Pifithrin-α hydrobromide

Biological Activity

Pifithrin-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).

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
   Fox JT, Sakamuru S, Huang R
   Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
2. PEPD is a pivotal regulator of p53 tumor suppressor
   L Yang, Y Li, A Bhattachar, Y Zhang
   Nat Commun, 2017;8(1):2052.
3. Novel Pactamycin Analogs Induce p53 Dependent Cell-Cycle Arrest at S-Phase in Human Head and Neck Squamous Cell Carcinoma (HNSCC) Cells.
   Guha G, Lu W, Li S, Liang X, Kulesz-Martin M, Mahmud T, Indra A, Ganguli-Indra G
   PLoS ONE, 2015;10(5):e0125322.
4. Regulators of Salmonella-host interaction identified by peripheral blood transcriptome profiling: roles of TGFB1 and TRP53 in intracellular Salmonella replication in pigs
   T Huang, X Huang, B Shi, F Wang, W Feng, M Yao
   Vet. Res., 2018;49(1):121.
5. A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy.
   Komarov et al.
   Science, 1999;285:1733
6. Suppression of p53: a new approach to overcome side effects of antitumor therapy.
   Komarova and Gudkov
   Biochemistry, 2000;65:41
7. The p53 inhibitor, pifithrin-α, suppresses self-renewal of embryonic stem cells.
   Abdelalim and Tooyama
   Biochem.Biophys.Res.Comm., 2012;420:605
8. The p53 inhibitor pifithrin-α is a potent agonist of the aryl hydrocarbon receptor.
   Hoagland et al.
   J.Pharmacol.Exp.Ther., 2005;314:603
9. A synthetic inhibitor of p53 protects neurons against death induced by ischemic and excitotoxic insults, and amyloid β-peptide.
   Culmsee et al.
   J.Neurochem., 2001;77:220

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