Table 1.
Inhibitors of SUMO activating and conjugating enzymes. List of the small molecules, which inhibit SUMO conjugation. The IC50 are those obtained with purified recombinant enzymes or on cell lines. Only the molecules that were either validated on cells in vitro or in vivo in mouse models are indicated. Only one is being used in humans (TAK-981).
| Inhibitor Name | Structure | IC50 (µM) | Target | Use | Reference |
|---|---|---|---|---|---|
| Gingkolic acid |
|
3 | SAE1/SAE2 | In vitro | [72,110] |
| Anacardic acid |
|
2.2 | SAE1/SAE2 |
In vitro
In vivo |
|
| Kerriamycin B |
|
11.70 | SAE1/SAE2 | In vitro | [111] |
| Spectomycin B1 |
|
4.4 | UBC9 | In vitro | [112] |
| 2D08 |
|
6 | UBC9 |
In vitro
In vivo |
[78,113] |
| Davidiin |
|
0.150 | SAE1/SAE2 | In vitro | [114] |
| Tannic acid |
|
12.80 | SAE1/SAE2 | In vitro | [115] |
| ML-792 |
|
0.003 | SAE1/SAE2 | In vitro | [104] |
| COH000 |
|
0.200 | SAE1/SAE2 |
In vitro
In vivo |
[105,106] |
| TAK-981 | NA | NA | SAE1/SAE2 |
In vitro
In vivo |
ClinicalTrials.gov Identifier: NCT03648372) |