2. Apoptosis
  3. MDM-2/p53 Apoptosis
  4. 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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p53 Activator 17

p53 Activator 17 Chemical Structure

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p53 Activator 17 Related Antibodies

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Description

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[1].

In Vitro

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.

p53 Activator 17 Related Antibodies

Apoptosis Analysis[1]

Cell Line: HUH7 p53-Y220C
Concentration: 60 μM
Incubation Time: 48 h
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.

Real Time qPCR[1]

Cell Line: HUH7 p53-Y220C cells, MCF7 p53-Y220C cells
Concentration: 60 μM
Incubation Time: 24 h
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.
Molecular Weight

333.23

Formula

C15H17BrN4
SMILES

BrC1=CC=C2C(C(N3C=CC=C3)=NN2CCN(C)C)=C1
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Room temperature in continental US; may vary elsewhere.
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p53 Activator 17 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

p53 Activator 17MDM-2/p53Apoptosisp53-Y220Cmutant p53 reactivationapoptosis inductionindazole derivativesInhibitorinhibitorinhibit

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