GSK-3β-IN-28
GSK-3β inhibitor 28 is selective and non-competitivea glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 14.82 nM. GSK-3β inhibitor 28 can upregulate the expression level of phosphorylated GSK-3β and downregulate the expression of p-NF-κB, P65, C-myc and Cyclin D1. GSK-3β inhibitor 28 can induce cells apoptosis, G1 phase arrest and inhibit migration. GSK-3β inhibitor 28 can be used for the research of cancer, such as colorectal cancer.
For research use only. We do not sell to patients.
- Formula: C21H16ClN3O3S
- Molecular Weight:425.89
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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GSK-3β 14.82 nM (IC50) |
GSK-3β inhibitor 28 (Compound 7f) shows strong inhibitory activity against SW480, MDA-MB-231, and A549 cells with IC50 values of 14.58, 14.61, 19.15 μM, and weak activity against MoLM13 (IC50 = 25.75 μM) and HepG2 (IC50 = 51.51 μM) cells[1].
GSK-3β inhibitor 28 (1 μM) exhibits good selectivity against most kinases (MAPK, EGFR, Src) except GSK-3α, showing only a moderate inhibition rate (58.0%) against GSK-3α[1].
GSK-3β inhibitor 28 (0.78-25 μM, 72 h) shows IC50 values >25μM against LX-2 (hepatic stellate cells) and MIHA (normal hepatocytes) cells[1].
GSK-3β inhibitor 28 (5-20 μM, 24 h) inhibits migration and reduces colony numbers in SW480 cells[1].
GSK-3β inhibitor 28 (5-20 μM, 24 h) induces apoptosis and G1 phase arrest in SW480 cells[1].
GSK-3β inhibitor 28 (10-20 μM) upregulates p-GSK-3β expression and downregulates the expression of p-NF-κB, P65, C-myc, Cyclin D1, and XIAP proteins in SW480 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW480 cells
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Concentration:5, 10 and 20 μM
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Incubation Time:24 h
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Result:Increased proportion of cells in G1 phase.
Decreased proportions in S and G2 phases.
Chemical Information
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Molecular Weight 425.89
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Formula C21H16ClN3O3S
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SMILES
O=C(N1CCC2=CC=CC=C2)N(C3=CC4=C(N(C(C=C)=O)C=C4Cl)C=C3)SC1=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)