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) Biological Activity Technical Data Solubility Calculators DatasheetsReferences

Biological Activity

Restores mutant p53 activity. Binds p53 DNA binding domain (K_d = 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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Product Datasheets

Certificate of Analysis / Product Datasheet Safety Datasheet Select another language: English German French Spanish View SDS

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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Keywords: SCH 529074, supplier, SCH529074, p53, activates, restores, mutant, p53, activity, induces, apoptosis, Transcription, Factors, HDM2, p53, p53, Tocris Bioscience

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