p53 Activator 17
p53 Activator 17 is a p53-Y220C activator. p53 Activator 17 exhibits selective cytotoxicity and pro-apoptotic activity in p53-Y220C mutant cancer cell lines, with minimal effects in wild-type or p53-null cells. p53 Activator 17 induces a mutant-to-wild-type conformational shift in cellular p53-Y220C, accompanied by transcriptional activation of canonical p53 target genes, including BBC3 (PUMA) and MDM2. p53 Activator 17 can be used for the study of hepatocellular carcinoma and breast cancer.
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- Formule: C15H17BrN4
- Masse moléculaire:333.23
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
p53 Activator 17 (Compound JC36) (60 μM, 24 h) selectively induces a wild-type conformational change in the p53-Y220C mutant protein in HUH7 cells, but has no effect on wild-type p53 in MCF7 cells[1].
p53 Activator 17 (30-120 μM, 48 h) selectively inhibits the viability of HUH7 cells, MCF7 cells, and other cells carrying the p53-Y220C mutation[1].
p53 Activator 17 (60 μM, 48 h) significantly increases apoptosis in HUH7 p53-Y220C cells[1].
p53 Activator 17 (60 μM, 24 h) significantly increases the expression of p53 target genes in HUH7 p53-Y220C and MCF7 p53-Y220C cells[1].
p53 Activator 17 (60 μM, 24 h) increases the total p53 protein level in MCF7 p53-Y220C cells; no significant changes were observed in HUH7 p53-Y220C and MCF7 p53wt cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HUH7 p53-Y220C
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Concentration:60 μM
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Incubation Time:48 h
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Result:Significantly increased apoptosis in HUH7 p53-Y220C cells (total apoptotic cells increased by approximately 14-fold).
Apoptosis was increased but not significantly in MCF7 p53-Y220C; apoptosis increased by 1.9-fold in MCF7 p53wt.
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Cell Line:HUH7 p53-Y220C cells, MCF7 p53-Y220C cells
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Concentration:60 μM
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Incubation Time:24 h
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Result:Significantly increased expression of C3 (PUMA) and MDM2 in HUH7 p53-Y220C cells.
Significantly increased expression of BBC3 and CDKN1A (p21) in MCF7 p53-Y220C.
In MCF7 p53wt, MDM2 expression was increased, but BBC3 expression remained unchanged.
Chemical Information
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Masse moléculaire 333.23
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Formule C15H17BrN4
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SMILES
BrC1=CC=C2C(C(N3C=CC=C3)=NN2CCN(C)C)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
p53 Activator 17 Related Classifications
HY-179507 Related Classifications
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