y-27632

Y-27632 is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

Y-27632 dihydrochloride (Y-27632 2HCl) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 dihydrochloride also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

Y27632 HCl hydrate is an orally effective, ATP-competitive ROCK1/ROCK2 inhibitor (Ki=220 nM/300 nM) that inhibits caspase-3 and suppresses stem cell apoptosis induced by multiple conditions. It is suitable for studying induced pluripotent stem cell (iPSC) culture.

Y-30141 is closely related to the commonly used ROCK inhibitor, Y-27632. This compound inhibits the kinase activity of both ROCK-I and ROCK-II by competitively binding to the catalytic site, showing 20 to 30 times greater affinity for ROCK kinases compared to other Rho effector kinases. Furthermore, the inhibition mechanism and action profile of Y-30141 have also been investigated.

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).

AS8351 (NSC51355) is a histone demethylase inhibitor. It has been used in combination with CHIR99021, A 83-01, BIX01294, SC-1, Y-27632, OAC2, SU 16f, and JNJ-10198409 to induce reprogramming of human fetal lung fibroblasts into functional cardiomyocytes.