Rho Kinase (ROCK) Inhibitors
Rho-associated protein kinases (ROCKs) are enzymes that phosphorylate Serine/Threonine residues on various cytoskeletal proteins involved in modulating the shape (morphology, polarity) and movement (motility, contractility) of cells. ROCK 1 and 2 are the two main human ROCKs which are similar in sequence but have different downstream targets. ROCKs are involved in various aspects of actin-filament organization that is central to the elasticity/contractility of a cell (important during cytokinesis). ROCKs contribute to phosphorylation of tumor suppressor proteins, cell fate determination proteins, downregulation of insulin signaling, membrane-blebbing during apoptosis, shaping neuronal architecture, neurite elongation and cell-cell adhesion events. Justifiably, ROCK signaling is important in many diseases including diabetes, neurodegenerative diseases, cardiovascular diseases, pulmonary hypertension, Atherosclerosis and cancer. ROCK inhibitors have a lot of therapeutic potential for the treatment of many of these diseases including the prevention of cell migration, tissue thickening during tumor formation and invasion of malignant cells into healthy tissues during cancer progression. Several small-molecules like Fasudil and Y-27632 have been broadly used as ATP-competitive ROCK inhibitors. BioVision offers a wide selection of structurally diverse ROCK inhibitors for research including some inhibitors as ready-to-use EZSolution™ products.
