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AS 1892802 is a potent and selective inhibitor of ROCK with IC50 values of 52, 57 and 122 nM for human ROCK2, rat ROCK2 and human ROCK1, respectively [1].

Rho kinase (ROCK) is a serine-threonine kinase and is a downstream effector of Rho, a small GTP-bound protein. ROCK phosphorylates target proteins such as myosin light chain kinase and LIM kinase and regulates cellular shape modification, migration, growth and contraction [2].

AS 1892802 is a potent ROCK inhibitor. AS 1892802 inhibited ROCK1 and ROCK2 with IC50 values of 1.69 and 0.10 μM, respectively [3]. In ATDC5 cells, AS1892802 induce chondrocyte differentiation. In HIG82 cells, AS1892802 significantly inhibited prostaglandin E2 production induced by IL-1β or bradykinin [4].

In both an adjuvant-induced arthritis (AIA) rat model and a monoiodoacetate (MIA) -induced arthritis (MIA) rat model, AS1892802 showed potent antinociceptive effect with ED50 value of 0.15 mg/kg [1]. In monoiodoacetate-induced arthritis and streptozotocin-induced neuropathy models, AS1892802 showed analgesic effect [2]. In MIA-injected rats, the mRNA levels of ROCK I and II increased in knee joints. AS1892802 significantly inhibited cartilage damage in a dose-dependent way [4].

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