GSK429286A
Catalog No.S1474 Synonyms: RHO-15
Molecular Weight(MW): 432.37
GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.
4 Customer Reviews
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ROCK antagonists interfere with infection-induced changes in cell shape, but do not reduce HCMV yield. (A) ROCK antagonists block actin reorganization after infection. Fibroblasts were treated with solvent (DMSO) or drug (10 uM Y27632 or 140 nM GSK429286A) beginning 1 h after mock infection or infection with WT virus. Cells received fresh medium containing solvent or drug every 24 h. Cultures were assayed for actin using labeled phalloidin (red), pUL37 (green), and DNA (blue). (B) ROCK antagonist blocks cell rounding at 24 hpi. Fibroblasts were treated with solvent or drug beginning 1 h after mock infection or infection with WT virus. Cultures received fresh medium with drug every 24 h and were analyzed by treatment with 5 μM fluorophore calcein red-orange AM for 1 h, followed by spinning disk confocal Z-stack live cell imaging and reconstruction of 3D images. (C) ROCK activity does not influence virus yield. Fibroblasts were treated with solvent or ROCK antagonists beginning 1 h after infection with WT HCMV. Cultures received fresh medium with drug every 24 h, and extracellular virus yields were determined by plaque assay.
Proc Natl Acad Sci U S A 2014 111(12), E1140-8. GSK429286A purchased from Selleck.
HLMVECs grown to confluence in six-well plates were preincubated with vehicle (0.1% DMSO), Y27632 (10 uM), or GSK429286 (10 uM) for 2 hours, followed by treatment with 1 EU/ml LPS for 2 hours. Western blot analysis was performed for diphosphorylated myosin light chain (ppMLC) and β-actin.
Am J Respir Cell Mol Biol 2014 50(1), 170-9. GSK429286A purchased from Selleck.
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ROCK is required for ETAR-induced YAP/TAZ activation. Serum-starved HCT116 cells were pretreated with GSK429286 (0.5 μmol/L) or Y27632 (1 μmol/L) for 4 hours, followed by treatment with 100 nmol/L of ET-1 for 1 hour. Phosphorylation and protein levels of YAP/TAZ were determined by immunoblotting.
Cancer Res, 2017, 77(9):2413-2423. GSK429286A purchased from Selleck.
The location of E-cadherin and β-catenin was detected by immunofluorescence staining. Data are mean ± SD of four independent experiments
Respir Res, 2017, 18(1):111. GSK429286A purchased from Selleck.
Purity & Quality Control
Choose Selective ROCK Inhibitors
Biological Activity
| Description | GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively. | ||||||||||||||||
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| Features | Greater selectivity than Y-27632. | ||||||||||||||||
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| In vitro |
GSK429286A slightly inhibits RSK and p70S6K with IC50 of 0.78 μM and 1.94 μM, respectively. GSK429286A significantly inhibits rat aortic ring dilation with IC50 of 190 nM. [1] GSK429286A at 1 μM reduces ROCK2 activity over 20-fold, under conditions in which the only other kinase tested that is significantly inhibited is MSK1 whose activity is reduced ~5-fold. GSK429286A is a more selective ROCK2 inhibitor than the widely utilized ROCK inhibitor Y-27632 as assessed on kinase-specificity panel, and does not significantly inhibit LRRK2 even at doses as high as 30 μM (500-fold higher than IC50 of inhibition of ROCK2). Like GSK269962A but not sunitinib, GSK429286A treatment at 10 μM ablates basal or G14V-Rho mutant induced phosphorylation of MYPT at Thr850 in HEK-293 cells to a similar extent as H-1152 and Y-27632, consistent with ROCK mediating this phosphorylation, whereas GSK429286A does not inhibit ERM protein phosphorylation either in the presence or absence of G14V-Rho. [2] |
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| Cell Data |
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| In vivo | GSK429286A has 61% oral bioavailability in male Sprague-Dawley rats. Oral administration of GSK429286A at single doses of 3-30 mg/kg dramatically reduces mean arterial pressure in the spontaneously hypertensive rats (SHRs) in a dose-dependent manner, with a maximum decrease of 50 mmHg after approximately 2 hours treatment at dose of 30 mg/kg. [1] |
Protocol
| Animal Research:[1] |
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Solubility (25°C)
| In vitro | DMSO | 87 mg/mL (201.21 mM) |
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| Ethanol | 4 mg/mL (9.25 mM) | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 15% Captisol+citrate vehicle For best results, use promptly after mixing. |
15 mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 432.37 |
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| Formula | C21H16F4N4O2 |
| CAS No. | 864082-47-3 |
| Storage | powder |
| in solvent | |
| Synonyms | RHO-15 |
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
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Question 1:
The product sold by Selleckchem has an “A” at the end. I am wondering if GSK429286A is the same compound as GSK429286?
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Answer:
For the compound GSK429286A and GSK429286, they are the same comopund and have a identical CAS# (864082-47-3). Attached please find the reference about GSK429286A, which published by GSK, and the link is followed: http://www.ncbi.nlm.nih.gov/pubmed/19740074.
