Stemcell, 73802, Rho Kinase Inhibitor IV

Rho Kinase Inhibitor IV is a selective and potent inhibitor of Rho-associated coiled-coil containing protein kinase 2 (ROCK2; IC₅₀ = 11.8 nM; Tamura et al.). It is a glycyl analog of Fasudil (Catalog #73662) with increased specificity for ROCK2 (Tamura). Rho Kinase Inhibitor IV is more potent than other ROCK inhibitors, including Y-27632 (Ki = 220 nM) and Fasudil (IC₅₀ = 158 nM). It shows good specificity for ROCK2 compared to other kinases such as calcium/calmodulin-dependent kinase type II (IC₅₀ = 2.57 μM), PKG (IC₅₀ = 2.35 μM), Aurora A (IC₅₀ = 3.26 μM), or PKA or PKC (IC₅₀ ≥ 10 μM each). ROCK1 and ROCK2 act downstream of the G protein Rho to regulate actin-myosin turnover and dynamics, and play an important role in stem cell renewal, smooth muscle contraction, cell adhesion, and proliferation (Narumiya et al.; Olson; Watanabe et al.). This product is supplied as a 5 mg/mL solution in methanol.

DIFFERENTIATION

· Promotes neurite growth in primary rat neuronal cultures (Al-Ali et al.).

· Impairs primitive gut tube development including midgut elongation in Xenopus embryos (Reed et al.).

DISEASE MODELING

· Reduces intraocular pressure in a rabbit model of glaucoma (Tamura et al.).