SB-242235　是一种有效、选择性的　p38 MAP 激酶抑制剂，在人的软骨细胞中　IC50　值为 1.0 μM。
CAS：193746-75-7
分子式：C19H20FN5O
分子量：353.39
纯度：98%
存储：Store at -20°C

Background:

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.