Biological Activity
Potent and selective p38 MAP kinase inhibitor (IC50 = 44 nM for p38α). Displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580 (Cat. Nos. 1202 and 1402). Reduces inflammatory cytokine production and is neuroprotective following oral administration in vivo.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Technical Data
| M. Wt | 368.41 |
| Formula | C20H21FN4O2 |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 193551-21-2 |
| PubChem ID | 5166 |
| InChI Key | ZQUSFAUAYSEREK-UHFFFAOYSA-N |
| Smiles | O[C@@H]1CC[C@@H](N2C=NC(C4=CC=C(F)C=C4)=C2C3=CC=NC(OC)=N3)CC1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 3.68 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 368.41. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.71 mL | 13.57 mL | 27.14 mL |
| 5 mM | 0.54 mL | 2.71 mL | 5.43 mL |
| 10 mM | 0.27 mL | 1.36 mL | 2.71 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Barone et al (2001) SB 239063, a second-generation p38 mitogen-activated protein kinase inhibitor, reduces brain injury and neurological deficits in cerebral focal ischemia. J.Pharmacol.Exp.Ther. 296 312 PMID: 11160612
Legos et al (2002) The selective p38 inhibitor SB-239063 protects primary neurons from mild to moderate excitotoxic injury. Eur.J.Pharmacol. 447 37 PMID: 12106800
Underwood et al (2000) SB 239063, a potent p38 MAP kinase inhibitor, reduces inflammatory cytokine production, airways eosinophil infiltration, and persistence. J.Pharmacol.Exp.Ther. 293 281 PMID: 10734180
Keywords: SB 239063, supplier, Potent, selective, p38, MAP, kinases, inhibitors, inhibits, orally, active, MAPK, Signaling, Signalling, Mitogen-Activated, Protein, SB239063, GlaxoSmithKline, GSK, p38, p38, Tocris Bioscience
