CAS NO: | 864420-54-2 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
Cas No. | 864420-54-2 |
Canonical SMILES | ClC1=CC=C(CCNC2CCN(CC3=CC=CC=C3)CC2)C(Cl)=C1 |
分子式 | C20H24Cl2N2 |
分子量 | 363.32 |
溶解度 | DMSO: 250 mg/mL (688.10 mM) |
储存条件 | Store at -20℃ |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
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[1]. M22 (0.37-90 μM; 24 h) blocks neddylation pathway selectively and suppresses degradation of CRL substrates in A549 cells[1].M22 (0.1-100 μM; 48 h) inhibits A549 cell proliferation completely at 30 µM (GI50=5.5 µM, GI90=19.3 µM)[1].M22 (15-30 μM; 36 h) promotes apoptosis in A549 cell line[1]. Cell Viability Assay[1] Cell Line: A549 cells 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[1]. [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. |