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GSK429286A

Name: GSK429286A
Brand: Selleck Chemicals
SKU: S1474
Rating: 5 (21 reviews)

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.

CAS No. 864082-47-3

Selleck's GSK429286A has been cited by 21 publications

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ROCK Signaling Pathway Map

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?=

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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 (from reference)

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

References

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
Storage	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

Download GSK429286A SDF

In vivo Formulation Calculator (Clear solution)

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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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