NEDD8 inhibitor M22

Research use only, not for human use.

NEDD8 inhibitor M22 is a novel, potent, selective reversible NEDD8 activating enzyme (NAE) inhibitor.

NEDD8 inhibitor M22 is a novel, potent, selective reversible NEDD8 activating enzyme (NAE) inhibitor; inhibit A549 cell proliferation completely at 30 uM (GI50=5.5 uM and GI90=19.3 uM); produces tumor inhibition in AGS xenografts in nude mice and low acute toxicity in zebrafish model; exhibts different binding mode compared with MLN4924.

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. Cell Viability Assay Cell Line:A549 cells Concentration:0.37, 1.11, 3.33, 10, 30, 90 μM Incubation Time:24 hours Result:Inhibited formations of Uba3-NEDD8 and Ubc12-NEDD8.Resulted in a corresponding decrease in the abundance of Cullins-NEDD8.

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.

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Proteasome/Ubiquitin

E1

E1

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864420-54-2

363.326

C20H24Cl2N2

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (688.10 mM)

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1-benzyl-N-(2,4-dichlorophenethyl)piperidin-4-amine

(-20℃)

With Ice Pack

≥ 2 years