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Pifithrin-a hydrobromide
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. Also aryl hydrocarbon receptor (AHR) agonist, causes upregulation of
AHR target gene CYP1A1 (EC50 = 1.1 μM).
Komarovet
al (1999) A chemical inhibitor of p53 that protects mice from the side
effects of cancer therapy. Science 285 1733. Komarova and
Gudkov (2000) Suppression of p53: a new approach to overcome side effects
of antitumor therapy. Biochemistry 6541. Culmseeet
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. Hoaglandet al (2005) The p53
inhibitor pifithrin-α is a potent agonist of the aryl hydrocarbon receptor.
J.Pharmacol.Exp.Ther. 314 603.
“Tocris is to be congratulated for continuing to meet the current demand for a rapid and reliable source of high-quality compounds that are urgently needed as pharmacological tools by a growing international population of cannabinoid researchers..”
