ROCK2-IN-2 is a selective ROCK2 inhibitor extracted from patent US20180093978A1, Compound A-30, has an IC50 of <1 μM.
Rho-associated protein kinase (ROCK) is a member of the serine-threonine protein kinase family. ROCK, which exists in two isoforms, ROCK1 and ROCK2, is an effector molecule of RhoA, and the RhoA/ROCK signaling pathway is involved in a number of cellular functions, which include, for example, actin organization, cell adhesion, cell migration, and cytokinesis. In addition, the RhoA/ROCK signaling pathway is involved in regulating smooth muscle contraction. Inhibitors of ROCK have been reported to be useful for treating multiple medical disorders, such as fibrosis, inflammatory disorders, autoimmune disorders, and cardiovascular disorders[1].
[1]. Aicher, Thomas Daniel, et al. INDAZOLYL THIADIAZOLAMINES AND RELATED COMPOUNDS FOR INHIBITION OF RHO-ASSOCIATED PROTEIN KINASE AND THE TREATMENT OF DISEASE. US20180093978A1.