GTGKT
GTGKT is a CAGE inhibitor. GTGKT binds to CAGE and blocks the binding of CAGE to GSK3β. GTGKT alters the localization of CAGE and inhibits the binding of CAGE to the promoter sequence of Cyclin D1. GTGKT enhances the Apoptotic effect of anticancer agents. GTGKT reduces the expression of Cyclin D1. GTGKT decreases the tumorigenic potential of melanoma and hepatocellular carcinoma cells.
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- CAS. Nr.: 254732-11-1
- Formel: C18H34N6O8
- Molecular Weight:462.50
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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GSK-3β |
GTGKT (10 μM; 48 h) reduces the expressions of cyclinD1 and pGSK3βSer9, and inhibits the binding of CAGE-GSK3β in Malme3MR-Taxol cancer cells[1].
GTGKT (10 μM; 48 h) reduces the migration and invasion capacities of anticancer agent-resistant Malme3MR melanoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:anti-cancer agent-resistant Malme3MR, SNU387R, and Malme3MR-Taxol cancer cells
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Concentration:10 μM
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Incubation Time:48 h
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Result:Decreased the expression of cyclinD1 and inactive pGSK3βSer9 without altering CAGE expression in Malme3MR, SNU387R, and Malme3MR-Taxol cells.
Inhibited the binding of CAGE to GSK3β in all three cell lines.
Directly bound to CAGE (but not GSK3β) in Malme3MR and Malme3MR-Taxol cells for biotin-labeled peptide.
GTGKT (10-50 μg/mouse; i.v.; five times; 35 days) dose-dependently reduces subcutaneous hepatocellular carcinoma tumor volume in athymic nude mice by decreasing cyclinD1, pGSK3βSer9, and MDR1 expression, increasing phospho-cyclinD1Thr286 expression, and inhibiting CAGE-GSK3β binding[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nu/nu (5-6-week-old females)[1]
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Dosage:10 μg/mouse; 50 μg/mouse
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Administration:i.v.; five times; 35 days
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Result:Significantly reduced tumor volume compared to PBS control at 10 μg/mouse.
Resulted in a greater, statistically significant reduction in tumor volume compared to PBS control at 50 μg/mouse.
Decreased expression of cyclinD1, pGSK3βSer9, and MDR1 in tumor lysates.
Increased expression of phospho-cyclinD1Thr286 in tumor lysates.
Inhibited the binding of CAGE to GSK3β in tumor tissue.
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Animal Model:BALB/c nu/nu (5-6-week-old females)[1]
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Dosage:10 μg/mouse; 50 μg/mouse
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Administration:i.v.; five times; 35 days
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Result:Significantly reduced tumor volume compared to PBS control at 10 μg/mouse.
Significantly reduced tumor volume compared to PBS control at 50 μg/mouse, with greater efficacy than the lower dose.
Decreased expression of cyclinD1, pGSK3βSer9, and MDR1 in tumor lysates.
Increased expression of phospho-cyclinD1Thr286 in tumor lysates.
Inhibited the binding of CAGE to GSK3β in tumor tissue.
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Animal Model:BALB/c nu/nu (4-week-old females)[1]
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Dosage:50 μg/mouse
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Administration:i.v.; five times; 4 weeks
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Result:Drastically reduced the number of surface metastatic lung nodules compared to mock and GTGRT peptide controls.
Decreased expression of cyclinD1, pGSK3βSer9, and MDR1 in lung/tumor lysates.
Inhibited the binding of CAGE to GSK3β.
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Animal Model:BALB/c nu/nu (5-6-week-old females)[1]
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Dosage:50 μg/mouse
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Administration:i.v.; single dose
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Result:Detected strong, specific fluorescence in subcutaneous Malme3MR tumors 12 hours after injection.
Observed minimal fluorescence in normal organs (kidney, liver, spleen, lung) 12 hours after injection.
Chemical Information
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CAS. Nr. 254732-11-1
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Molecular Weight 462.50
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Formel C18H34N6O8
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Sequence
Gly-Thr-Gly-Lys-Thr
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Sequence Shortening
GTGKT
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
GTGKT Related Classifications
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