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GSK429286A ROCK inhibitor

Name: GSK429286A
SKU: S1474
Availability: InStock
Rating: 5 (23 reviews)

Cat.No.S1474

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

Chemical Structure

Molecular Weight: 432.37

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.92%

99.92

Related Targets	DNA/RNA Synthesis CDK Microtubule Associated Ras HSP PD-1/PD-L1 Aurora Kinase Casein Kinase Rho Serine/threonin kinase eIF Chk Myc Kinesin PLK DHFR PAK PERK DYRK RUNX PP2A PFKFB AP-1 MPS1 Wee1 p21 BMI-1 LIM kinase Nur77 APC
Related Products	Y-27632 Dihydrochloride Y-27632 Fasudil HCl Thiazovivin (TZV) RKI-1447 Ripasudil hydrochloride dihydrate GSK269962A HCl Y-39983 Dihydrochloride Hydroxyfasudil HCl Chroman 1 DJ4 GSK269962A Azaindole 1 (BAY-549) ROCK2 Antibody [G16E9] ROCK2 Antibody [K12H24] Zelasudil ROCK2 + ROCK1 Antibody [A21E5] WAY-624704 ROCK1 Antibody [L9K19] NRL-1049 ROCK1 Antibody [A18A7]

Cell Culture, Treatment & Working Concentration

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

Chemical Information, Storage & Stability

Molecular Weight	432.37	Formula	C₂₁H₁₆F₄N₄O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	864082-47-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	RHO-15			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

Solubility

In vitro
Batch:

DMSO : 86 mg/mL (198.9 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	15% Captisol 1 citrate vehicle Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (23.13mM)	Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 15% Captisol+citrate vehicle clear solution, and mix evenly to make it a uniform suspension. The mixed solution should be used immediately for optimal results.
Clear solution	2% DMSO 1 40% PEG300 2 5%Tween80 3 53%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (6.94mM)	Taking the 1 mL working solution as an example, add 20 μL of 150 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 530 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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.

Mechanism of Action

Features	Greater selectivity than Y-27632.
Targets/IC₅₀/Ki	ROCK1 ^[1] (Cell-free assay) 14 nM ROCK2 ^[2] (Cell-free assay) 63 nM
In vitro	GSK429286A slightly inhibits RSK and p70S6K with IC50 of 0.78 μM and 1.94 μM, respectively. This compound significantly inhibits rat aortic ring dilation with IC50 of 190 nM. ^[1] This chemical 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. It 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, this compound 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 it does not inhibit ERM protein phosphorylation either in the presence or absence of G14V-Rho. ^[2]
In vivo	GSK429286A has 61% oral bioavailability in male Sprague-Dawley rats. Oral administration of this compound 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]
References	[1] https://pubmed.ncbi.nlm.nih.gov/17201405/ [2] https://pubmed.ncbi.nlm.nih.gov/19740074/

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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 it is the same compound as GSK429286?

Answer:
For the compound GSK429286 and this compound, they are the same and have an identical CAS# (864082-47-3). Attached please find the reference about it, which was published by GSK, and the link is followed: http://www.ncbi.nlm.nih.gov/pubmed/19740074.

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