SB-242235 is a potent and selective p38 MAP kinase inhibitor, with an IC 50 of 1.0u3000μM in primary human chondrocytes.
Storage Temp
Store at -80°C
Shipped In
Ice chest + Ice pads
Product Description
SB-242235 is a potent and selective p38 MAP kinase inhibitor, with an IC 50 of 1.0 μM in primary human chondrocytes
In Vitro
SB 242235 (0-10 μM) dose-dependently inhibits the activation of MAPKAP K2 with an IC 50 of 1.0 μM in human chondrocytes stimulated with IL-1β. SB 242235 inhibits intracellular p38 activity, MAPKAP K2 was then isolated from these cells and assayed using HSP27 as a substrate. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: Human chondrocytes Concentration: 0 μM,0.01 μM,0.1 μM,1 μM,10 μM Incubation Time: 15 minutes Result: Dose-dependently inhibited the activation of MAPKAP K2 with an IC 50 of 1.0 μM.
In Vivo
SB242235 (100 mg/kg; p.o.) abolishes MAP-KAPK-2 activity and HSP27 phosphorylation. SB242235 inhibits expression of the pro-inflammatory cytokines interleukin (IL)-6 and KC (murine IL-8) and COX-2. SB-242235 is demonstrated non-linear elimination kinetics that manifested as a decrease in clearance with increasing dose and apparent oral bioavailability > 100% at high oral doses in rat and monkey. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female SKH-1 hairless mice (4–6 weeks)Dosage: 100 mg/kg Administration: Oral administered, 30 minutes prior to ultraviolet B (UVB) irradiation Result: Abolished MAP-KAPK-2 activity and heat shock protein 27 (HSP27) phosphorylation.
IC50& Target:IC50: 1.0 μM (p38 MAPK, primary human chondrocytes)
Associated Targets(Human)
HSPB1TchemHeat shock protein beta-1 (1 Activities)
