| 货号 | 14072-500ug |
| 描述 | Porcupine (PORCN) is a membrane bound O-acyltransferase that mediates palmitoylation of Wnt family proteins.1 This step is required for secretion and biologic activity of Wnt proteins, which have roles in embryonic development and cancer.1,2 LGK974 is a potent and specific small molecule inhibitor of PORCN (IC50 = 0.4 nM).3 It greatly reduces Wnt secretion without decreasing its synthesis and without increasing cytotoxicity.3 LGK974 is orally bioavailable in mice and induces tumor regression in mouse breast tumors produced by mammary tumor virus-driven Wnt1 signaling.3 It also blocks carcinogenesis in other Wnt-related tumors at doses that have limited impact on stem cell renewal.3,4,5 |
| 别名 | PORCN Inhibitor IV; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Gao, X. and Hannoush, R.N. Single-cell imaging of Wnt palmitoylation by the acyltransferase porcupine. Nature Chemical Biology 10(10), 61-68 (2014). 2.Proffitt, K.D.,Madan, B.,Ke, Z., et al. Pharmacological inhibition of the Wnt acyltransferase PORCN prevents growth of WNT-driven mammary cancer. Cancer Research 73(2), 502-507 (2013). 3.Liu, J.,Pan, S.,Hsieh, M.H., et al. Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974. Proceedings of the National Academy of Sciences of the United States of America 110(50), 20224-20229 (2013). 4.Jiang, X.,Hao, H.X.,Growney, J.D., et al. Inactivating mutations of RNF43 confer Wnt dependency in pancreatic ductal adenocarcinoma. Proceedings of the National Academy of Sciences of the United States of America 110(31), 12649-12654 (2013). 5.Lum, L. and Clevers, H. The unusual case of porcupine. Science 337, 922-923 (2012). | |
| 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 | 396.4 |
| 分子式 | C23H20N6O |
| CAS号 | 1243244-14-5 |
| 稳定性 | ≥ 2 years |
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