产品说明书
LGK974
 |
同义名 : | WNT974;PORCN Inhibitor IV;NVP-LGK974 |
| CAS号 : | 1243244-14-5 | |
| 货号 : | A169157 | |
| 分子式 : | C23H20N6O | |
| 纯度 : | 99%+ | |
| 分子量 : | 396.445 | |
| MDL号 : | MFCD27501026 | |
| 存储条件： |
粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 30 mg/mL(75.67 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
IP 2% DMSO+2% Tween80+30% PEG300+water 3.6 mg/mL clear PO 0.5% CMC-Na 86 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 描述 | LGK974, known as WNT974, represents a highly specific and orally bioavailable inhibitor of Porcupine (PORCN), a key enzyme involved in the post-translational modification of Wnt proteins, with an impressive IC50 of 0.1 nM[1]. | ||
| 作用机制 | LGK interacts with PORCN to inhibit its acyltransferase activity. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| 293T | Function Assay | IC50 of 1 nM to compete off [3H]-GNF-1331 in a dose-dependent manner | 24277854 | ||
| 293T | Function Assay | IC50 of 0.4 nM to inhibits Wnt signaling in the aforementioned Wnt coculture assay | 24277854 | ||
| Capan-2 | 1 μM | Growth Inhibition Assay | inhibits the growth of pancreatic cancer cell lines with RNF43 mutation | 23847203 | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.52mL 0.50mL 0.25mL |
12.61mL 2.52mL 1.26mL |
25.22mL 5.04mL 2.52mL |
| 参考文献 |
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