Pifithrin-β (hydrobromide)

Pifithrin-β is a potent p53 inhibitor with an IC50 of 23 μM.

Signaling Pathways >> Apoptosis >> MDM-2/p53

Research Areas >> Cancer

IC50: 23 μM (p53)[1]

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].

[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.

Pifithrin-α hydrobromide | RG7388 | Nutlin-3a | AMG232 | Stylomycin aminonucleoside | RG7112 | APR-246 | NVP-HDM201 | SAR 405838 | RITA (NSC 652287) | NVP-CGM097 | Tenovin-1 | SJ 172550 | CBL0137 HCl