NAE-IN-M22 |
| Catalog No.GC61623 |
NAE-IN-M22 est un inhibiteur puissant, sélectif et réversible de l'enzyme activatrice NEDD8 (NAE), avec une puissance dans la gamme micromolaire. NAE-IN-M22 inhibe plusieurs lignées cellulaires cancéreuses et induit l'apoptose dans les cellules A549. NAE-IN-M22 peut également inhiber la croissance tumorale in vivo.
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Cas No.: 864420-54-2
Sample solution is provided at 25 µL, 10mM.
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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.
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