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GSK-3 inhibitor 4

Name: GSK-3 inhibitor 4
Brand: TargetMol
SKU: T77341
Price: 350 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T77341Cas No. 2227279-83-4

GSK-3 inhibitor 4 is an orally active and brain-permeable compound that acts as a triple inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM (CDK2), and 0.68 μM (CDK5). It effectively reduces Tau protein levels and can be used in the study of Alzheimer's disease.

GSK-3 inhibitor 4

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Purity: 99.82%

Catalog No. T77341Cas No. 2227279-83-4

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$350	In Stock	In Stock
5 mg	$970	In Stock	In Stock
10 mg	$1,200	In Stock	In Stock
25 mg	$1,590	In Stock	In Stock
50 mg	$1,980	In Stock	In Stock
100 mg	$2,500	-	In Stock
500 mg	$3,930	-	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.

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Purity:99.82%

Appearance:Solid

Color:Yellow

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	GSK-3 inhibitor 4 is an orally active and brain-permeable compound that acts as a triple inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM (CDK2), and 0.68 μM (CDK5). It effectively reduces Tau protein levels and can be used in the study of Alzheimer's disease.
Targets&IC50	GSK-3β:0.56 nM, CDK5:0.68 μM, GSK-3α:0.45 nM, CDK2:0.47 μM
In vitro	GSK-3 inhibitor 4 (compound 40) demonstrates excellent selectivity and efficacy against CDK2 (840-fold, IC50 = 0.47 μM), CDK5 (1200-fold, IC50 = 0.68 μM), GSK-3β (IC50 = 0.56 nM), and GSK-3α (IC50 = 0.45 nM). It also exhibits good permeability and a high capacity for binding to plasma proteins and brain tissue due to its lipophilicity.[1]
In vivo	GSK-3 inhibitor 4 (10 mg/kg; p.o.) reduced pTau396 by 37% when administered orally as a nanosuspension. GSK-3 inhibitor 4 (2 mg/kg, i.v.; 10 mg/kg, p.o.) exhibits low to moderate clearance (15.8 to 23.3 mL/min/kg) and is well absorbed orally in solution.[1]

Chemical Properties

Molecular Weight	403.38
Formula	C₂₂H₁₅F₂N₅O
Cas No.	2227279-83-4
Smiles	N(C(=O)C1=NC(NC2=CC=C(F)C=C2)=NC=C1)C=3C(=CC=NC3)C4=CC=C(F)C=C4
Relative Density.	1.401 g/cm3 at 20℃ (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 (123.95 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4791 mL	12.3953 mL	24.7905 mL	123.9526 mL
5 mM	0.4958 mL	2.4791 mL	4.9581 mL	24.7905 mL
10 mM	0.2479 mL	1.2395 mL	2.4791 mL	12.3953 mL
20 mM	0.1240 mL	0.6198 mL	1.2395 mL	6.1976 mL
50 mM	0.0496 mL	0.2479 mL	0.4958 mL	2.4791 mL
100 mM	0.0248 mL	0.1240 mL	0.2479 mL	1.2395 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