Targeting neddylation E2s: a novel therapeutic strategy in cancer

Table 2 Summary of inhibitors targeting UBE2M and DCN1

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