Home Cell Cycle ROCK inhibitor GSK429286A For research use only.

GSK429286A

Synonyms: RHO-15

GSK429286A (RHO-15) is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.

GSK429286A Chemical Structure

GSK429286A Chemical Structure

CAS No. 864082-47-3

Purity & Quality Control

GSK429286A Related Products

Signaling Pathway

ROCK Signaling Pathways

ROCK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells Function assay Inhibition of human recombinant ROCK1 expressed in Sf9 cells at 10 mM, IC50=0.014 μM 17201405
Click to View More Cell Line Experimental Data

Biological Activity

Description GSK429286A (RHO-15) 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
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]
In Vivo
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]
Animal Research Animal Models Male spontaneously hypertensive rats (SHRs)
Dosages ~30 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 432.37 Formula

C21H16F4N4O2
CAS No. 864082-47-3 SDF Download GSK429286A SDF
Smiles CC1=C(C(CC(=O)N1)C2=CC=C(C=C2)C(F)(F)F)C(=O)NC3=C(C=C4C(=C3)C=NN4)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 86 mg/mL ( (198.9 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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.

Handling Instructions

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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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