Y-33075 (hydrochloride) (Synonyms: RKI-983, SNJ-1656, Y-39983)

Y-33075 is an inhibitor of Rho-associated kinase 2 (ROCK2; IC₅₀ = 3.6 nM).¹ It is selective for ROCK2 over PKC and calcium/calmodulin-dependent protein kinase II (CaMKII; IC₅₀s = 420 and 810 nM, respectively). Topical application of Y-33075 (0.05% v/v) reduces intraocular pressure in rabbit and cynomolgus monkeys. Y-33075 (10 and 100 µM) increases axonal regeneration at the crush site in a cat model of surgically-induced optic nerve damage.² It also inhibits demyelination and reduces the incidence of relapse episodes in a mouse model of chronic relapsing experimental autoimmune encephalomyelitis (EAE).³

1.Tokushige, H., Inatani, M., Nemoto, S., et al.Effects of topical administration of y-39983, a selective rho-associated protein kinase inhibitor, on ocular tissues in rabbits and monkeysInvest. Ophthalmol. Vis. Sci.48(7)3216-3222(2007) 2.Sagawa, H., Terasaki, H., Nakamura, M., et al.A novel ROCK inhibitor, Y-39983, promotes regeneration of crushed axons of retinal ganglion cells into the optic nerve of adult catsExp. Neurol.205(1)230-240(2007) 3.Gao, C., Huang, L., Long, Y., et al.Y-39983, a selective Rho-kinase inhibitor, attenuates experimental autoimmune encephalomyelitis via inhibition of demyelinationNeuroimmunomodulation20(6)334-340(2013)