Dexloxiglumide, an active enantiomer of Loxiglumide, inhibits smoothmusclecell contractions induced by cholecystokinin-octapeptide (CCK-8). It is a selective antagonist of cholecystokinin type A (CCKA) receptors.
Collagenase, Type VIII 具有水解Type VIII collagen的能力,可应用于动脉粥样硬化形成的研究。Type VIII collagen作为内皮细胞分化及血管生成的调控因子,不仅是平滑肌细胞等细胞粘附迁移的底物,还可能在动脉粥样硬化的发展中积累。此外,内毒素激活的Collagenase, Type VIII表达能够减少Type VIII collagen的产生,进而有助于抑制动脉粥样硬化的进程。
BK 129 is a local anesthetic with relaxant properties. BK 129 inhibits Ca2+ entry into the smoothmusclecell 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 smoothmusclecell 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, smoothmuscle 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).