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GSK854

Name: GSK854
Brand: TargetMol
SKU: T24115
Price: 84 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T24115Cas No. 1316059-00-3

Alias GSK-854, GSK 854

GSK854 is a highly selective and potent inhibitor of troponin I interacting kinase (TNNI3K) that inhibits myocardial infarction-injured cellular pyroptosis and apoptosis in mice, which may limit oxidative stress, injury, and adverse remodeling in the ischemic heart.

GSK854

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Purity: 98.91%

Catalog No. T24115Alias GSK-854, GSK 854Cas No. 1316059-00-3

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$84	In Stock	In Stock
5 mg	$198	In Stock	In Stock
10 mg	$328	In Stock	In Stock
25 mg	$653	In Stock	In Stock
50 mg	$993	In Stock	In Stock
100 mg	$1,550	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$272	In Stock	In Stock

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

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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Batch Information

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Purity:98.91%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

GSK854 AI Summary

GSK854 exhibits potent bioactivity in inhibiting TNNI3K, with an IC50 value of <= 10.0 nM for binding to human full-length TNNI3K and an IC50 of 8.0 nM for inhibiting TNNI3K autophosphorylation. It demonstrates high selectivity against BRAF, with an IC50 of 250.0 nM, and a selectivity index ratio of at least 25.0. The compound shows promising oral bioavailability in rat plasma at 48.0%, a moderate volume of distribution at steady state of 1.9 L/kg, and a relatively short half-life of 2.3 hours. Furthermore, notable drug uptake is observed in various tissues in mice, with concentrations of 0.4 μM in blood and 1.1 μM in the heart, indicating its potential therapeutic applications targeting TNNI3K..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	GSK854 is a highly selective and potent inhibitor of troponin I interacting kinase (TNNI3K) that inhibits myocardial infarction-injured cellular pyroptosis and apoptosis in mice, which may limit oxidative stress, injury, and adverse remodeling in the ischemic heart.
Synonyms	GSK-854, GSK 854

Chemical Properties

Molecular Weight	482.96
Formula	C₁₈H₁₉ClN₆O₄S₂
Cas No.	1316059-00-3
Smiles	CCS(=O)(=O)c1ccc(cc1Nc1cc(Nc2ccc(Cl)cn2)ncn1)S(=O)(=O)NC
Relative Density.	1.31g/cm3

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 100 mg/mL (207.06 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.28 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	2.0706 mL	10.3528 mL	20.7056 mL	103.5282 mL
5 mM	0.4141 mL	2.0706 mL	4.1411 mL	20.7056 mL
10 mM	0.2071 mL	1.0353 mL	2.0706 mL	10.3528 mL
20 mM	0.1035 mL	0.5176 mL	1.0353 mL	5.1764 mL
50 mM	0.0414 mL	0.2071 mL	0.4141 mL	2.0706 mL
100 mM	0.0207 mL	0.1035 mL	0.2071 mL	1.0353 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