Catalog Number: 1267
Chemical Name: 1-(4-Methylphenyl)-2-(4,5,6,7-tetrahydro-2-imino-3(2H)-benzothiazolyl)ethanone hydrobromide
Biological Activity
Inhibitor of p53; reversibly blocks p53-dependent transcriptional activation and apoptosis. Protects against neuronal death in models of stroke and neurodegenerative disorders. Active in vivo; protects mice from the side-effects of cancer therapy associated with p53 induction. Supresses self-renewal of embryonic stem cells. Also aryl hydrocarbon receptor (AHR) agonist, causes upregulation of AHR target gene CYP1A1 (EC50 = 1.1 μM). Cyclic analog available (Cat. No. 3843).
Technical Data
  • M.Wt:
    367.3
  • Formula:
    C16H18N2OS.HBr
  • Solubility:
    Soluble to 100 mM in DMSO
  • Storage:
    Desiccate at -20°C
  • CAS No:
    63208-82-2
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. A synthetic inhibitor of p53 protects neurons against death induced by ischemic and excitotoxic insults, and amyloid β-peptide.
    Culmsee et al.
    J.Neurochem., 2001;77:220
  2. The p53 inhibitor pifithrin-α is a potent agonist of the aryl hydrocarbon receptor.
    Hoagland et al.
    J.Pharmacol.Exp.Ther., 2005;314:603
  3. A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy.
    Komarov et al.
    Science, 1999;285:1733
  4. Suppression of p53: a new approach to overcome side effects of antitumor therapy.
    Komarova and Gudkov
    Biochemistry, 2000;65:41
  5. The p53 inhibitor, pifithrin-α, suppresses self-renewal of embryonic stem cells.
    Abdelalim and Tooyama
    Biochem.Biophys.Res.Comm., 2012;420:605
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Pifithrin-α hydrobromide include:

2 Citations: Showing 1 - 2
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  1. Novel Pactamycin Analogs Induce p53 Dependent Cell-Cycle Arrest at S-Phase in Human Head and Neck Squamous Cell Carcinoma (HNSCC) Cells.
    Authors: Guha Et al.
    PLoS One 2015;10:e0125322
  2. Regulation of p53 and suppression of apoptosis by the soluble guanylyl cyclase/cGMP pathway in human ovarian cancer cells.
    Authors: Fraser Et al.
    Cell Commun Signal 2006;25:2203

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