| 产品描述： | NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo |
| 靶点： |
NEDD8 activating enzyme (NAE) |
| 体外研究： |
M22 (0.37-90 μM; 24 h) blocks neddylation pathway selectively and suppresses degradation of CRL substrates in A549 cells. M22 (0.1-100 μM; 48 h) inhibits A549 cell proliferation completely at 30 µM (GI50=5.5 µM, GI90=19.3 µM). M22 (15-30 μM; 36 h) promotes apoptosis in A549 cell line. Cell Viability Assay Cell Line: A549 cells Concentration: 0.37, 1.11, 3.33, 10, 30, 90 μM Incubation Time: 24 hours Result: Inhibited formations of Uba3-NEDD8 and Ubc12-NEDD8.Resulted in a corresponding decrease in the abundance of Cullins-NEDD8.Decreased the degradations of p27 and CDT1.Prevented p53 from degradation. |
| 体内研究： |
M22 (60 mg/kg; i.p. once daily for 14 d) inhibits tumor growth in nude mice bearing AGS xenografts[1].M22 (0.36-90 μM) has low acute toxicity in zebrafish model |
| 参考文献： |
1. Lu P, et, al. Discovery of a novel NEDD8 Activating Enzyme Inhibitor with Piperidin-4-amine Scaffold by Structure-Based Virtual Screening. ACS Chem Biol. 2016 Jul 15;11(7):1901-7. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.752 ml |
13.762 ml |
27.523 ml |
| 5 mM |
0.55 ml |
2.752 ml |
5.505 ml |
| 10 mM |
0.275 ml |
1.376 ml |
2.752 ml |
| 50 mM |
0.055 ml |
0.275 ml |
0.55 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京