NAE-IN-M22是一种有效，选择性和可逆的NEDD8活化酶(NAE)抑制剂，效力在微摩尔范围内。NAE-IN-M22抑制多种癌细胞生长并诱导A549细胞凋亡。NAE-IN-M22还可以在体内抑制肿瘤的生长。
货号:ajcx32130
CAS:864420-54-2
分子式:C20H24Cl2N2
分子量：363.32
溶解度:DMSO: 250 mg/mL (688.10 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.