Name | 4E2RCat |
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Synonyms |
5-{5-[(3-Benzyl-4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]-2-furyl}-2-chlorobenzoic acid
Benzoic acid, 2-chloro-5-[5-[[4-oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene]methyl]-2-furanyl]- |
Description | 4E2RCat is an inhibitor of eIF4E-eIF4G interaction with an IC50 of 13.5 μM. |
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Related Catalog | |
Target |
IC50: 13.5 μM (eIF4E-eIF4G)[1] |
In Vitro | 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]. |
In Vivo | 4E2RCat inhibits protein synthesis in vivo and it is not a consequence of increased cell death[1]. |
Cell Assay | 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 |
Density | 1.6±0.1 g/cm3 |
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Boiling Point | 659.0±65.0 °C at 760 mmHg |
Molecular Formula | C22H14ClNO4S2 |
Molecular Weight | 455.934 |
Flash Point | 352.3±34.3 °C |
Exact Mass | 455.005280 |
LogP | 5.09 |
Vapour Pressure | 0.0±2.1 mmHg at 25°C |
Index of Refraction | 1.760 |
Storage condition | 2-8℃ |