1. Apoptosis
  2. MDM-2/p53
  3. P53R3

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。

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P53R3 Chemical Structure

P53R3 Chemical Structure

CAS No. : 922150-12-7

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
分子量

592.56

Formula

C32H35Cl2N5O2

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

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

溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 100 mg/mL (168.76 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6876 mL 8.4380 mL 16.8759 mL
5 mM 0.3375 mL 1.6876 mL 3.3752 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.94%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6876 mL 8.4380 mL 16.8759 mL 42.1898 mL
5 mM 0.3375 mL 1.6876 mL 3.3752 mL 8.4380 mL
10 mM 0.1688 mL 0.8438 mL 1.6876 mL 4.2190 mL
15 mM 0.1125 mL 0.5625 mL 1.1251 mL 2.8127 mL
20 mM 0.0844 mL 0.4219 mL 0.8438 mL 2.1095 mL
25 mM 0.0675 mL 0.3375 mL 0.6750 mL 1.6876 mL
30 mM 0.0563 mL 0.2813 mL 0.5625 mL 1.4063 mL
40 mM 0.0422 mL 0.2109 mL 0.4219 mL 1.0547 mL
50 mM 0.0338 mL 0.1688 mL 0.3375 mL 0.8438 mL
60 mM 0.0281 mL 0.1406 mL 0.2813 mL 0.7032 mL
80 mM 0.0211 mL 0.1055 mL 0.2109 mL 0.5274 mL
100 mM 0.0169 mL 0.0844 mL 0.1688 mL 0.4219 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
P53R3
目录号:
HY-122578
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