SB203580 is a pyridinylimidazole-based inhibitor of p38-MAPK at an IC50 of 0.3-0.5 uM. [1] It also inhibits PKB phosphorylation at an IC50 of 3-5 uM and blocks the key cell cycle event of retinoblastoma protein phosphorylation in IL-2-stimulated T-cells. SB203580 was found to inhibit the activation of p70S6K, but at a location downstream of PI3K. [1]
Independent studies indicate at concentrations of 10 uM, SB203580 activates phosphorylation of ERK1/2 and JNK, which in turn may activate gene transcription regulated by NF-kB. [2] Similarly, SB203580 was shown to stimulate the phosphorylation and activation of cPLA2, CAMKIIa and arachidonic acid release. [3]
In an L1210 mouse leukemic cell line resistant to vincristine, SB203580 is believed to play a role in the reversal of Pgp-mediated multidrug resistance. [4]
Technical information:
| Chemical Formula: | C21H16FN3OS | |
| CAS #: | 152121-47-6 | |
| Molecular Weight: | 377.43 | |
| Purity: | >98% | |
| Appearance: | White | |
| Chemical Name: | 4-(4-(4-fluorophenyl)-2-(4-(methylsulfinyl)phenyl)-1H-imidazol-5-yl)pyridine | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | SB-203580, SB 203580, SB203580 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Lali et al., The pyridinyl imidazole inhibitor SB203580 blocks phosphoinositide-dependent protein kinase activity, protein kinase B phosphorylation, and retinoblastoma hyperphosphorylation in interleukin-2-stimulated T cells independently of p38 mitogen-activated protein kinase. J. Biol. Chem. 2000, 275(10), 7395-7402. Pubmed ID: 10702313 |
| 2. | Birkenkamp et al., The p38 MAP kinase inhibitor SB203580 enhances nuclear factor-kappa B transcriptional activity by a non-specific effect upon the ERK pathway. Br. J. Pharmacol. 2000, 131, 99-107. Pubmed ID: 10960075 |
| 3. | Fatima et al., Cytosolic phospholipase A2 activation by the p38 kinase inhibitor SB203580 in rabbit aortic smooth muscle cells. J. Pharmacol. Exp. Ther. 2001, 298(1), 331-338. Pubmed ID: 11408559 |
| 4. | Barancik et al., SB203580, a specific inhibitor of p38-MAPK pathway, is a new reversal agent of P-glycoprotein-mediated multidrug resistance. Eur. J. Pharmaceut. Sci. 2001, 14, 29-36. Pubmed ID: 10960075 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
