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GSK429286A

Name: GSK429286A
Brand: TargetMol
SKU: T2633
Price: 35 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2633Cas No. 864082-47-3

Alias RHO-15

GSK429286A (RHO-15) is a specific inhibitor of ROCK1/2 (IC50: 14/63 nM).

GSK429286A

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Purity: 98.49%

Catalog No. T2633Alias RHO-15Cas No. 864082-47-3

GSK429286A (RHO-15) is a specific inhibitor of ROCK1/2 (IC50: 14/63 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$35	In Stock	In Stock
5 mg	$56	In Stock	In Stock
10 mg	$85	In Stock	In Stock
25 mg	$139	In Stock	In Stock
50 mg	$215	In Stock	In Stock
100 mg	$369	-	In Stock
1 mL x 10 mM (in DMSO)	$63	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Batch Information

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Purity:98.49%

Appearance:Solid

Color:White to Yellow

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	GSK429286A (RHO-15) is a specific inhibitor of ROCK1/2 (IC50: 14/63 nM).
Targets&IC50	ROCK2:63 nM, p70 S6K:1940 nM, ROCK1:14 nM, RSK:780 nM
In vitro	GSK429286A (3-30 mg/kg, p.o.) significantly reduces the mean arterial pressure in spontaneous hypertensive rats in a dose-dependent manner, with a maximum reduction of 50 mmHg approximately 2 hours after administering a dose of 30 mg/kg. In male Sprague-Dawley rats, the oral bioavailability of GSK429286A is 61%.
In vivo	GSK429286A at a concentration of 1 μM significantly reduces the activity of ROCK2 by 20-fold, whereas it only reduces MSK1 activity by approximately 5-fold at the same concentration. This compound exhibits higher selectivity as an ROCK2 inhibitor compared to the commonly used inhibitor Y-27632, showing negligible inhibition against LRRK2 even at 30 μM, with an IC50 that is 500 times higher for ROCK2. Similar to GSK269962A, GSK429286A at 10 μM can eliminate phosphorylation at Thr850 of MYPT induced either by the baseline or by the G14V-Rho mutant in HEK-293 cells, demonstrating effects similar to those of H-1152 and Y-27632 and consistent with ROCK-mediated phosphorylation. Regardless of the presence of G14V-Rho, GSK429286A does not affect the phosphorylation of ERM proteins. Additionally, GSK429286A mildly inhibits RSK (IC50: 0.78 μM) and p70S6K (IC50: 1.94 μM). It also significantly inhibits the dilation of rat aortic rings (IC50: 190 nM).
Kinase Assay	Binding affinity assays: TR-FRET-binding affinity assays are performed for BCL-2, BCL-XL, and MCL-1 in 4.52?mM monobasic potassium phosphate, 15.48?mM dibasic potassium phosphate, 1?mM sodium EDTA, 0.05% Pluronic F-68 detergent, 50?mM sodium chloride, and 1?mM DTT (pH 7.5). For MCL-1 assays, GST-tagged MCL-1 (1?nM) is mixed with 100?nM f-Bak, 1?nM Tb-labeled anti-GST antibody, and compound at room temperature (RT) for 60?min. Fluorescence is measured on an Envision plate reader using a 340/35?nm excitation filter and 520/525 (f-Bak) and 495/510?nm (Tb-labeled anti-GST antibody) emission filters.
Synonyms	RHO-15

Chemical Properties

Molecular Weight	432.37
Formula	C₂₁H₁₆F₄N₄O₂
Cas No.	864082-47-3
Smiles	CC1=C(C(CC(=O)N1)c1ccc(cc1)C(F)(F)F)C(=O)Nc1cc2cn[nH]c2cc1F
Relative Density.	1.468

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 4 mg/mL (9.25 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 140 mg/mL (323.8 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.63 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3128 mL	11.5642 mL	23.1283 mL	115.6417 mL
5 mM	0.4626 mL	2.3128 mL	4.6257 mL	23.1283 mL

DMSO

	1mg	5mg	10mg	50mg
10 mM	0.2313 mL	1.1564 mL	2.3128 mL	11.5642 mL
20 mM	0.1156 mL	0.5782 mL	1.1564 mL	5.7821 mL
50 mM	0.0463 mL	0.2313 mL	0.4626 mL	2.3128 mL
100 mM	0.0231 mL	0.1156 mL	0.2313 mL	1.1564 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc