All AbMole products are for research use only, cannot be used for human consumption.
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.
Clin Cancer Res. 2018 Jul 1;24(13):3149-3162.
Targeting bromodomain and extra-terminal (BET) family proteins in castration resistant prostate cancer (CRPC)
GSK269962A purchased from AbMole
 |
Source | Clin Cancer Res (2018). Figure 5. ROCK inhibitor (Abmole Bioscience) |
| Method | ||
| Cell Lines | CP50 PDX-O | |
| Concentrations | 10 μM | |
| Incubation Time | 30 to 45 minutes | |
| 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 |
| 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. |
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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