GSK429286A

Catalog No.S1474 Synonyms: RHO-15

For research use only.

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

GSK429286A Chemical Structure

CAS No. 864082-47-3

Selleck's GSK429286A has been cited by 21 publications

Purity & Quality Control

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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

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 NVP2SpppTnWwY4Tpc44h[XO|YYm= MUXJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFKRQ1uxJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiYYSgNVAhdU1uIFnDOVA:OC5yMUSg{txO Ml7NQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd{MEG0NFUoRjF5MkCxOFA2RC:jPh?=
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 (from reference)

Animal Research:[1]
  • Animal Models: Male spontaneously hypertensive rats (SHRs)
  • Dosages: ~30 mg/kg
  • Administration: Oral gavage

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 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

Chemical Information

Molecular Weight 432.37
Formula

C21H16F4N4O2

CAS No. 864082-47-3
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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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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