(S)-Glycyl-H-1152 (hydrochloride)

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.{17734,17735,17322} Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK2).{17736} It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (fasudil) and exhibits better specificity. Thus, it poorly inhibits Ca2+/calmodulin-dependent kinase type II, protein kinase (PK) G, and Aurora A (IC50 = 2.57, 2.35, and 3.26 ?M, respectively) as well as PKA or PKC (IC50 ?10 ?M for each).{17736} The potency of Glycyl-H-1152 is superior to that of other ROCK inhibitors, including Y-27632 (Ki = 220 nM) and HA-1077 (IC50 = 158 nM).{17736,17737}