EC Number   |
Inhibitors |
Structure |
|---|
   2.3.2.23 | 5-chloro-1,3-benzoxazole-2-thiol |
- |
   |
| 2.3.2.23 | 5-[(piperidin-1-yl)methyl]pyrazolo[1,5-a]pyrimidin-7(4H)-one |
- |
|
| 2.3.2.23 | 6-chloro-1,3-benzoxazole-2-thiol |
- |
|
| 2.3.2.23 | 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide |
i.e. EM02, almost complete inhibition of FANCD2 ubiquination |
|
| 2.3.2.23 | CC0651 |
a small-molecule inhibitor that selectively inhibits Ube2R1, the specialized E2 for SCF E3 ligases, which builds K48-linked polyUb chains on its targets for proteasomal degradation. In a co-crystal structure of Ube2R1, Ub, and CC0651, the inhibitor is sandwiched between the E2 and Ub |
|
| 2.3.2.23 | CC0651 |
- |
|
| 2.3.2.23 | ethyl 3-(2,2'-dihydroxy[1,1'-biphenyl]-4-yl)propanoate |
- |
|
| 2.3.2.23 | eupalinolide B |
Kd value 0.00925 mM. UBE2D3 is modified by EB in residue Cys85, the presence of eupalinolide B enhances the thermal stabilization of UBE2D3. Eupanolide B effectively inhibits the activity of UBE2D3 and prevents the degradation of IkappaBalpha and the activation of NF-kappaB |
|
| 2.3.2.23 | more |
allosteric inhibition of the SUMO E2 enzyme Ubc9. Identification of two distinct small molecule fragments that bind to Ubc9 at a site distal from its catalytic cysteine. These fragments and related compounds inhibit SUMO conjugation to the enzyme with IC50 values of 1.9-5.8 mM. Mechanistic and biophysical analyses, coupled with molecular dynamics simulations, point toward ligand-induced rigidification of Ubc9 as a mechanism of inhibition, overview |
|
| 2.3.2.23 | more |
backside binding by accessory elements of the RING E3 Rad18 inhibits the intrinsic chain-forming activity of Ube2B; enzyme UBE2E1 performs autoubiquitylation, ubiquitylation results in inhibition of E2 activity; the backside-binding element of the E3 AO7 decreases the processivity of chain building by the E2 Ube2D2 |
|
