Rho-associated protein kinase 2 (ROCK2) regulates the formation of actin stress fibers and focal adhesions, smooth muscle contraction, and gene expression. KD 025 is an orally bioavailable inhibitor of ROCK2 that is greater than 200-fold selective over ROCK1 (IC50s = 105 nM and 24 µM, respectively).{28734} Treatment of fibrosis-derived smooth muscle cells with KD 025 (40 µM) for 24 hours reduces the expression of connective tissue growth factor and remodels actin cytoskeleton.{28734} KD 025 decreases cell-spanning F-actin fibers and increases motility of microvascular endoethelial cells.{28735} In mice, KD 025 given by oral gavage dose-dependently reduces infarct volume after transient middle cerebral artery occlusion without causing significant hypotension.{28736} In humans, oral KD 025 diminishes STAT3 phosphorylation and pro-inflammatory cytokine production in CD4+ T cells while up-regulating phosphorylation of STAT5 in regulatory T cells, altering the immune response.{27716}
产品描述
An orally bioavailable inhibitor of ROCK2 that is greater than 200-fold selective over ROCK1 (IC50s = 105 nM and 24 µM, respectively); increases motility of microvascular endoethelial cells; alters cell function and inflammatory responses in vivo
