GSK3β-IN-4
GSK3β-IN-4 is a selective, potent, orally active and brain-penetrant ATP-competitive GSK3β inhibitor with an IC50 of 0.37 nM. GSK3β-IN-4 shows an IC50 of 2.75 nM and SI of 7.4 for GSK3α. GSK3β-IN-4 reduces tau phosphorylation at Ser396 by inhibiting GSK3β and imoroves cognitive deficits in Alzheimer's disease models. GSK3β-IN-4 can be used for the research of Alzheimer's disease.
For research use only. We do not sell to patients.
- CAS No.: 3083425-61-7
- Formula: C26H26N4O2
- Molecular Weight:426.51
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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GSK-3β 0.37 nM (IC50) |
GSK-3α 2.75 nM (IC50) |
GSK3β-IN-4 (Compound 39a) significantly inhibits Tau phosphorylation (EC50 = 0.06 μM) at Ser396 in Tau (P301L) 293T cells with low cytotoxicity (IC50= 80.75 μM)[1].
GSK3β-IN-4 inhibits GSK3β in an ATP-competitive manner with IC50 values of 1.27 nM, 7.14 nM, and 77.8 nM at 1 × Km, 10 × Km, and 100 × Km ATP concentrations, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GSK3β-IN-4 (5-25 mg/kg, p.o., daily for 14 days) imoroves cognitive deficits and tau Ser396 phosphorylation levels in an Okadaic acid (HY-N6785)-induced mouse model of Alzheimer's disease[1].
GSK3β-IN-4 (5 mg/kg, p.o., once daily for 60 days) meliorates spatial learning and memory impairments in 6-month-old 3×Tg-AD mice, reduces Tau Ser396 phosphorylation in the hippocampal CA3 region, with efficacy comparable to Donepezil (HY-14566) (5 mg/kg), and shows no impact on motor function[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (Okadaic acid-induced model of Alzheimer's disease)[1]
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Dosage:5 mg/kg, 25 mg/kg
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Administration:Orally administration
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Result:Reduced tau phosphorylation (pS396) in the hippocampus and temporal.
Reduced escape latency and improved spatial memory retention, as evidenced by increased time spent in the target quadrant and higher platform-crossing frequency.
Did not cause locomotor dysfunction.
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Animal Model:3×Tg-AD mice (transgenic model of Alzheimer's disease)[1]
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Dosage:5 mg/kg
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Administration:Orally administration
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Result:Improved spatial learning and memory deficits.
Reduced escape latency during hidden platform trials and increased time spent in the target quadrant during probe tests.
Revealed a reduction in pS396 tau levels in the hippocampal CA3 region.
Chemical Information
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CAS No. 3083425-61-7
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Molecular Weight 426.51
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Formula C26H26N4O2
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SMILES
O=C(C1CCCC1)NC2=C3C(C4=CC=C(C(N[C@@H](C5=CC=CC=C5)C)=O)C=C4N3)=CC=N2
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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)
GSK3β-IN-4 Related Classifications
HY-179723 Related Classifications
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