| 货号 | 10748-5mg |
| 描述 | In addition to its transactivational functions, p53 mediates apoptosis by binding with the anti-apoptotic proteins Bcl-xL and Bcl-2 at the mitochondrial surface.1,2 Pifithrin-μ (PFT-μ) is an inhibitor of p53-mediated apoptosis, preventing p53 binding to Bcl-xL and Bcl-2 at the mitochondria without affecting p53 transactivational activities1 In vitro, PFT-μ binds both p53 (Kd = 0.82 mM) and Bcl-xL (Kd = 0.80 mM).3 PFT-μ reduces p53-mediated apoptosis induced by γ-radiation in mouse thymocytes in vitro and protects mice from doses of radiation that cause lethal hematopoietic syndrome. At 25 μM, PFT-μ reduces apoptosis triggered by nutlin-3, which inhibits MDM2/p53 binding and potentiates p53-mediated growth arrest and apoptosis.2 PFT-μ also interacts selectively with heat shock protein 70 (HSP70), leading to disruption of the association between HSP70 and many of its co-chaperones and substrate proteins.4 |
| 别名 | PFT-μ;2-Phenylethynesulfonamide; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Strom, E.,Sathe, S.,Komarov, P.G., et al. Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation. Nature Chemical Biology 2(9), 474-479 (2006). 2.Vaseva, A.V.,Marchenko, N.D., and Moll, U.M. The transcription-independent mitochondrial p53 program is a major contributor to nutlin-induced apoptosis in tumor cells. Cell Cycle 8(11), 1711-1719 (2009). 3.Hagn, F.,Klein, C.,Demmer, O., et al. BclxL changes conformation upon binding to wild-type but not mutant p53 DNA binding domain. The Journal of Biological Chemisty 285(5), 3439-3450 (2010). 4.Leu, J.I.,Pimkina, J.,Frank, A., et al. A small molecule inhibitor of inducible heat shock protein 70. Molecular Cell 36(1), 15-27 (2009). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 181.2 |
| 分子式 | C8H7NO2S |
| CAS号 | 64984-31-2 |
| 稳定性 | ≥ 2 years |
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