AChE/GSK-3β-IN-1
AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research.
For research use only. We do not sell to patients.
- CAS No.: 2412364-73-7
- Formula: C31H35N7O3S
- Molecular Weight:585.72
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
AChE/GSK-3β-IN-1 (compound GT15) (300 nM) has strong binding affinities with GSK3 family and exhibits a potent inhibitory activity against dual tyrosine phospho-regulated kinase 1 (DYRK1) (DYRK1α and DYRK1β with IC50 of 28.3 nM and 119.7 nM, respectively)[1].
AChE/GSK-3β-IN-1 (compound GT15) (5-15 µM; 1 hours; N2a-tau cells) exhibits good permeability across the blood-brain-barrier and ability to inhibit the phosphorylation of tau protein[1].
AChE/GSK-3β-IN-1 (compound GT15) (5 µM; BV2 cells) prevents the increase of ROS caused by LPS and reduces oxidative stress[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:N2a-tau cells
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Concentration:5, 10, and 15 µM
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Incubation Time:6 hours
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Result:Decreased the level of phosphorylated tau protein was reduced to 49% at 5 µM and 17% at 15 µM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR male mice[1]
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Dosage:15 mg/kg
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Administration:Oral administration
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Result:Improved the cognitive impairment of the mice.
Chemical Information
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CAS No. 2412364-73-7
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Molecular Weight 585.72
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Formula C31H35N7O3S
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SMILES
CNC(C(S1)=C(N=C1C2=CC(NC(CNCCNC3=C4CCCCC4=NC5=CC=CC=C35)=O)=NC=C2)OCC6CC6)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AChE/GSK-3β-IN-1 Related Classifications
HY-150537 Related Classifications
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