Oncogenesis

Table 2 Inhibitors against E2-E1 or E2-E3 interactions.

From: Discovery of neddylation E2s inhibitors with therapeutic activity

Si No	Name & type	Potency	Target protein	Cellular Activity	References
1	HA-1141	IC₅₀ < 10 µM^a	UBA3	Inhibit CULLIN 1–5 neddylation and induce ER stress-dependent autophagy in H358 cells.	[38]
2	HA-9104	IC₅₀ = 49 µM^a	UBE2F	Inhibit CULLIN5 neddylation and accumulate CRL5 substrate NOXA	[77]
3	Arctigenin	IC₅₀ < 2.5 µM	UBE2M	Inhibit CULLIN 1-4 neddylation and accumulate tumor suppressor PDCD4 protein.	[78]
4	NAcM-OPT	IC₅₀ = 80 nM	DCN1	Inhibit CULLIN1 and CULLIN3 neddylation in 10 µM in HCC95 cells.	[79]
5	NAcM-COV	IC₅₀ ≤ 40 nM	DCN1	Inhibit CULLIN1 and cullin3 neddylation at 10 µM in HCC95 cells.	[79]
6	Compound 27	IC₅₀ = 0.2 µM	DCN1	Inhibit CULLIN1 and CULLIN3 neddylation at 10 µM in HCC95 cells	[80]
7	Compound 40	IC₅₀ = 0.1 µM	DCN1	Thermally stabilizes DCN1, and inhibits anchorage-independent growth in a DCN1 amplified squamous cell carcinoma cell line	[81]
8	DI-591	K_i = 12 nM	DCN1	Inhibit CULLIN3 neddylation in 0.3 µM concentration in THLE2 cells.	[39]
9	DI-404	K_d = 6.7 nM	DCN1	Converts CULLIN3 into a predominantly unneddylated form at 1 μM in H2170 cells.	[82]
10	DI-1548	K_i < 1 nM	DCN1	Selectively inhibit CULLIN3 neddylation and accumulate NRF2 levels in U2OS cells.	[83]
11	DI-1859	K_i < 1 nM	DCN1	Selectively inhibit CULLIN3 neddylation and accumulate NRF2 levels in U2OS cells.	[83]
12	WS-383	IC₅₀ = 11 nM	DCN1	Inhibit CULLIN1 and CULLIN3 neddylation in <3 µM in MGC-803 cells.	[84]
13	DC-2	IC₅₀ = 15 nM	DCN1	Inhibit CULLIN1 and CULLIN3 neddylation at 10 µM in PC9 and H1975 cells.	[85]
14	DN-2	IC₅₀ = 9.6 nM	DCN1	Inhibit CULLIN3 neddylation and reversed Ang-II induced cardiac fibroblast activation.	[86]
15	SK-464	IC₅₀ = 26 nM	DCN1	Inhibit migration and invasion of cancer cells and CULLIN3 neddylation.	[87]

^aActivity is reported based on the visual band of inhibition of CULLIN neddylation

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