SCH 529074

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Cat.No. 4240 - SCH 529074 | C31H36Cl2N6 | CAS No. 922150-11-6
Description: Restores mutant p53 activity
Chemical Name: N3-[2-[[4-[Bis(4-chlorophenyl)methyl]-1-piperazinyl]methyl]-4-quinazolinyl]-N1,N1-dimethyl-1,3-propanediamine
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature
Pathways

Biological Activity

Restores mutant p53 activity. Binds p53 DNA binding domain (Kd = 1-2 μM) and restores wild-type function to many oncogenic mutants by acting as a chaperone. Inhibits ubiquitination of p53 by HDM2. Triggers apoptosis in tumor cell lines and reduces tumor growth in a xenograft model.

Technical Data

M. Wt 563.56
Formula C31H36Cl2N6
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 922150-11-6
PubChem ID 12001922
InChI Key NCAJLQDPTZBGJV-UHFFFAOYSA-N
Smiles CN(C)CCCNC2=NC(CN3CCN(C(C5=CC=C(Cl)C=C5)C4=CC=C(Cl)C=C4)CC3)=NC1=CC=CC=C12

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

SolubilitySoluble to 100 mM in ethanol and to 10 mM in DMSO with sonication

Preparing Stock Solutions

The following data is based on the product molecular weight 563.56. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.77 mL 8.87 mL 17.74 mL
5 mM 0.35 mL 1.77 mL 3.55 mL
10 mM 0.18 mL 0.89 mL 1.77 mL
50 mM 0.04 mL 0.18 mL 0.35 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Demma et al (2010) SCH529074, a small molecule activator of mutant p53, which binds p53 DNA binding domain (DBD), restores growth-suppressive function to mutant p53 and interrupts HDM2-mediated ubiquitination of wild type p53. J.Biol.Chem. 285 10198 PMID: 20124408

Essmann & Schulze-Osthoff (2012) Translational approaches targeting the p53 pathway for anti-cancer therapy. Br.J.Pharmacol. 165 328 PMID: 21718309


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Citations for SCH 529074

Citations are publications that use Tocris products.

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.

Pathways for SCH 529074

p53

p53 Signaling Pathway

p53 signaling plays an important role in the co-ordination of the cellular response different types of stress such as DNA damage and hypoxia. The downstream signals lead to apoptosis, senescence and cell cycle arrest.

Protocols

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