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Pifithrin-α hydrobromideCat. No. 1267 |
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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: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
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 '-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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