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A LIMK and ROCK inhibitor
LX7101 is a potent inhibitor of LIM kinase (LIMK) 1 and 2 and Rho-associated kinase 1 (ROCK-1) and ROCK-2 with IC50 values of 32, 4.3, 69, and 32 nM, respectively. It is selective, showing no cross reactivity in a panel of binding assays including 78 receptors and transporters and 430 additional kinases, at a concentration of 10 μM. Topical administration (3 μl of 1 mg/ml solution) of LX7101 to the eye reduces intraocular pressure in a dexamethasone-induced mouse model of glaucoma.
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