dcn1-ubc12 interaction

WS-383 is a selective, potent and reversible DCN1-UBC12 interaction inhibitor(IC50 of 11 nM).

DI-591 is a potent, high-affinity, cell-penetrant inhibitor of the DCN1‑UBC12 interaction. It binds to DCN1 and DCN2 with Ki values of 12 nM and 10.4 nM, respectively, while showing little to no binding to DCN3, DCN4, and DCN5. DI-591 selectively inhibits neddylation of cullin 3 without significant or only weak effects on other cullin family members.

WS-383 free base is a selective and reversible DCN1-UBC12 interaction inhibitor with an IC50 of 11 nM.

DI-1548 is a potent, selective, irreversible covalent inhibitor of DCN1 (IC50 = 4.6 nM). It efficiently and selectively inhibits the neddylation of Cullin 3 at nanomolar concentrations without significantly affecting the neddylation of other Cullin proteins, such as Cullin 1, 2, 4A, 4B, and 5, and exhibits no cytotoxicity. The covalent bond formation between DI-1548 and DCN1 disrupts the DCN1-UBC12 interaction, leading to the disassembly of the neddylation complex and the subsequent inactivation of CRL3. This process results in the accumulation of NRF2 and the upregulation of its target genes, providing hepatoprotective effects in mouse models. DI-1548 is applicable in studies related to liver injury.

DI-404 is a high-Affinity Peptidomimetic the DCN1-UBC12 Protein-Protein Interaction inhibitor (Kd= 6.9 nM). DI-404 effectively and selectively inhibits the neddylation of cullin 3 over other cullin members.

NAcM-OPT HCL is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor that targets N-Acetyl-UBE2M (E2 conjugating enzyme, UBC12) interaction with DCN1 with IC50 of 79 nM.