Glycyl H-1152 hydrochloride - CAS 913844-45-8

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) .

Others, Aurora Kinase, ROCK, CaMK

Neuroscience, Stem Cells, Others, Chromatin/Epigenetic, Cytoskeletal Signaling, Cell Cycle/Checkpoint

913791

C18H26Cl2N4O3S

449.39

Cl.Cl.C[C@H]1CN(CCCN1S(=O)(=O)c1cccc2cncc(C)c12)C(=O)CN

-20°C

Ice Packs

Small Compound