Catalog Number: 4240
Chemical Name: N3-[2-[[4-[Bis(4-chlorophenyl)methyl]-1-piperazinyl]methyl]-4-quinazolinyl]-N1,N1-dimethyl-1,3-propanediamine
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
  • Solubility:
    Soluble to 100 mM in ethanol and to 10 mM in DMSO with sonication
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    922150-11-6
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.
Background References
  1. 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.
    Demma et al.
    J.Biol.Chem., 2010;285:10198
  2. Translational approaches targeting the p53 pathway for anti-cancer therapy.
    Essmann & Schulze-Osthoff
    Br.J.Pharmacol., 2012;165:328

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