Rho Kinase Inhibitor IV (2HCl), 500 µg

STEMCELL Technologies supplies a selective and potent small-molecule inhibitor of Rho-associated coiled-coil containing protein kinase 2 (ROCK2), with an IC₅₀ of 11.8 nM reported by Tamura et al. The compound is a glycyl analog of Fasudil with increased specificity for ROCK2, and 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 with 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), and 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.

The product is supplied as the dihydrochloride salt of (S)-Glycyl-H-1152 (CAS 913844-45-8), with chemical formula C₁₈H₂₄N₄O₃S · 2HCl, molecular weight 449.4 g/mol, and purity ≥ 98%, as a 5 mg/mL solution in methanol. Published applications include promoting neurite growth in primary rat neuronal cultures, impairing primitive gut tube development including midgut elongation in Xenopus embryos, and reducing intraocular pressure in a rabbit model of glaucoma. The product is stable for 12 months from date of receipt when stored at -20°C and protected from prolonged light exposure. For research use only.