产品
编 号:F486183
分子式:C20H24Cl2N2
分子量:363.32
产品类型
结构图
CAS No: 864420-54-2
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产品详情
生物活性:
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.
体内研究:
M22 (60 mg/kg; i.p. once daily for 14 d) inhibits tumor growth in nude mice bearing AGS xenografts.M22 (0.36-90 μM) has low acute toxicity in zebrafish model.
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.