| 应用 |
Two Rho-associated kinases (ROCK), ROCK1 and ROCK2, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC = 11.8 nM for ROCK2). It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (fasudil) and exhibits better specificity. Thus, it poorly inhibits Ca/calmodulin-dependent kinase type II, protein kinase (PK) G, and Aurora A (IC = 2.57, 2.35, and 3.26 μM, respectively) as well as PKA or PKC (IC ≥10 μM for each). The potency of Glycyl-H-1152 is superior to that of other ROCK inhibitors, including Y-27632 (K = 220 nM) and HA-1077 (IC = 158 nM). |
