(S)-(+)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLYNYL)SULFONYL]HOMOPIPERAZINE Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Rho-associated kinase (ROCK), activated by GTP-
linked Rho, phosphorylates targets that are involved in cytoskeletal remodeling, smooth muscle contraction, and neuronal development. H-
1152 is a potent, specific, ATP-
competitive, and cell permeable inhibitor of ROCK (K
i = 1.6 nM). It is a more potent inhibitor of ROCK than either Y-
27632 (K
i = 140 nM) or HA-
1077 (K
i = 330 nM). H-
1152 poorly inhibits PKA, PKC, and myosin light chain kinase (K
i = 0.63, 9.27, and 10.1 μM, respectively). It has been used to examine the role of ROCK in such diverse processes as stress fiber assembly, vasoconstriction, as well as spontaneously tonic smooth muscle and neurite extension.
Biologische Aktivit?t
Rho-kinase (ROCK) inhibitor that displays high selectivity over other protein kinases (IC 50 values are 0.012, 0.180, 0.360, 0.745, 3.03, 5.68 and 28.3 μ M for ROCKII, CAMKII, PKG, Aurora A, PKA, PKC and MLCK respectively). Inhibits sulprostone-induced contractions in guinea pig aorta (IC 50 = 190 nM) and displays proerectile effects in rats.
(S)-(+)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLYNYL)SULFONYL]HOMOPIPERAZINE Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte