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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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| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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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 |
| 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. |
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