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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。
P53R3图片
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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation 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 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 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 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 p53R273Hcells. 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 effectsin vitro.