P53R3 是一种有效的 p53 reactivator，可恢复 p53 热点突变体（包括 p53^R175H、p53^R248W 和 p53^R273H）的序列特异性 DNA 结合。P53R3 以比 PRIMA-1 高得多的特异性诱导 p53 依赖性抗增殖作用。P53R3 增强了野生型 p53 和 p53^M237I 向几个靶基因启动子的募集。 P53R3 强烈增强死亡受体死亡受体 5 (DR5) 的 mRNA、总蛋白和细胞表面表达。 P53R3 可以用于癌症研究。

P53R3 is a potent p53 reactivator and restores sequence-specific DNA binding of p53 hot spot mutants, including p53, p53 and p53. P53R3 induces p53-dependent antiproliferative effects with much higher specificity than PRIMA-1. P53R3 enhances the recruitment of wild-type p53 and p53 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.

Solid

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

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

[1]. Alejandro Parrales, et al. Targeting Oncogenic Mutant p53 for Cancer Therapy. Front Oncol

In Vitro: DMSO : ≥ 100 mg/mL (168.76 mM)配制储备液