Sb-203580

DescriptionSB 203580 (152121-47-6) is a potent and selective inhibitor of p38 MAP kinase, IC50=50 and 500 nM for p38 and p38β2 respectively.1 No other kinases (in a panel of 30) were significantly inhibited including p38γ and δ at 10 μM.2A potent inhibitor of inflammatory cytokine production (IC50=15-25 mg/kg in mice and rats) in animal models of arthritis, bone resorption, endotoxin shock and immune function.3

UsesA pyridinyl imidazole which acts as a specific inhibitor of p38 MAP kinase. Does not inhibit the MAP kinase homologs JNK and p42 MAP kinase

UsesA p38 MAPK inhibitor with an IC50 range of 0.3-0.5 μM and blocks PKB phosphorylation with an IC50 range of 3-5 μM.

UsesMDCK cells were treated with SB 203580 to study the role of MAPK signaling in inducing hypertonicity of cell membrane and potassium depletion.16 It was used to inhibit MAPK signaling in mouse cortical neurons17 and human hepatocellular carcinoma cell lines.18

General DescriptionReduces epirubicin-induced cell injury and caspase-3/7 activity. A highly specific, potent, cell-permeable, selective, reversible, and ATP-competitive inhibitor of p38 kinase (IC50 = 34 nM in vitro, 600 nM in cells). Also known as reactivating kinase (RK) and CSBP (cytokine synthesis anti-inflammatory drug binding protein). Does not significantly inhibit JNK or p42 MAP kinase even at 100 μM. Inhibits IL-1 and TNF-α production from LPS-stimulated human monocytes and the human monocyte cell line THP-1 (IC50 = 50-100 nM). SB 203580 has also been shown to be an effective inhibitor of inflammatory cytokine production in vivo in both mice and rats.