Wnt-C59 is a potent porcupine (PORCN) inhibitor. Wnt-C59 inhibits PORCN activity in vitro at nanomolar concentrations, as assessed by inhibition of Wnt palmitoylation, Wnt interaction with the carrier protein Wntless/WLS, Wnt secretion, and Wnt activation of -catenin reporter activity. In mice, Wnt-C59 displayed good bioavailability, as once daily oral administration was sufficient to maintain blood concentrations well above the IC(50). C59 blocked progression of mammary tumors in MMTV-WNT1 transgenic mice while downregulating Wnt/-catenin target genes. Porcupine (PORCN) is a membrane bound O-acyltransferase that is required for Wnt palmitoylation, secretion, and biologic activity.
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化学信息
| 名称 | Wnt-C59 |
| Iupac 化学名称 | Wnt-C59 |
| 同义词 | WntC59; Wnt-C 59; Wnt-C59 |
| 英文同义词 | WntC59; Wnt-C 59; Wnt-C59 |
| 分子式 | C25H21N3O |
| 分子量 | 379.45 |
| Smile | Cc1cc(ccn1)c2ccc(cc2)CC(=O)Nc3ccc(cc3)c4cccnc4 |
| InChiKey | KHZOJCQBHJUJFY-UHFFFAOYSA-N |
| InChi | InChI=1S/C25H21N3O/c1-18-15-22(12-14-27-18)20-6-4-19(5-7-20)16-25(29)28-24-10-8-21(9-11-24)23-3-2-13-26-17-23/h2-15,17H,16H2,1H3,(H,28,29) |
| Cas号 | 1243243-89-1 |
| MDL | MFCD22201167 |
| 相关CAS号 | |
| 外观性状 | crystalline solid |
| 纯度 | 98% |
| 存储 | 3 years -20ºCpowder |
| 可溶性 | Soluble in DMSO |
| 处理方式 | |
| 运输条件 | Shipped under ambient temperature as non-hazardous chemical. |
| 海关编码 | |
| Targets | |
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study | |