P53R3

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

P53R3 是一种新型 p53 重激活剂，可在凝胶迁移测定中恢复内源表达的 p53(R175H) 和 p53(R273H) 突变体的序列特异性 DNA 结合。

P53R3 is a novel p53 reactivator that restores sequence-specific DNA binding of the endogenously expressed p53(R175H) and p53(R273H) mutants in gel-shift assays; induces p53-dependent antiproliferative effects with much higher specificity and over a wider range of concentrations than PRIMA-1; strongly enhances the mRNA, total protein and cell surface expression of DR5.

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.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.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).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. Cell Viability AssayCell 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.

——

——

Apoptosis

MDM2-p53

MDM2-p53

——

——

922150-12-7

592.565

C32H35Cl2N5O2

>98% (HPLC)

In Vitro:?DMSO : ≥ 100 mg/mL (168.76 mM)

——

methyl (2-((4-(bis(4-chlorophenyl)methyl)piperazin-1-yl)methyl)quinazolin-4-yl)-L-valinate

(-20℃)

With Ice Pack

≥ 2 years