Rho Kinase Inhibitor IV (2HCl), 1 mg

A small molecule from STEMCELL Technologies that functions as a RHO/ROCK pathway inhibitor and is described as a potent and selective inhibitor of Rho-associated coiled-coil containing protein kinase 2 (ROCK2), with a reported IC50 of 11.8 nM. It 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). Selectivity data show reduced activity against 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).

Also known by the synonym (S)-Glycyl-H-1152, the dihydrochloride salt has CAS number 913844-45-8, molecular formula C18H24N4O3S · 2HCl, molecular weight 449.4 g/mol, and a purity of ≥ 98%. The product is supplied as a solution in methanol and should be stored at -20°C, protected from prolonged exposure to light; it is stable as supplied for 12 months from date of receipt.

Published research 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 classified as hazardous because it is supplied in methanol, which is present at 99.5% and is highly flammable, toxic if inhaled, swallowed, or in contact with skin, and can cause damage to organs. A California Proposition 65 warning applies because the product can expose users to methanol, which is known to the State of California to cause birth defects or other reproductive harm. For research use only; not intended for human or animal diagnostic or therapeutic uses.