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.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| 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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related ROCK Products |
|---|
| 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. |
| ROCK-IN-6
ROCK-IN-6 is a potent and selectiveROCK2 inhibitor with an IC50 of 2.19 nM. |
| ROCK-IN-4
ROCK-IN-4 is a potent ROCK inhibitor maintaining NO releasing ability. |
| ROCK-IN-32
ROCK-IN-32 is a ROCK inhibitor, with an IC50 value of 11 nM for ROCK2. |
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