货号 | 14748-50mg |
描述 | Pifithrin-α (PFT-α; Item No. 13326) is a reversible inhibitor of p53-dependent transcription and apoptosis.1 Cyclic PFT-α, also known as PFT-β, is a stable analog of PFT-α, formed by the condensation of pifithrin-α in solution.2 It inhibits the growth of the cancer cell lines IGROV-1, A2780, and HCT116 (IC50 = 23, 77, and 103 μM, respectively).3,2 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.4,5 In addition, 10 μM cyclic PFT-α blocks p53-dependent protection from DNA damage, induced by hydrogen peroxide or ultraviolet radiation, in melanocytes.6 |
别名 | Cyclic PFT-α;PFT-β;Pifithrin-β; |
供应商 | Cayman |
应用文献 | |
1.Komarov, P.G.,Komarova, E.A.,Kondratov, R.V., et al. A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy. Science 285, 1733-1737 (1999). 2.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. Molecular Cancer Therapeutics 4(9), 1369-1377 (2005). 3.Christodoulou, M.S.,Colombo, F.,Passarella, D., et al. Synthesis and biological evaluation of imidazolo[2,1-b]benzothiazole derivatives, as potential p53 inhibitors. Bioorganic & Medicinal Chemistry 19(5), 1649-1657 (2011). 4.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). 5.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). 6.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. Molecular Cancer Research 10(6), 778-786 (2012). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 349.3 |
分子式 | C16H16N2S • HBr |
CAS号 | 511296-88-1 |
稳定性 | ≥ 2 years |
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