LGK974, aslo known as is a selective and orally bioavailable Porcupine (PORCN) inhibitor under development for the treatment of cancers that are driven by the Wnt pathway in a Wnt ligand-dependent manner. WNT974 binds to and inhibits PORCN in the endoplasmic reticulum (ER), which blocks post-translational acylation of Wnt ligands and inhibits their secretion. This prevents the activation of Wnt ligands, interferes with Wnt-mediated signaling, and inhibits cell growth in Wnt-driven tumors. Porcupine, a membrane-bound O-acyltransferase (MBOAT), is required for the palmitoylation of Wnt ligands, and plays a key role in Wnt ligand secretion and activity. Wnt signaling is dysregulated in a variety of cancers.
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化学信息
名称 | LGK974 (WNT974) |
Iupac 化学名称 | 2-(2',3-dimethyl-[2,4'-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide |
同义词 | LGK-974;LGK 974;WNT974;WNT 974;WNT-974 |
英文同义词 | LGK-974;LGK 974;WNT974;WNT 974;WNT-974 |
分子式 | C23H20N6O |
分子量 | 396.44 |
Smile | CC1=NC=CC(=C1)C1=NC=C(C=C1C)CC(=O)NC1=NC=C(C=C1)C1=NC=CN=C1 |
InChiKey | XXYGTCZJJLTAGH-UHFFFAOYSA-N |
InChi | InChI=1S/C23H20N6O/c1-15-9-17(12-28-23(15)18-5-6-25-16(2)10-18)11-22(30)29-21-4-3-19(13-27-21)20-14-24-7-8-26-20/h3-10,12-14H,11H2,1-2H3,(H,27,29,30) |
Cas号 | 1243244-14-5 |
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 | |