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In vitro: SR-3677 had an IC50 of ~3 nM in enzyme and cell based assays and had an off-target hit rate of 1.4% against 353 kinases, and inhibited only 3 out of 70 nonkinase enzymes and receptors. Pharmacology studies showed that SR-3677 was efficacious in both, increasing ex vivo aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation. SR-3677 inhibited only three adrenergic receptors: α1a, α1b, and α2a with 53%, 68%, and 76% inhibition, respectively, at 3 ?M inhibitor concentration, which indicates IC50 values in the 1 ?M range or ~300 times higher than the IC50 against ROCK-II in cell-based assays. In vivo: Continuous exposure of 25 ?M SR-3677 increases the outflow facility by 60% at 1 h perfusion, increasing to 70-80% for the 2-5 h time points (p < 0.01). This 70-80% increase in outflow is the maximal response that can be attained and is achieved at doses 2-4-fold lower than needed for Y-27632, a well studied ROCK inhibitor.TM tissue derived from the eyes perfused with 25 ?M SR-3677 shows a very faint band for p-MLC suggesting greater than 90% inhibition of Rho kinase in the TM tissue at this dose.
| Molecular Weight | 408.45 |
| Formula | C22H24N4O4 |
| CAS Number | 1072959-67-1 |
| Solubility (25°C) | 10mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related ROCK Products |
|---|
| Y-27632 dihydrochloride
Y-27632 is a potent, selective inhibitor of Rho-associated protein kinases (ROCK) with IC50 values of 140-220 nM for ROCK1 and ROCK2. In addition, Y-27632 inhibited LPA-induced entosis. |
| Thiazovivin
Thiazovivin is a selective small molecule Rho-associated kinase (ROCK) inhibitor which significantly improves (200-fold) the efficiency of iPSC generation from human fibroblasts. |
| Fasudil hydrochloride
Fasudil hydrochloride is a potent Rho-associated kinase inhibitor with IC50 of 10.7 μM. |
| RKI-1447
RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 6 nM, respectively. |
| GSK429286A
GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively. |
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