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SB 242235

CAS No. : 193746-75-7

MCE 站：SB 242235

产品活性：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。

研究领域：MAPK/ERK Pathway  |  Autophagy

作用靶点：p38 MAPK  |  Autophagy

In Vitro: 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.
SB 242235 inhibits intracellular p38 activity, MAPKAP K2 was then isolated from these cells and assayed using HSP27 as a substrate.

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.

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