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GSK429286A is a cell-permeable, selective Rho-associated kinase (ROCK) inhibitor with an IC50 of 14 nM. GSK429286A also possessed exciting selectivity (30-fold) against a panel of 33 kinases, including RSK1 (IC50 = 3.1 μM) and p70S6K (Ic50 = 2.85μM). ROCKs are serine/threonine specific protein kinases which play a crucial role in organization of the actin cytoskeleton. ROCK inhibitors have been found to prevent apoptosis, as well as to enhance the survival and cloning efficiency of dissociated human embryonic stem (ES) cells without affecting their self-renewal properties or pluripotency.
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| Animal models | Male spontaneously hypertensive rats (SHRs) |
| Formulation | Formulated in 6% Hydroxypropyl-β-Cyclodextrin (pH4.0) and 5% DMSO solution |
| Dosages | ~30 mg/kg |
| Administration | Oral gavage |
| Molecular Weight | 432.37 |
| Formula | C21H16F4N4O2 |
| CAS Number | 864082-47-3 |
| Solubility (25°C) | DMSO 75 mg/mL |
| 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. |
| GSK269962A
GSK269962A is a potent ROCK inhibitor with IC50 values of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2, respectively. |
| 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 |
|---|
| 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. |
| 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. |
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Products are for research use only. Not for human use. We do not sell to patients.
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