| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C21H16FN3O2S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
SB 203580 sulfone is an analog of the p38 MAP kinase inhibitor SB 203580. It inhibits IL-1 production, with an IC50 of 0.2 μM in monocytes, and binds competitively to CSAID-binding proteins (CSBP), inhibiting CSBP-mediated stress response signaling with an IC50 of 0.03 μM. It also inhibits 5-LO, with an IC50 of 24 μM, and can be used in research on inflammatory diseases[1][2]. It is supplied as an off-white to light yellow solid (C21H16FN3O2S, MW 393.43) at 99.25% purity.
Physical & Chemical Properties
| CAS Number | 152121-46-5 |
|---|---|
| Molecular Formula | C21H16FN3O2S |
| Molecular Weight | 393.43 g/mol |
| Purity | 99.25% |
| Appearance | Solid |
| Color | Off-white to light yellow |
| SMILES | O=S(C1=CC=C(C2=NC(C3=CC=C(F)C=C3)=C(C4=CC=NC=C4)N2)C=C1)(C)=O |
| Target | IL-1 |
| Signaling Pathway | Immunology/Inflammation; Metabolic Enzyme/Protease |
| Solubility | In Vitro: DMSO: 100 mg/mL (254.17 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) DMF: 50 mg/mL (127.09 mM; Requires sonication and warming) |
| Storage | Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
IL-1 0.2 μM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[2]. Timothy F, et al. 2,4,5- triarylimidazole inhibitors of IL-1 biosynthesis. Bioorganic & Medicinal Chemistry Letters, 1995, 1171-1176.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (254.17 mM) | requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility) |
| DMF | 50 mg/mL (127.09 mM) | requires sonication and warming |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 5 mg/mL (12.71 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 5 mg/mL (12.71 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 5 mg/mL (12.71 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
IL-1 production in monocytes is inhibited by SB 203580 sulfone, with an IC50 of 0.2 μM[1]. In an assay using semi-purified enzyme from RBL-1 cells, SB 203580 sulfone is an inhibitor of 5-LO, with an IC50 value of 24 μM[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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