SR 3677 is a potent, ATP-competitive inhibitor of Rho-associated kinases (ROCKs) that shows greater potency against ROCK-II than ROCK-I in enzyme and cell-based assays (IC50 values are 3 and 56 nM, respectively). At 3 μM, SR 3677 inhibits only 5 (Akt3, Clk1, Clk2, Clk4, Lats2) out of 353 kinases with greater than 50% inhibition. SR 3677 is efficacious at inhibiting myosin light chain phosphorylation and increasing aqueous humor outflow in porcine eyes in an ex vivo model of glaucoma treatment.
