Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK-3 inhibitor 4 is an orally active and brain-permeable triple inhibitor of GSK-3, CDK2 and CDK5 with inhibitory effects on GSK-3β, GSK-3α, CDK2 and CDK5, with IC50 values of 0.56 nM, 0.45 nM, 0.47 μM, 0.68 μM, respectively.GSK-3 inhibitor 4 can effectively reduce Tau protein levels. GSK-3 inhibitor 4 can effectively reduce the level of Tau protein.GSK-3 inhibitor 4 can be used in the study of Alzheimer's disease.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 350.00 | |
5 mg | In stock | $ 970.00 | |
10 mg | In stock | $ 1,200.00 | |
25 mg | In stock | $ 1,590.00 | |
50 mg | In stock | $ 1,980.00 | |
100 mg | In stock | $ 2,500.00 | |
500 mg | In stock | $ 3,930.00 |
Description | GSK-3 inhibitor 4 is an orally active and brain-permeable triple inhibitor of GSK-3, CDK2 and CDK5 with inhibitory effects on GSK-3β, GSK-3α, CDK2 and CDK5, with IC50 values of 0.56 nM, 0.45 nM, 0.47 μM, 0.68 μM, respectively.GSK-3 inhibitor 4 can effectively reduce Tau protein levels. GSK-3 inhibitor 4 can effectively reduce the level of Tau protein.GSK-3 inhibitor 4 can be used in the study of Alzheimer's disease. |
Targets&IC50 | GSK-3α:0.45 nM, CDK5:0.68 μM, CDK2:0.47 μM, GSK-3β:0.56 nM |
In vitro |
GSK-3 inhibitor 4 (compound 40) is effective 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) exhibits excellent selectivity.[1] GSK-3 inhibitor 4 has good permeability and shows a high ability to bind 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 the nanosuspension was administered orally at a dose of 10 mg/kg.[1] GSK-3 inhibitor 4 (2 mg/kg, i.v.; 10 mg/kg, p.o.) exhibits low-moderate clearance, ranging from 15.8 to 23.3 mL/min/kg, and is well absorbed when administered orally as a solution.[1] |
Molecular Weight | 403.38 |
Formula | C22H15F2N5O |
CAS No. | 2227279-83-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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GSK-3 inhibitor 4 2227279-83-4 Cell Cycle/Checkpoint PI3K/Akt/mTOR signaling Stem Cells GSK-3 CDK GSK3inhibitor4 inhibitor inhibit