P53R3

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P53R3

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

922150-12-7

包装与价格：

包装	价格(元)
10mg	电议
25mg	电议

产品介绍

P53R3 是一种有效的 p53 reactivator，可恢复 p53 热点突变体（包括 p53R175H、p53R248W 和 p53R273H）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 p53M237I 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。

Cas No.

922150-12-7

分子式

C₃₂H₃₅Cl₂N₅O₂

分子量

592.56

溶解度

DMSO : ≥ 100 mg/mL (168.76 mM)

储存条件

4°C, stored under nitrogen

General tips

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

产品描述

P53R3 is a potentp53 reactivatorand restores sequence-specific DNA binding of p53 hot spot mutants, including p53^R175H, p53^R248W and p53^R273H. P53R3 induces p53-dependent antiproliferative effects with much higher specificity than PRIMA-1. P53R3 enhances the recruitment of wild-type p53 and p53^M237I to several target gene promoters. P53R3 strongly enhances the mRNA, total protein and cell surface expression of thedeath 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 p53^R273H(a DNA contact mutant) and p53R175H (a structural mutant) in WiDr colon tumour cells harbouring p53^R273H 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 p53^R175H-dependent effects are strong over a broad range of concentrations, but p53^R273H-dependent effects are weaker and requires high concentrations of P53R3^[1].
P53R3 induces p53^R248W reactivation is more pronounced proliferation inhibition than observed with p53^R273H. 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 p53^R175H and LN-308 p53^R273Hcells. But it does not affect cell cycle distribution of LN-308 p53^R248W 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 effectsin vitro.