Use and properties of ROCK-specific inhibitor Y-27632

Publisher Summary This chapter discusses the use and properties of Rho kinase (ROCK)-specific inhibitor Y-27632. The chapter describes three examples of in vitro applications of Y-27632 in tissues and cultured cells. Y-27632 and related compounds specifically bind to the ROCK family of kinases and inhibit their kinase activity. ROCK family of kinases is involved in the increase of actomyosin-based contractility through phosphorylation and down regulation of myosin phosphatase.Y-27632 inhibits ROCK by competing with ATP for binding to the catalytic site. The use of Y-27632 as a smooth muscle relaxant is also discussed in the chapter. The chapter explains the inhibition of lysophosphatidic acid (LPA)-induced neurite retraction in N1E-115 neuroblastoma cells and specificity of Y-27632 actions. The chapter concludes with a discussion of in viv o applications of Y-27632.