4E2RCat |
| رقم الكتالوجGC30785 |
4E2RCat هو مثبط لتفاعل eIF4E-eIF4G بتركيز IC50 يبلغ 13.5 ميكرومولار.
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Cas No.: 432499-63-3
Sample solution is provided at 25 µL, 10mM.
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4E2RCat is an inhibitor of eIF4E-eIF4G interaction with an IC50 of 13.5 μM.
4E2RCat prevents the interaction between eIF4E (the cap-binding protein) and eIF4G (a large scaffolding protein), inhibiting cap-dependent translation. It significantly decreases human coronavirus 229E (HCoV-229E) replication, reducing the percentage of infected cells and intra- and extracellular infectious virus titers. 4E2RCat inhibits cap-dependent translation in a dose-dependent manner. 4E2RCat inhibits cap-dependent FF translation but not EMCV IRES-driven Ren translation. 4E2RCat inhibits coronavirus replication in a dose- and time-dependent manner[1].
4E2RCat inhibits protein synthesis in vivo and it is not a consequence of increased cell death[1].
[1]. Cencic R, et al. Blocking eIF4E-eIF4G interaction as a strategy to impair coronavirus replication. J Virol. 2011 Jul;85(13):6381-9.
Cell experiment: | L132 cells are treated with 12.5 μM 4E2RCat for the indicated times and are processed for annexin V/propidium iodide staining. To this end, cell medium is collected. Cells are ished with 1 mL PBS, which is collected as well, and trypsinized in 200 μL 0.05% trypsin-EDTA. Cells are pooled with previously collected supernatants and spun for 2 min at 2,000 rpm and 4°C. The cell pellet is ished with 2 mL cold PBS, followed by another spin. After the second spin, the cell pellet is resuspended in 100 μL annexin V binding buffer and propidium iodide added to a final concentration of 5 μg/mL. After the addition of 5 μL annexin V-fluorescein isothiocyanate, samples are incubated for 15 min in the dark at room temperature and diluted. Fluorescence-activated cell sorter (FACS) analyses are performed using a FACScan instrument[1]. |
References: [1]. Cencic R, et al. Blocking eIF4E-eIF4G interaction as a strategy to impair coronavirus replication. J Virol. 2011 Jul;85(13):6381-9. | |
| Cas No. | 432499-63-3 | SDF | |
| Canonical SMILES | O=C(O)C1=CC(C2=CC=C(/C=C(SC(N3CC4=CC=CC=C4)=S)/C3=O)O2)=CC=C1Cl | ||
| Formula | C22H14ClNO4S2 | M.Wt | 455.93 |
| الذوبان | DMSO : 15.5 mg/mL (34.00 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1933 mL | 10.9666 mL | 21.9332 mL |
| 5 mM | 0.4387 mL | 2.1933 mL | 4.3866 mL |
| 10 mM | 0.2193 mL | 1.0967 mL | 2.1933 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
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