Pifithrin-α hydrobromide

Cat. No. 1267

Pifithrin-a hydrobromide C16H18N2OS.HBr [63208-82-2]

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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

Soluble to 100 mM in DMSO
Desiccate at -20°C

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.

Certificate of Analysis / Safety Data Sheet

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Abdelalim and Tooyama (2012) The p53 inhibitor, pifithrin-α, suppresses self-renewal of embryonic stem cells. Biochem.Biophys.Res.Comm. 420 605. PMID: 22445757.

Hoagland et al (2005) The p53 inhibitor pifithrin-α is a potent agonist of the aryl hydrocarbon receptor. J.Pharmacol.Exp.Ther. 314 603. PMID: 15843497.

Culmsee et al (2001) A synthetic inhibitor of p53 protects neurons against death induced by ischemic and excitotoxic insults, and amyloid β-peptide. J.Neurochem. 77 220. PMID: 11279278.

Komarova and Gudkov (2000) Suppression of p53: a new approach to overcome side effects of antitumor therapy. Biochemistry 65 41. PMID: 10702639.

Komarov et al (1999) A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy. Science 285 1733. PMID: 10481009.

If you know of a relevant reference for this product please let us know.

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

Guha et al (2015) Novel Pactamycin Analogs Induce p53 Dependent Cell-Cycle Arrest at S-Phase in Human Head and Neck Squamous Cell Carcinoma (HNSCC) Cells. PLoS One 10 e0125322. PMID: 25938491.

Fraser et al (2006) Regulation of p53 and suppression of apoptosis by the soluble guanylyl cyclase/cGMP pathway in human ovarian cancer cells. Cell Commun Signal 25 2203. PMID: 16288207.

Do you know of a great paper that uses Pifithrin-α hydrobromide from Tocris? If so please let us know.

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Keywords: Pifithrin-a hydrobromide, supplier, p53, inhibitors, inhibits, aryl, hydrocarbon, receptors, agonists, AHR, Transcription, Factors, Pifithrin-alpha, hydrobromide, Tocris Bioscience, p53 Inhibitor products

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