158089-95-3
158089-95-3 structure
- Name: S-2474
- Chemical Name: 2,6-ditert-butyl-4-[(2-ethyl-1,1-dioxo-1,2-thiazolidin-5-ylidene)methyl]phenol
- CAS Number: 158089-95-3
- Molecular Formula: C20H31NO3S
- Molecular Weight: 365.53000
- Catalog: Signaling Pathways Metabolic Enzyme/Protease 5-Lipoxygenase
- Create Date: 2016-07-05 05:43:45
- Modify Date: 2024-01-09 17:53:29
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S-2474 is an inhibitor of COX-2 and 5-lipoxygenase, with IC50s of 11 nM and 27 μM for COX-2 and COX-1 in human intact cells, and used as a nonsteroidal anti-inflammatory drug.
| Name | 2,6-ditert-butyl-4-[(2-ethyl-1,1-dioxo-1,2-thiazolidin-5-ylidene)methyl]phenol |
|---|---|
| Synonyms |
phenol,2,6-bis(1,1-dimethylethyl)-4-[(e)-(2-ethyl-1,1-dioxido-5-isothiazolidinylidene)methyl]
S-2474 |
| Description | S-2474 is an inhibitor of COX-2 and 5-lipoxygenase, with IC50s of 11 nM and 27 μM for COX-2 and COX-1 in human intact cells, and used as a nonsteroidal anti-inflammatory drug. |
|---|---|
| Related Catalog | |
| Target |
COX-2:11 nM (IC50) COX-1:27 μM (IC50) 5-Lipoxygenase |
| In Vitro | S-2474 is an inhibitor of COX-2 and 5-lipoxygenase, with IC50s of 11 nM and 27 μM for COX-2 and COX-1[1]. S-2474 prevents neurons from Aβ-induced cell death significantly in a concentration-dependent manner (IC50 =26±12 nM). S-2474 (10 μM) completely inhibits Aβ(25-35)-induced neuronal cell death. S-2474 also shows neuroprotective effects in the Aβ(1-40)-induced neuronal cell death. S-2474 inhibits the PGD2 generation in a concentration dependent manner (IC50=69.8±21.9 nM). S-2474 (10 μM) lowers the elevated level of PGD2 significantly and reduces radicals from Aβ(25-35)-treated neurons[2]. S-2474 significantly prevents neurons from undergoing sPLA2-IIA-induced cell death. S-2474 completely ameliorates sPLA2-IIA-induced apoptotic features such as the condensation of chromatin and the fragmentation of DNA. Moreover, S-2474 significantly inhibits the sPLA2-IIA-induced generation of PGD2. S-2474 inhibits sPLA2-IIA-induced neuronal cell death in a concentration-dependent manner (IC50 = 94 nM)[3]. |
| Cell Assay | Experiments are principally performed in the two conditions as follows. (i) Neurons (2.5×105 cells/cm2) are treated with 10 μM Aβ(25-35) or Aβ(1-40) in the presence or absence of S-2474 at 37°C. Vehicle controls are treated with culture medium containing 1% deionized water and 0.1% DMSO. Aβ controls are treated with culture medium containing 10 μM Aβ(25-35) and 0.1% DMSO. (ii) Neurons (2.5×105 cells/cm2) are treated with eicosanoids at 37°C. Vehicle controls are treated with culture medium containing 0.1% ethanol. Two different methods are employed for assessment of neurotoxicity of Aβ. First, the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide dye (MTT) reduction assay reflecting mitochondrial succinate dehydrogenase activity is employed. Second, residual cells are counted according to morphologic criteria; neurons with intact neurites and a smooth, round soma are considered viable, whereas those with degenerated neurites and an irregular soma are considered nonviable. |
| References |
| Molecular Formula | C20H31NO3S |
|---|---|
| Molecular Weight | 365.53000 |
| Exact Mass | 365.20200 |
| PSA | 65.99000 |
| LogP | 5.40220 |
| Storage condition | 2-8℃ |