Cyclic Pifithrin-α (hydrobromide)

Cyclic PFT-α, also known as PFT-β, is a stable analog of PFT-α, formed by the condensation of pifithrin-α in solution.¹ It inhibits the growth of the cancer cell lines IGROV-1, A2780, and HCT116 (IC₅₀ = 23, 77, and 103 μM, respectively).^1,2 At doses lower than those that inhibit growth, cyclic PFT-α induces autophagy in HCT116 cells and sensitizes IGROV-1 and H460 cells to anti-microtubule agents.^3,4 In addition, 10 μM cyclic PFT-α blocks p53-dependent protection from DNA damage, induced by hydrogen peroxide or ultraviolet radiation, in melanocytes.⁵

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1. Walton, M.I., Wilson, S.C., Hardcastle, I.R., et al. An evaluation of the ability of pifithrin-α and -β to inhibit p53 function in two wild-type p53 human tumor cell lines. Mol. Cancer Ther. 4(9), 1369-1377 (2005).

2. Christodoulou, M.S., Colombo, F., Passarella, D., et al. Synthesis and biological evaluation of imidazolo[2,1-b]benzothiazole derivatives, as potential p53 inhibitors. Bioorg. Med. Chem. 19(5), 1649-1657 (2011).

3. Tasdemir, E., Maiuri, M.C., Orhon, I., et al. p53 represses autophagy in a cell cycle-dependent fashion. Cell Cycle 7(19), 3006-3011 (2008).

4. Zuco, V., and Zunino, F. Cyclic pifithrin-α sensitizes wild type p53 tumor cells to antimicrotubule agent-induced apoptosis. Neoplasia 10(6), 587-596 (2008).

5. Kadekaro, A.L., Chen, J., Yang, J., et al. Alpha-melanocyte-stimulating hormone suppresses oxidative stress through a p53-mediated signaling pathway in human melanocytes. Mol. Cancer Res. 10(6), 778-786 (2012).