Pifithrin-α hydrobromide

Product Description

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).

Solubility

Preparing Stock Solutions for Pifithrin-α hydrobromide

The following data is based on the product molecular weight 367.30

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.72 mL	13.61 mL	27.23 mL
5 mM	0.54 mL	2.72 mL	5.45 mL
10 mM	0.27 mL	1.36 mL	2.72 mL
50 mM	0.05 mL	0.27 mL	0.54 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Abdelalim and Tooyama The p53 inhibitor, pifithrin-α, suppresses self-renewal of embryonic stem cells. Biochem.Biophys.Res.Comm. 2012 PMID: 22445757
• Komarova and Gudkov Suppression of p53: a new approach to overcome side effects of antitumor therapy. Biochemistry 2000 PMID: 10702639
• Hoagland The p53 inhibitor pifithrin-α is a potent agonist of the aryl hydrocarbon receptor. J.Pharmacol.Exp.Ther. 2005 PMID: 15843497
• Komarov A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy. Science 1999 PMID: 10481009
• Culmsee A synthetic inhibitor of p53 protects neurons against death induced by ischemic and excitotoxic insults, and amyloid β-peptide. J.Neurochem. 2001 PMID: 11279278