Biological Activity
Selective inhibitor of p38 MAPK (IC50 values are 50 and 500 nM for SAPK2a/p38 and SAPK2b/p38β2 respectively). Displays 100-500-fold selectivity over LCK, GSK-3β and PKBα. Shown to inhibit IL-2-induced T cell proliferation, cyclooxygenase-1 and -2, and thromboxane synthase. Enhances clonal growth of skin epithelial progenitor cells; stimulates neural stem cell (NSC) proliferation. Essential component of medium for maintaining stem cells in naive pluripotent state. Part of the MAPK Cascade Inhibitor Tocriset™ and MAPK Inhibitor Tocriset™. Water-soluble salt SB 203580 hydrochloride (Cat. No. 1402) also available.
Licensing Information
Sold with the permission of GlaxoSmithKline
Compound Libraries
SB 203580 is also offered as part of the Tocriscreen Plus and Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 377.44 |
| Formula | C21H16FN3OS |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 152121-47-6 |
| PubChem ID | 176155 |
| InChI Key | CDMGBJANTYXAIV-UHFFFAOYSA-N |
| Smiles | CS(=O)C1=CC=C(C=C1)C1=NC(=C(N1)C1=CC=NC=C1)C1=CC=C(F)C=C1 |
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 | |||
| 1eq. HCl | 37.74 | 100 | |
| DMSO | 9.44 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 377.44. 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 | 2.65 mL | 13.25 mL | 26.49 mL |
| 5 mM | 0.53 mL | 2.65 mL | 5.3 mL |
| 10 mM | 0.26 mL | 1.32 mL | 2.65 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Borsch-Haubold et al (1998) Direct inhibition of cyclooxygenase-1 and -2 by the kinase inhibitors SB 203580 and PD 98059. J.Biol.Chem. 273 28766 PMID: 9786874
Davies et al (2000) Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem.J. 351 95 PMID: 10998351
Saklatvala et al (1996) Role for p38 mitogen-activated protein kinase in platelet aggregation caused by collagen on a thromboxane analogue. J.Biol.Chem. 271 6586 PMID: 8636072
Sato et al (2008) Inhibitors of p38 mitogen-activated protein kinase enhance proliferation of mouse neural stem cells. J.Neurosci.Res. 86 2179 PMID: 18338804
Gafni et al (2013) Derivation of novel human ground state naive pluripotent stem cells. Nature 504 282 PMID: 24172903
Keywords: SB 203580, supplier, Selective, inhibitors, inhibits, p38, MAPK, Mitogen-Activated, Protein, Kinases, Signaling, Signalling, SB203580, GlaxoSmithKline, GSK, p38, Stem, Cell, Proliferation, p38, Tocris Bioscience
