhibitor of the nuclear transport receptor importin-β.

    In Vitro

    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.

    Importazole Related Antibodies
    Molecular Weight

    318.42

    Formula

    C20H22N4
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC(NC1=C2C=CC=CC2=NC(N3CCCC3)=N1)C4=CC=CC=C4
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    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.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.1405 mL 15.7025 mL 31.4051 mL
    5 mM 0.6281 mL 3.1405 mL 6.2810 mL
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    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.

    • Protocol 1

      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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (7.85 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: 99.99%

    COA (251 KB) LCMS (260 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    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
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    Importazole Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Importazole662163-81-7ApoptosisInhibitorinhibitorinhibit

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