SCH 529074
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
| Solubility | Soluble 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.
| 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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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
If you know of a relevant reference for SCH 529074, please let us know.
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Citations for SCH 529074
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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 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.
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