SB 242235 |
Katalog-Nr.GC37595 |
SB-242235 ist ein potenter und selektiver p38-MAP-Kinase-Inhibitor mit einem IC50-Wert von 1,0 μM in primÄren menschlichen Chondrozyten.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 193746-75-7
Sample solution is provided at 25 µL, 10mM.
SB-242235 is a potent and selective p38 MAP kinase inhibitor, with an IC50 of 1.0 μM in primary human chondrocytes[1]. IC50: 1.0 μM (p38 MAPK, primary human chondrocytes)[1]
SB 242235 (0-10 μM) dose-dependently inhibits the activation of MAPKAP K2 with an IC50 of 1.0 μM in human chondrocytes stimulated with IL-1β[1].SB 242235 inhibits intracellular p38 activity, MAPKAP K2 was then isolated from these cells and assayed using HSP27 as a substrate[1]. Western Blot Analysis[1] Cell Line: Human chondrocytes
SB242235 (100 mg/kg; p.o.) abolishes MAP-KAPK-2 activity and HSP27 phosphorylation[2].SB242235 inhibits expression of the pro-inflammatory cytokines interleukin (IL)-6 and KC (murine IL-8) and COX-2[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[3]. Animal Model: Female SKH-1 hairless mice (4-6 weeks)[2]
[1]. Badger, A.M., et al., Differential effects of SB 242235, a selective p38 mitogen-activated protein kinase inhibitor, on IL-1 treated bovine and human cartilage/chondrocyte cultures. Osteoarthritis Cartilage, 2000. 8(6): p. 434-43. [2]. Kim AL , et al. Role of p38 MAPK in UVB-induced inflammatory responses in the skin of SKH-1 hairless mice. J Invest Dermatol. 2005 Jun;124(6):1318-25. [3]. Ward, K.W., et al., SB-242235, a selective inhibitor of p38 mitogen-activated protein kinase. I: preclinical pharmacokinetics. Xenobiotica, 2002. 32(3): p. 221-33.
Average Rating: 5
(Based on Reviews and 19 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *