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Table 2 Summary of inhibitors targeting UBE2M and DCN1

From: Targeting neddylation E2s: a novel therapeutic strategy in cancer

Compound IC50 (TR-FRET) Effect Cell line Clinical trial
DI-404 [125] N/A Inhibits the neddylation of cullin3 Lung cancer cells N/A
DI-591 [124] N/A Inhibits the neddylation of cullin3 and increases the expression of NRF2 Liver cells N/A
NAcM-HIT [129] 8 μM Disturbs the interaction between UBE2M and DCN1 Lung cancer cells N/A
NAcM-OPT [130] 80 nM Inhibits the neddylation of cullin3 and cullin1 Liver cells N/A
NAcM-COV [131] < 40 nM Reduces the steady-state levels of neddylated cullin1 and cullin3 Liver cells N/A
DC-2 [132] 15 nM Decreases the neddylation of cullin3 Lung cancer cells N/A
    Esophageal cancer cells  
    Liver cancer cells  
    Breast cancer cells  
    Prostatic cancer cells  
Compound 27 [133] 0.2 μM Disturbs the neddylation of cullin1 and cullin3 Lung cancer cells N/A
WS-383 [134] 11 nM Inhibits the neddylation of cullin1 and cullin3 Gastric cancer cells N/A
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