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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 |
|---|
| OXA-06 hydrochloride
OXA-06 hydrochloride is an ATP-competitive ROCK inhibitor that blocks anchorage-dependent growth and invasion of non-small cell lung cancer cell lines. |
| Y-33075 hydrochloride
Y-33075 hydrochloride (Y-39983) is a selective ROCK inhibitor derived from Y-27632, and is more potent than Y-27632, with an IC50 of 3.6 nM. |
| SR-3677 dihydrochloride
SR-3677 dihydrochloride is a potent and selective ROCK-I and ROCK-II inhibitor with an IC50 values of 56 nM and 3 nM. |
| Akt/ROCK-IN-1
Akt/ROCK-IN-1 (B12) is a dual inhibitor for Akt and ROCK, with the IC50s of 0.023 nM and 1.47 nM, respectively. |
| Scaff10-8
Scaff10-8, bound to RhoA, inhibits the AKAP-Lbc-mediated RhoA activation. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
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