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SAR407899 is a potent and selective, ATP-competitive ROCK inhibitor with IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively.
SAR407899 inhibits ROCK-2 better than ROCK-1, with IC50s of 102 ± 19 nM and 276 ± 26 nM, respectively, in the presence of 40 μM ATP. SAR407899 also less potently inhibits PKC-Δ and MSK-1, with IC50s of 5.4 and 3.1 μM, respectively. SAR407899 (0.1, 0.3, 1.0, and 3.0 μM) specifically inhibits the ROCK-mediated phosphorylation of MYPTT696 in HeLa cells stimulated with PHEN, and shows such effects at 1 μM and 10 μM in primary rat aortic smooth muscle cells. SAR407899 (3 μM) completely blocks thrombin-induced shrinkage of human umbilical vein endothelial cells (HUVECs) and stress fiber formation.
SAR407899 (0.01-0.30 mg/kg; i.v.) efficiently reduces pressor responses to vasoconstrictor agents in rats.
| Molecular Weight | 244.29 |
| Formula | C14H16N2O2 |
| CAS Number | 923359-38-0 |
| Solubility (25°C) | DMSO 5 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related ROCK Products |
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| 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. |
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.
Products are for research use only. Not for human use. We do not sell to patients.
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