tcsc1726 SR-3677

SR-3677 is a potent and selective ROCK-II inhibitor with an IC₅₀ of ~3 nM.



IC50 & Target: IC50: ~3 nM (ROCK-II)^[1]

In Vitro: SR-3677 has an IC₅₀ of ~3 nM in enzyme and cell based assays and has an off-target hit rate of 1.4% against 353 kinases, and inhibits only 3 out of 70 nonkinase enzymes and receptors. The IC₅₀ value of SR-3677 for ROCK-I is 56±12 nM. The hydrophobic interaction of the benzodioxane phenyl ring with the hydrophobic surface of the pocket is the dominating factor that contributes to the high potency of SR-3677^[1].

In Vivo: ExVivo: Pharmacology studies shows that SR-3677 is efficacious in both, increasing ex vivo

aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation. Continuous exposure of 25 µM SR-3677 increases the outflow facility by 60% at 1 h perfusion, increasing to 70–80% for the 2–5 h time points^[1].