L14-8
L14-8 is a potent ferroptosis inducer. L14-8 promotes PLK1 degradation via ubiquitination, increasing TP53 phosphorylation to enhance SAT1 transcription, thereby triggering ferroptosis and cancer cell death. L14-8 can be used for the study of advanced prostate cancer.
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- Fòrmula: C30H25F2NO5
- Peso molecular:517.52
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
L14-8 (5-25 μM, 48 h) results in over 80% cell death in both C4-2B and 22Rv1 cells at 25 μM and does not significantly affect normal prostate cell growth[1].
L14-8 (10 μM, 24-48 h) induces ferroptosis by transcriptionally activating SAT1 expression and increase MDA level in C4-2B and 22Rv1 cells[1].
L14-8 (0-10 μM, 0-24 h) binds to PLK1 and enhances PLK1-mediated TP53 phosphorylation and expression, which is required for SAT1 transcription activation in C4-2B and 22Rv1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:C4-2B and 22Rv1 cells
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Concentration:5 and 7.5 μM
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Incubation Time:72 h
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Result:Significantly rescued the inhibitory effect of L14-8 on the viability of C4-2B and 22Rv1 cells.
Significantly reduced the sensitivity of the cells after knocking out TP53.
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Cell Line:C4-2B and 22Rv1 cells
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Concentration:10 μM
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Incubation Time:48 h
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Result:Dramatically increased the the expression of ferroptosis-related genes SAT1.
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Cell Line:C4-2B and 22Rv1 cells
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Concentration:0, 1, 2, 4, 8, 12 and 24 h
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Incubation Time:72 h
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Result:Significantly increased the thermal stability of endogenous PLK1.
Led to an increase in the protein levels of TP53 and phosphorylated TP53 (p-TP53) .
Significantly shortened the half-life of PLK1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C4-2B cells xenografted model established in male 4-week-old BALB/c nude mice[1]
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Dosage:10 and 20 mg/kg
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Administration:Intraperitoneal injection (i.p.), once daily for 25 days
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Result:Significantly suppressed tumor growth in a dose-dependent manner.
Decreased cancer proliferation.
Had no changes in major organs such as the heart, kidney, liver, lung, and spleen with high doses.
Had similar liver and kidney function indices between vehicle treatment in lower doses.
Chemical Information
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Peso molecular 517.52
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Fòrmula C30H25F2NO5
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SMILES
FC1=CC=C([C@@H](OC(C=C)=O)CC[C@@H]2[C@@H](C3=CC=C(OC(C=C)=O)C=C3)N(C4=CC=C(F)C=C4)C2=O)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
L14-8 Related Classifications
HY-175000 Related Classifications
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