Dexloxiglumide, an active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8). It is a selective antagonist of cholecystokinin type A (CCKA) receptors.
BK 129 is a local anesthetic with relaxant properties. BK 129 inhibits Ca2+ entry into the smooth muscle cell and Ca2+ release from sarcoplasmic reticulum.
DL-threo dihydrosphingosine is a cell-permeable inhibitor of the extracellular signal-regulated kinase (ERK) signalling cassette in mammalian cells. DL-threo dihydrosphingosine is effective against both growth factor- and G-protein-dependent activation of
FK-739 is an angiotensin type 1 receptor antagonist. FK 739 inhibits the specific binding of [125I]-angiotensin II to rat aortic smooth muscle cell membrane (IC50 = 8.6 nM) without displacing the specific binding of [125I]-angiotensin II to bovine cerebel
Cytochalasin D is an actin inhibitor, the removal of actin stress fibers is crucial for the chondrogenic differentiation. It may be an inhibitor of some fertilization processes such as sperm penetration or sperm head decondensation. Cytochalasin D inhibit
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).