R&D Systems Inc. Tocris Bioscience Boston Biochem

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

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.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

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

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

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.

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.

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

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Keywords: Pifithrin-a hydrobromide, supplier, p53, inhibitors, aryl, hydrocarbon, receptors, agonists, AHR, Transcription, Factors, Pifithrin-alpha, hydrobromide

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