Ibetazol
Based on 1 Customer Validation
Ibetazol is a Importin β1 (KPNB1) inhibitor and nucleocytoplasmic transport disruptor. Ibetazol binds covalently to Cys585 of Importin β1, blocks both Importin β1-mediated direct transport and Importin α-dependent nuclear import processes, without affecting transport mediated by other nucleocytoplasmic transport proteins. Ibetazol induces cytoplasmic accumulation of Importin α1, and inhibits nuclear import of substrates carrying nuclear localization signals (NLS), including the NLS-cMyc reporter gene, RelA/p65 and SREBP1. Ibetazol triggers spindle malformation and chromosome misalignment by disrupting the mitotic function of Importin β1. Ibetazol inhibits the proliferation of cells expressing wild-type Importin β1. Ibetazol has a high activity-cytotoxicity window, lacks intrinsic fluorescence, and acts rapidly on nucleocytoplasmic transport processes. Ibetazol serves as a tool compound for investigating nuclear import processes specifically mediated by Importin β1.
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- Purity: 99.8%
- 화학식: C13H11F3N2OS
- 분자량:300.30
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
Ibetazol (0.01-100 μM; 2 h) induces cytoplasmic relocalization of importin α1-mNeonGreen in HeLa Kyoto cells with an EC50 of 6.1 ± 1.9 μM, indicating inhibition of importin β1-mediated nuclear import[1].
Ibetazol (0.01-100 μM; 2 h) inhibits importin β1/importin α-dependent nuclear import of the NLS(cMyc)-AcGFPx2 reporter in HeLa Kyoto cells[1].
Ibetazol (0.01-100 μM; 3 h) inhibits direct importin β1-dependent nuclear import of SREBP1 in HeLa Kyoto cells[1].
Ibetazol (50 μM; 2 h) induces cytoplasmic relocalization of importin α1 in HAP1 cells, and this requires a functional Cys585 residue on importin β1, confirming Cys585 as the binding site[1].
Ibetazol (50 μM; 1 h during mitotic synchronization and release) impairs mitotic spindle formation and chromosome alignment in synchronized HeLa Kyoto cells, consistent with inhibition of importin β1-mediated mitotic functions[1].
Ibetazol (up to 60 μM; 24 h) is non-cytotoxic to HEK293T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HAP1 cells (wild-type, importin β1₍C392A₎, importin β1₍C543A₎, importin β1₍C585A₎, and control silent mutant lines)
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Concentration:Serial dilutions
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Incubation Time:48 h
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Result:Inhibited proliferation of wild-type and importin β1₍C392A₎/importin β1₍C543A₎ mutant HAP1 cells with an IC50 of ~6 μM (6.7 μM for importin β1₍C392A₎, 5.1 μM for importin β1₍C543A₎).
Inhibited proliferation of importin β1₍C585A₎ mutant cells with a significantly higher IC50 of 11.8 μM.
Chemical Information
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Appearance Solid
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분자량 300.30
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화학식 C13H11F3N2OS
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Color White to off-white
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SMILES
FC(F)(F)C1=CC(C2=CC=CC=C2)=NC(S(CC)=O)=N1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 10 mg/mL (33.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 1 mg/mL (3.33 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (3.33 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
순도&문서
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3300 mL | 16.6500 mL | 33.3000 mL | 83.2501 mL |
| 5 mM | 0.6660 mL | 3.3300 mL | 6.6600 mL | 16.6500 mL | |
| 10 mM | 0.3330 mL | 1.6650 mL | 3.3300 mL | 8.3250 mL | |
| 15 mM | 0.2220 mL | 1.1100 mL | 2.2200 mL | 5.5500 mL | |
| 20 mM | 0.1665 mL | 0.8325 mL | 1.6650 mL | 4.1625 mL | |
| 25 mM | 0.1332 mL | 0.6660 mL | 1.3320 mL | 3.3300 mL | |
| 30 mM | 0.1110 mL | 0.5550 mL | 1.1100 mL | 2.7750 mL |
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