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| 25mg |
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| 50mg |
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Purity: ≥98%
Importazole is a 2,4-diaminoquinazoline that was found in a high-throughput small molecule screen for FRET-based compounds that interfere with the interaction between importin-β and RanGTP. Importazole is a small molecule inhibitor of the transport receptor importin-β that specifically prevents importin-β-mediated nuclear import. In vitro, it is a potent importin-β/Ran interaction inhibitor. Importazole specifically prevents importin-β-mediated nuclear import from occurring in both Xenopus egg extracts and cultured cells, while leaving transportin- and CRM1-mediated nuclear import and export unaffected. Importazole interferes with the release of an importin-β-cargo FRET probe and leads to both anticipated and unanticipated defects in spindle assembly when added during mitosis. Importazole is a useful tool for assessing the role of the importin-β-/RanGTP pathway at particular cell cycle stages.
| Targets |
importin-β
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| ln Vitro |
In vitro, importazole is a potent inhibitor of the Ran/importin-β interaction. Importazole specifically prevents importin-β-mediated nuclear import from occurring in both Xenopus egg extracts and cultured cells, without disrupting transportin-mediated nuclear import or CRM1-mediated nuclear export. Importazole interferes with the release of an importin-β cargo FRET probe and leads to both anticipated and unanticipated defects in spindle assembly when added during mitosis[1]. By blocking the NF-κB signal pathway in vitro, it also prevents multiple myeloma cells from proliferating and causes them to undergo apoptosis[2].
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| ln Vivo |
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| Enzyme Assay |
Importazole, a 2,4-diaminoquinazoline identified from a FRET-based, high-throughput small molecule screen for compounds that interfere with the interaction between RanGTP and importin-β, is a small molecule inhibitor of the transport receptor importin-β that specifically blocks importin-β-mediated nuclear import. It is an effective inhibitor of the Ran/importin-β interaction in vitro.
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| Cell Assay |
HEK 293 cells stably expressing NFAT-GFP are grown on glass coverslips to approximately 50% confluency prior to drug treatment. Leptomycin B is administered at 10 ng/mL and importazole is always used at a concentration of 40 M. A 0.4% concentration of DMSO is used as a control. 1.25 μM of ionomycin is added. Treatments with importazole and leptomycin B last an hour each. Prior to fluorescence microscopy, cells are fixed with 4% formaldehyde in all experiments. With 1 g/mL Hoechst dye, DNA is seen. The percentage of 100 cells from each condition that exhibit nuclear accumulation of NFAT-GFP is calculated[1] for quantification.
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| References |
| Molecular Formula |
C20H22N4
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| Molecular Weight |
318.42
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| Exact Mass |
318.1844
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| Elemental Analysis |
C, 75.44; H, 6.96; N, 17.60
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| CAS # |
662163-81-7
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| Related CAS # |
662163-81-7;Importazole HCl;
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| Appearance |
Solid powder
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| SMILES |
CC(C1=CC=CC=C1)NC2=NC(=NC3=CC=CC=C32)N4CCCC4
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| InChi Key |
HKGJEZIGDHFJFL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H22N4/c1-15(16-9-3-2-4-10-16)21-19-17-11-5-6-12-18(17)22-20(23-19)24-13-7-8-14-24/h2-6,9-12,15H,7-8,13-14H2,1H3,(H,21,22,23)
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| Chemical Name |
N-(1-phenylethyl)-2-pyrrolidin-1-ylquinazolin-4-amine
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.85 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.3141 mL | 1.5703 mL | 3.1405 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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