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.
For research use only. We do not sell to patients.
- Formula: C15H17BrN4
- Molecular Weight:333.23
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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
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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Molecular Weight 333.23
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Formula C15H17BrN4
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SMILES
BrC1=CC=C2C(C(N3C=CC=C3)=NN2CCN(C)C)=C1
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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)
p53 Activator 17 Related Classifications
HY-179507 Related Classifications
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