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GSK963

Name: GSK963
Brand: TargetMol
SKU: T5054
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T5054Cas No. 2049868-46-2

Alias GSK963 (Racemate)

GSK963 (Racemate), a structurally distinct, potent and selective inhibitor of RIP1 kinase(IC50=29 nM).

GSK963

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Purity: 98.00%

Catalog No. T5054Alias GSK963 (Racemate)Cas No. 2049868-46-2

GSK963 (Racemate), a structurally distinct, potent and selective inhibitor of RIP1 kinase(IC50=29 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$30	In Stock	In Stock
2 mg	$43	In Stock	In Stock
5 mg	$72	In Stock	In Stock
10 mg	$122	In Stock	In Stock
25 mg	$247	In Stock	In Stock
50 mg	$397	In Stock	In Stock
100 mg	$582	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$79	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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Purity:98.00%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	GSK963 (Racemate), a structurally distinct, potent and selective inhibitor of RIP1 kinase(IC50=29 nM).
Targets&IC50	RIP1:29 nM
In vitro	The increased potency of GSK 963 relative to Nec-1 in vitro also translated into increased efficacy in the TNF+zVAD-induced model of sterile shock.?At a dose of 2 mg/kg, GSK 963 was able to completely inhibit temperature loss in response to TNF+zVAD, ?the phenotype of the recently described RIP1 kinase-dead knock-in mice.?The level of inhibition of temperature loss in this acute model at different doses of GSK 963 was in line with the predictions of efficacy based on modeling of the pharamacokinetic profile and in vitro potency of GSK 963.
In vivo	GSK 963 efficiently blocked necroptosis in both murine and human cells with IC50 values of 1 nM and 4 nM, respectively, whereas the inactive analog GSK 962 was at least 1000-fold less potent in these assays.
Kinase Assay	GSK′963 was tested against 339 kinases using a P33-radiolabeled assay at Reaction Corp Biology. The compound was tested at a single dose in duplicate at 10?μM. Reactions were carried out at 10?μM ATP. Data are reported as % enzyme activity (relative to DMSO controls).
Synonyms	GSK963 (Racemate)

Chemical Properties

Molecular Weight	230.31
Formula	C₁₄H₁₈N₂O
Cas No.	2049868-46-2
Smiles	CC(C)(C)C(=O)N1N=CC[C@H]1c1ccccc1
Relative Density.	1.06 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: 40 mg/mL (173.68 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 2 mg/mL (8.68 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

DMSO

	1mg	5mg	10mg	50mg
1 mM	4.3420 mL	21.7099 mL	43.4197 mL	217.0987 mL
5 mM	0.8684 mL	4.3420 mL	8.6839 mL	43.4197 mL
10 mM	0.4342 mL	2.1710 mL	4.3420 mL	21.7099 mL
20 mM	0.2171 mL	1.0855 mL	2.1710 mL	10.8549 mL
50 mM	0.0868 mL	0.4342 mL	0.8684 mL	4.3420 mL
100 mM	0.0434 mL	0.2171 mL	0.4342 mL	2.1710 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