Introduction：Basic information about CAS 511296-88-1|Pifithrin-β (hydrobromide), including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Pifithrin-β is a potent p53 inhibitor with an IC50 of 23 μM.
Related Catalog
Signaling Pathways >>Apoptosis >>MDM-2/p53Research Areas >>Cancer
Target
IC50: 23 μM (p53)[1]
In Vitro
Pifithrin-α, an inhibitor of the p53 protein, is regarded as a lead compound for cancer and neurodegenerative disease therapy. Pifithrin-α is very unstable in culture medium and rapidly converts to its condensation product pifithrin-β, the N-acetyl derivative[2]. After 24 h, the viability assay shows that the pretreatments with 1 and 10 μM pifithrin-β exerts neuroprotective effects[3].
References
[1]. Christodoulou MS, et al. Synthesis and biological evaluation of imidazolo[2,1-b]benzothiazole derivatives, as potential p53 inhibitors. Bioorg Med Chem. 2011 Mar 1;19(5):1649-57.
[2]. Fernández-Cruz ML, et al. Biological and chemical studies on aryl hydrocarbon receptor induction by the p53 inhibitor pifithrin-α and its condensation productpifithrin-β. Life Sci. 2011 Apr 25;88(17-18):774-83.
[3]. Da Pozzo E, et al. p53 functional inhibitors behaving like pifithrin-β counteract the Alzheimer peptide non-β-amyloid component effects in human SH-SY5Y cells. ACS Chem Neurosci. 2014 May 21;5(5):390-9.
p53 mediates cigarette smoke-induced apoptosis of pulmonary endothelial cells: inhibitory effects of macrophage migration inhibitor factor.
Am. J. Respir. Cell. Mol. Biol. 44 , 323-32, (2011)
Exposure to cigarette smoke (CS) is the most common cause of emphysema, a debilitating pulmonary disease histopathologically characterized by the irreversible destruction of lung architecture. Mountin...
