y-27632

Y-27632 是一种 ROCK-I 和 ROCK-II 抑制剂，具有口服有效性、ATP 竞争性。Y-27632 还抑制分离诱导的小鼠前列腺干或祖细胞凋亡。

Y-27632 dihydrochloride (Y-27632 2HCl) 是一种 ROCK-I 和 ROCK-II 抑制剂，具有口服有效性、ATP 竞争性。Y-27632 dihydrochloride 还抑制分离诱导的小鼠前列腺干或祖细胞凋亡。

AS8351 (NSC51355) 是一种组蛋白去甲基化酶抑制剂，可以诱导人胎儿肺成纤维细胞重编程为功能性心肌细胞。

Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, 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 (IC50 = 11.8 nM for ROCK-II). 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 μM, respectively) as well as PKA or PKC (IC50 ≥ 10 μM for each). 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).

Y27632 is a selective ROCK inhibitor, which inhibits ET-1-induced increases in natriuretic peptide production, cell size, protein synthesis, and myofibrillar organization. Y27632 prevents dimethylnitrosamine-induced hepatic fibrosis in rats, increases apoptosis and disrupts the actin cortical mat in embryonic avian corneal epithelium, affects initial heart myofibrillogenesis in cultured chick blastoderm, promotes the proliferation and cell cycle progression of cultured astrocyte from spinal cord.

Y-33075 is a selective inhibitor of ROCK derived from Y-27632, and is more potent than Y-27632, with an IC50 of 3.6 nM.