Uses
Pifithrin-β (PFT β) is a potent p53 inhibitor with an IC50 of 23 μM.
Definition
ChEBI: 2-(4-methylphenyl)-5,6,7,8-tetrahydroimidazo[2,1-b][1,3]benzothiazole is a member of imidazoles.
General Description
A cell-permeable and very stable analog of Pifithrin-α (Cat. No.
506132), with similar biological function, but with reduced cytotoxicity. A chemical inhibitor of p53. Reversibly inhibits p53-dependent transactivation of p53-responsive genes; also reversibly blocks p53-mediated apoptosis. Acts as a P-gp modulator by changing relative substrate specificity of the transporter. This compound has been reported to be a potent STAT6 transcriptional inhibitor.
Biochem/physiol Actions
Cell permeable: yes
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. DOI:
10.1016/j.bmc.2011.01.039[2] Fernández-Cruz ML, et al. Biological and chemical studies on aryl hydrocarbon receptor induction by the p53 inhibitor pifithrin-α and its condensation product pifithrin-β. Life Sci. 2011 Apr 25;88(17-18):774-83. DOI:
10.1016/j.lfs.2011.02.019[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.
