H-1152 化学特性,用途語,生産方法
説明
Rho-associated kinase (ROCK), activated by GTP-
linked Rho, phosphorylates targets that are involved in cytoskeletal remodeling, smooth muscle contraction, and neuronal development. H-
1152 is a potent, specific, ATP-
competitive, and cell permeable inhibitor of ROCK (K
i = 1.6 nM). It is a more potent inhibitor of ROCK than either Y-
27632 (K
i = 140 nM) or HA-
1077 (K
i = 330 nM). H-
1152 poorly inhibits PKA, PKC, and myosin light chain kinase (K
i = 0.63, 9.27, and 10.1 μM, respectively). It has been used to examine the role of ROCK in such diverse processes as stress fiber assembly, vasoconstriction, as well as spontaneously tonic smooth muscle and neurite extension.
生物活性
Rho-kinase (ROCK) inhibitor that displays high selectivity over other protein kinases (IC 50 values are 0.012, 0.180, 0.360, 0.745, 3.03, 5.68 and 28.3 μ M for ROCKII, CAMKII, PKG, Aurora A, PKA, PKC and MLCK respectively). Inhibits sulprostone-induced contractions in guinea pig aorta (IC 50 = 190 nM) and displays proerectile effects in rats.
H-1152 上流と下流の製品情報
原材料
準備製品