GSK429286A

Catalog No.S1474 Synonyms: RHO-15

GSK429286A Chemical Structure

Molecular Weight(MW): 432.37

GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.

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In DMSO USD 640 In stock
USD 180 In stock
USD 680 In stock
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3 Customer Reviews

  • 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.

  • 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.

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Biological Activity

Description GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.
Features Greater selectivity than Y-27632.
Targets
ROCK1 [1]
(Cell-free assay)
ROCK2 [2]
(Cell-free assay)
14 nM 63 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells MUnGeY5kfGmxbjDhd5NigQ>? NELufY5KdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IGLPR2syKGW6cILld5Nm\CCrbjDT[lkh[2WubIOgZZQhOTBibV2sJGlEPTB;MD6wNVQh|ryP MXmxO|IxOTRyNR?=

... Click to View More Cell Line Experimental Data

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]
+ Expand
  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 87 mg/mL (201.21 mM)
Ethanol 4 mg/mL (9.25 mM)
Water Insoluble
In vivo Add solvents individually and in order:
15% Captisol+citrate vehicle
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
Formula

C21H16F4N4O2

CAS No. 864082-47-3
Storage powder
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

  • Question 1:

    The product sold by Selleckchem has an “A” at the end. I am wondering if GSK429286A is the same compound as GSK429286?

  • 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID