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GSK299115A

Name: GSK299115A
Brand: TargetMol
SKU: T27471
Price: 336 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T27471Cas No. 864082-35-9

Alias GSK-299115A, GSK 299115A

GSK299115A (GSK-299115A) is a selective ROCK1 Inhibitor. GSK299115A exhibits IC50 of 8nM, 620nM, 560nM for ROCK1, RSK1, p70S6K, respectively.

GSK299115A

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Purity: 99.81%

Catalog No. T27471Alias GSK-299115A, GSK 299115ACas No. 864082-35-9

GSK299115A (GSK-299115A) is a selective ROCK1 Inhibitor. GSK299115A exhibits IC50 of 8nM, 620nM, 560nM for ROCK1, RSK1, p70S6K, respectively.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$336	In Stock	In Stock
5 mg	$813	In Stock	In Stock
10 mg	$1,130	In Stock	In Stock
25 mg	$1,680	In Stock	In Stock
50 mg	$2,260	-	In Stock
100 mg	$2,970	-	In Stock
1 mL x 10 mM (in DMSO)	$995	In Stock	In Stock

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

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.81%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

GSK299115A AI Summary

GSK299115A is a multi-target kinase inhibitor with bioactivity against enzymes such as ROCK1, RSK1, p70S6K, GRK5, GRK2, and Yes1 kinase. It shows varying potencies with IC50 values for GRK5, GRK2, and PKA being 79.4 µM, 3.2 µM, and 63.1 µM respectively, and has lower potency for GRK1 (> 1 mM). For Yes1 kinase, the potency is reported at 2919.2 nM. Additionally, it inhibits Lassa Virus entry at a concentration of 12538.5 nM. GSK299115A also affects IKK-alpha, IKK-beta, IKK-epsilon, Mer Kinase, PIP5K1, and TBK1, showing inhibition rates at various concentrations. Pharmacokinetic properties in Sprague-Dawley rats include an oral bioavailability factor of 1.0% at 0.9 mg/kg, volume of distribution (Vdss) of 2.4 L.kg-1, clearance rate (CL) of 57.0 mL.min-1.kg-1, half-life (T1/2) of 0.8 hours, and a peak plasma concentration (Cmax) of 804.28 nM. These properties suggest GSK299115A may be useful for research into kinase-related diseases and potentially as a therapeutic agent..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	GSK299115A (GSK-299115A) is a selective ROCK1 Inhibitor. GSK299115A exhibits IC50 of 8nM, 620nM, 560nM for ROCK1, RSK1, p70S6K, respectively.
Synonyms	GSK-299115A, GSK 299115A

Chemical Properties

Molecular Weight	415.27
Formula	C₂₀H₁₆Cl₂N₄O₂
Cas No.	864082-35-9
Smiles	C(NC=1C=C2C(=CC1)NN=C2)(=O)C=3C(CC(=O)NC3C)C4=CC(Cl)=C(Cl)C=C4
Relative Density.	1.479 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (120.4 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4081 mL	12.0404 mL	24.0807 mL	120.4036 mL
5 mM	0.4816 mL	2.4081 mL	4.8161 mL	24.0807 mL
10 mM	0.2408 mL	1.2040 mL	2.4081 mL	12.0404 mL
20 mM	0.1204 mL	0.6020 mL	1.2040 mL	6.0202 mL
50 mM	0.0482 mL	0.2408 mL	0.4816 mL	2.4081 mL
100 mM	0.0241 mL	0.1204 mL	0.2408 mL	1.2040 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