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GSK-3 inhibitor 4
🥰Excellent
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
🥰Excellent
Purity: 98.77%
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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $350 | In Stock | |
| 5 mg | $970 | In Stock | |
| 10 mg | $1,200 | In Stock | |
| 25 mg | $1,590 | In Stock | |
| 50 mg | $1,980 | In Stock | |
| 100 mg | $2,500 | In Stock | |
| 500 mg | $3,930 | In Stock |
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Purity:98.77%
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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.Product Introduction
Bioactivity
Chemical Properties
| 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, GSK-3α:0.45 nM, CDK2:0.47 μM, CDK5:0.68 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] |
| 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 | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (123.95 mM)  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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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 mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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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
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