GSK-3β inhibitor 6
GSK-3β inhibitor 6 is a potent GSK-3β inhibitor with an IC50 value of 24.4 μM. GSK-3β inhibitor 6 shows high hepatocyte glucose uptake (38%). GSK-3β inhibitor 6 can be used in the research of numerous diseases like diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder.
For research use only. We do not sell to patients.
- CAS No.: 3033944-50-9
- Formula: C20H17BrN4
- Molecular Weight:393.28
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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 24.4 μM (IC50) |
GSK-3β inhibitor 6 (Compound B30, 0-30 μΜ, 30 min) shows good GSK-3β kinase inhibitory activity (IC50: 24.4 μM)[1].
GSK-3β inhibitor 6 (5 μM, 3 h) shows high hepatocyte glucose uptake (38%) with no significant toxicity against HepG2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats (pharmacokinetic assay)[2]
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Dosage:2 mg/kg, 20 mg/kg
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Administration:Intravenous injection (2 mg/kg), oral administration (20 mg/kg)
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Result:Pharmacokinetic profile of GSK-3β inhibitor 6 (Compound 5k).
F: oral bioavailability.Compound Route Dose (mg/kg) t1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (hr•ng/mL) AUC0-∞ (hr•ng/mL) CL (mL/hr/kg) F (%) GSK-3β inhibitor 6 Oral administration 20 1.41 1.33 288 1030 1073 18719 11.4 GSK-3β inhibitor 6 Intravenous injection 2 2.13 0.08 449 872.89 940.48 2190.83
Chemical Information
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CAS No. 3033944-50-9
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Molecular Weight 393.28
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Formula C20H17BrN4
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SMILES
CC1=CC=CC(C)=C1NC2=NC=CC(C3=CNC4=CC=C(C=C43)Br)=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
[1]. Shuwen Han, et al. Structural-Based Optimizations of the Marine-Originated Meridianin C as Glucose Uptake Agents by Inhibiting GSK-3β. Mar Drugs. 2021 Mar 12;19(3):149. [Content Brief]
[2]. Shuwen Han, et al. Structure-Based design of Marine-derived Meridianin C derivatives as glycogen synthase kinase 3β inhibitors with improved oral bioavailability: From aminopyrimidyl-indoles to the sulfonyl analogues. Bioorg Chem. 2022 Feb;119:105537. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GSK-3β inhibitor 6 Related Classifications
HY-143260 Related Classifications
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