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编 号:F486183
分子式:C20H24Cl2N2
分子量:363.32
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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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.
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