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

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.

For research use only. We do not sell to patients.

P53R3 Chemical Structure

P53R3 Chemical Structure

CAS No. : 922150-12-7

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Based on 1 publication(s) in Google Scholar

P53R3 Related Antibodies

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Description

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].

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].

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

P53R3 Related Antibodies

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.
Molecular Weight

592.56

Formula

C32H35Cl2N5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)[C@@H](C(OC)=O)NC1=C2C=CC=CC2=NC(CN3CCN(C(C4=CC=C(Cl)C=C4)C5=CC=C(Cl)C=C5)CC3)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (168.76 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: 99.94%

SDS (251 KB)

COA (251 KB) HNMR (197 KB) RP-HPLC (258 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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P53R3 Related Classifications

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.

Keywords:

P53R3922150-12-7MDM-2/p53p53R248W,?reactivationLN-308p53R273Hp53R175Hmutanttumorcancerp21GADD45BAXPUMAPIG3MDM2Inhibitorinhibitorinhibit

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