Wnt-C59
货号：
16644-50mg 基本售价：
8330.0 元 规格：
50 mg
产品信息
概述| 货号 | 16644-50mg |
| 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 Wnt-C59 is a potent inhibitor of PORCN, as measured by prevention of Wnt3A activation (IC50 = 74 pM).2 As palmitoylation of Wnt is required for its secretion, Wnt-C59 completely blocks Wnt3A secretion into culture media.2 Wnt-C59 prevents activation of all evaluated Wnt family members.2 This compound is effective in vivo as well as in vitro. Whether given by intravenous (2.5 mg/kg) or oral administration (5 mg/kg), Wnt-C59 displays a half-life in blood of approximately 1.94 hours, and remains greater than 10-fold above the in vitroIC50 concentration for at least 16 hours after a single oral dose.2 It blocks the progression of both basal-like and triple-negative breast cancers while downregulating Wnt/β-catenin pathway target genes in mice.2,3 |
| 别名 | PORCN Inhibitor II; |
性能| 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.Wend, P.,Runke, S.,Wend, K., et al. WNT10B/β-catenin signalling induces HMGA2 and proliferation in metastatic triple-negative breast cancer. EMBO Mol.Med. 5(2), 264-279 (2013).
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| 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 | 379.5 |
| 分子式 | C25H21N3O |
| CAS号 | 1243243-89-1 |
| 稳定性 | ≥ 2 years |
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