p38 MAPK Inhibitor
Protein Kinase Inhibitor
For in vitro use only!
Shipping: shipped on blue ice
Storage Conditions: store at -20 °C
Shelf Life: 12 months
Molecular Formula: C21H16FN3OS
Molecular Weight: 377.43 g/mol
Purity: ≥ 98 %
Form: very light yellow crystalline solid
Solubility: 50 mg/ml soluble in DMSO.
SB203580 is a recognized inhibitor of p38-MAPKs. The IC50 for inhibition of p38-MAPK stimulation of MAPKAPK2 was approximately 0.07 μM, whereas that for total SAPK/JNK activity was 3-10 μM. SB203580 did not inhibit immunoprecipitated JNK1 isoforms.
The pyridinyl imidazole compounds were found to act as specific inhibitors of p38a and p38b but not p38g and p38d through competition with ATP for the same binding site on the p38 kinase.
SB203580 can inhibit the key cell cycle event of retinoblastoma protein phosphorylation in interleukin-2-stimulated T cells. Studies on the proximal regulator of this event, the phosphatidylinositol 3-kinase/protein kinase B (PKB)(Akt/Rac) kinase pathway, showed that SB203580 blocked the phosphorylation and activation of PKB by inhibiting the PKB kinase, phosphor-inositide-dependent protein kinase 1.
Kalmes et al. (1999) Raf-1 is activated by the p38 mitogen-activated protein kinase inhibitor SB203580. FEBS Lett. 444:71.
Lali et al. (2000) 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. 275:7395.
Clerk et al. (1998) The p38-MAPK inhibitor, SB203580, inhibits cardiac stress-activated protein kinases/c-Jun N-terminal kinases (SAPKs/JNKs). FEBS Lett. 426:93.
Wiener et al. (2008) IL-18 induces a marked gene expression profile change and increased Ccl1 (I-309) production in mouse mucosal mast cell homologs. International Immunology. 20 (12):1565-1573.
Cianciulli et al. (2009) f-Met-Leu-Phe Stimulates Nitric Oxide Production in Chick Embryo Neurons: The Role of NF-kB. Immunopharmacology and Immunotoxicology 31 (1):51-63.