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P53R3

Catalog No.GC65961

P53R3 is a potent p53 reactivator and restores sequence-specific DNA binding of p53 hot spot mutants, including p53R175H, p53R248W and p53R273H. P53R3 induces p53-dependent antiproliferative effects with much higher specificity than PRIMA-1. P53R3 enhances the recruitment of wild-type p53 and p53M237I to several target gene promoters. P53R3 strongly enhances the mRNA, total protein and cell surface expression of the death receptor death receptor 5 (DR5). P53R3 is used for cancer research.

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P53R3 Chemical Structure

Cas No.: 922150-12-7

Size Price Stock Qty
10mg
$540.00
In stock
25mg
$1,035.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents

P53R3 is a potent p53 reactivator and restores sequence-specific DNA binding of p53 hot spot mutants, including p53R175H, p53R248W and p53R273H. P53R3 induces p53-dependent antiproliferative effects with much higher specificity than PRIMA-1. P53R3 enhances the recruitment of wild-type p53 and p53M237I to several target gene promoters. P53R3 strongly enhances the mRNA, total protein and cell surface expression of the death receptor death receptor 5 (DR5). P53R3 is used for cancer research[1].

P53R3 (10 μg/ml; 24 hours; in the absence or presence of the unlabelled p53 consensus oligonucleotide) restores p53-specific DNA binding activity to p53R273H (a DNA contact mutant) and p53R175H (a structural mutant) in WiDr colon tumour cells harbouring p53R273H and KLE cells with p53R175H[1].
P53R3 (1-33 μg/ml; 24 hours) inhibits the proliferation of the LN-308 sublines expressing mutant p53 plasmids in a p53-dependent manner. The p53R175H-dependent effects are strong over a broad range of concentrations, but p53R273H-dependent effects are weaker and requires high concentrations of P53R3[1].
P53R3 induces p53R248W reactivation is more pronounced proliferation inhibition than observed with p53R273H. P53R3 does not exhibit cytotoxic effects even at concentrations close to its solubility limit (33 μg/ml)[1].
P53R3 (33 μg/ml; 18 hours) induces a strong decrease in S phase cells and a G0/G1 cell cycle arrest in LN-308 p53R175H and LN-308 p53R273H cells. But it does not affect cell cycle distribution of LN-308 p53R248W cells[1].

Cell Viability Assay[1]

Cell Line: p53 null LN-308 human glioma cells with a control plasmid or plasmids encoding the mutants p53R175H, p53R248W and p53R273H
Concentration: 1-33 μg/mL
Incubation Time: 24 hours
Result: Induced p53-dependent and -independent antiproliferative and cytotoxic effects in vitro.

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