| 货号 | 17214-1mg |
| 描述 | Peptidyl-prolyl isomerases (PPIases) assist in the folding of newly-synthesized proteins, regulating the stability, localization, and activity of mature proteins.1 PPIase-Parvulin Inhibitor is a cell-permeable inhibitor of the PPIases Pin1 and Pin4 (IC50s = 1.5 and 1.0 µM, respectively), interacting with the PPIase domain.2 It blocks the proliferation of cancer cells that overexpress Pin1 and Pin4 (IC50 range = 2-5 µM), and similarly inhibits wild type mouse embryonic fibroblasts (MEFs) but not Pin1-/-MEFs.2 PPIase-Parvulin Inhibitor does not inhibit topoisomerase I or bind DNA. Also referred to as PiB, this compound is commonly used to determine the role of Pin1 in regulating various substrates and cellular functions.3,4,5,6 |
| 别名 | HIC 016C;PiB; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Hanes, S.D. Prolyl isomerases in gene transcription. Biochimica et Biophysica Acta (2014). 2.Uchida, T.,Takamiya, M.,Takahashi, M., et al. Pin1 and Par14 peptidyl prolyl isomerase inhibitors block cell proliferation. Chemistry & Biology 10(1), 15-24 (2003). 3.Farrell, A.S.,Pelz, C.,Wang, X., et al. Pin1 regulates the dynamics of c-Myc DNA binding to facilitate target gene regulation and oncogenesis. Molecular and Cellular Biology 33(15), 2930-2949 (2015). 4.Ghosh, A.,Saminathan, H.,Kanthasamy, A., et al. The peptidyl-prolyl isomerase Pin1 up-regulation and proapoptotic function in dopaminergic neurons: Relevance to the pathogenesis of Parkinson disease. The Journal of Biological Chemisty 288(30), 21955-21971 (2013). 5.Rustighi, A.,Zannini, A.,Tiberi, L., et al. Prolyl-isomerase Pin1 controls normal and cancer stem cells of the breast. EMBO Mol.Med. 6(1), 99-119 (2014). 6.Antonelli, R.,Pizzarelli, R.,Pedroni, A., et al. Pin1-dependent signalling negatively affects GABAergic transmission by modulating neuroligin2/gephyrin interaction. Nat.Commun. 5, 1-14 (2014). | |
| 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 | 438.4 |
| 分子式 | C22H18N2O8 |
| CAS号 | 64005-90-9 |
| 稳定性 | ≥ 2 years |
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