GSK-3 inhibitor 4
Based on 1 Customer Validation
GSK-3 inhibitor 4 is an orally active and brain-penetrant inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM, and 0.68 μM, respectively. GSK-3 inhibitor 4 effectively reduces the phosphorylation level of Tau protein. GSK-3 inhibitor 4 can be used in Alzheimer's disease (AD) studies.
For research use only. We do not sell to patients.
- Purity: 99.02%
- CAS No.: 2227279-83-4
- Formula: C22H15F2N5O
- Molecular Weight:403.38
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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-3α 0.45 nM (IC50) |
GSK-3β 0.56 nM (IC50) |
CDK2 0.47 μM (IC50) |
CDK5 0.68 μM (IC50) |
GSK-3 inhibitor 4 (compound 40) exhibits excellent selectivity 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)[1].
GSK-3 inhibitor 4 has good permeability and exhibits a high ability to bind to plasma proteins and brain tissue due to its lipophilic nature[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GSK-3 inhibitor 4 (2 mg/kg, i.v.; 10 mg/kg, p.o.) exhibite low-moderate clearance ranging from 15.8 to 23.3 mL/min/kg and are well-absorbed when administered orally as a solution[1].
Pharmacokinetic Parameters of GSK-3 Inhibitor 4 (compound 40) in Mice[1]
| IV PK parameters | oral PK parameters | |||||
| CL (mL min-1 kg-1) | Vdss (L/kg) | MRT (h) | t1/2 (h) | AUCtot (μM h) | Cmax (μM) | F% |
| 18.9 | 2.6 | 2.3 | 2.8 | 11.7 | 1.5 | 53 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:3xTg mice were bred onto the C57BL6 background and bred as homozygotes. Male animals between the ages of five to seven months were used for the study[1].
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Dosage:10 mg/kg
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Administration:Oral gavage (p.o.)
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Result:Produced a 37% reduction in pTau396, when administered orally as a nanosuspension at a dose of 10 mg/kg.
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Animal Model:male C57BL6 mice (Pharmacokinetic assay)[1]
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Dosage:2 mg/kg, 10 mg/kg.
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Administration:Kept for 8 h fasting prior to formulation administration. intravenous and oral routes of administration to mice at a dose of 2 and 10 mg/kg, respectively.
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Result:Exhibited clearance ranging from 15.8 to 23.3 mL /min/kg , halflives ranging from 2.5 to 2.9 h and were readily orally bioavailable (F% = 53).
Chemical Information
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CAS No. 2227279-83-4
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Appearance Solid
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Molecular Weight 403.38
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Formula C22H15F2N5O
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Color Light yellow to yellow
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SMILES
O=C(C1=NC(NC2=CC=C(C=C2)F)=NC=C1)NC3=C(C4=CC=C(F)C=C4)C=CN=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GSK-3 inhibitor 4 Related Classifications
HY-154852 Related Classifications
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