Chemical Name: 1-(4-Methylphenyl)-2-(4,5,6,7-tetrahydro-2-imino-3(2H)-benzothiazolyl)ethanone hydrobromide
Biological ActivityPifithrin-α hydrobromide is an 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).
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Tocris products are intended for laboratory research use only, unless stated otherwise.
A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy.
Komarov et al.
Suppression of p53: a new approach to overcome side effects of antitumor therapy.
Komarova and Gudkov
The p53 inhibitor, pifithrin-α, suppresses self-renewal of embryonic stem cells.
Abdelalim and Tooyama
The p53 inhibitor pifithrin-α is a potent agonist of the aryl hydrocarbon receptor.
Hoagland et al.
A synthetic inhibitor of p53 protects neurons against death induced by ischemic and excitotoxic insults, and amyloid β-peptide.
Culmsee et al.
Citations for Pifithrin-α hydrobromide
The citations listed below are publications that use Tocris products. Selected citations for Pifithrin-α hydrobromide include:
4 Citations: Showing 1 - 4
The ATPase activity of Asna1/TRC40 is required for pancreatic progenitor cell survival.
Authors: Norlin Et al.
Zinc deficiency causes neural tube defects through attenuation of p53 ubiquitylation.
Authors: Li Et al.
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
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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Reviews for Pifithrin-α hydrobromide
Average Rating: 5 (Based on 3 Reviews)
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The inhibitor worked nicely, and the results were consistent. We are happy with the quality of the product.
Pifithrin-alpha were dissolved in DMSO and used at a final concentration of 40 µM for pifithrin-alpha according to previous studies in which 3-100 µM pifithrin-alpha.
We used the p53 inhibitor in order to tackle the p53 protein in-vitro for some cellular proliferation assays,