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GSK269962A is a potent ROCK inhibitor with IC50 values of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2, respectively. GSK269962A displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases. GSK269962A induces vasorelaxation in preconstricted rat aorta (IC50 = 35 nM). GSK269962A induced a reduction in blood pressure of approximately 10, 20, and 50 mm Hg at doses of 1, 3, and 30 mg/kg. GSK269962A represents a novel class of ROCK inhibitors that have profound effects in the vasculature and may enable us to further evaluate the potential beneficial effects of ROCK inhibition in animal models of cardiovascular as well as other chronic diseases.
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Application | |
| Results | Nuclear BRD4 expression increased significantly (p=0.008) as patients progressed from HSPC |
| Molecular Weight | 570.6 |
| Formula | C29H30N8O5 |
| CAS Number | 850664-21-0 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Best-selling 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. |
| H-1152
H-1152, an isoquinolinesulfonamide derivative, is a more specific, stronger and membrane-permeable inhibitor of Rho-kinase with a Ki value of 1.6 nM, but poor inhibitor of other serine/threonine kinases. |
| Y-39983 dihydrochloride
Y-39983 (Y-33075) dihydrochloride is a selective ROCK inhibitor with an IC50 of 3.6 nM, derived from Y-27632, inhibited ROCK more potently than Y-27632. |
| TC-S 7001
BAY-549 (TC-S 7001) is a potent and highly selective, orally active ROCK inhibitor, with IC50 values of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2, respectively. |
| Other ROCK Products |
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| 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. |
| Fasudil
Fasudil (HA-1077) is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM, respectively. |
| RKI-1313
Inhibition of ROCK in human H1299 cells assessed as decrease in phosphorylation of MYPT-1 after 1 hr by Western immunoblotting assay. |
| Hydroxyfasudil hydrochloride
Hydroxyfasudil (HA-1100), an active metabolite of fasudil hydrochloride, is a specific Rho-kinase(ROCK) inhibitor with IC50 values of 0.73 μM and 0.72 μM for ROCK1 and ROCK2, 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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