dcn1-ubc12

DCN1-UBC12-IN-1 is a potent and specific DCN1-UBC12 inhibitor with an IC50 value of 2.86 nM and anti-cardiac fibrogenic activity.

DCN1-UBC12-IN-2 is a potent and specific DCN1-UBC12 inhibitor with an IC50 value of 9.55 nM, targeting DCN1-UBC12 interactions and inhibiting Ang II-induced activation of cardiac fibroblasts.

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

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

Yucasin is a highly potent inhibitor of auxin (IAA) biosynthesis that blocks the tryptophan-dependent pathway by specifically inhibiting the activity of YUCCA (YUC) flavin-containing monooxygenases. It serves as a valuable tool for investigating the regulatory mechanisms of auxin in plant growth, development, and stress responses.

WS-384 is an orally active dual inhibitor of LSD1 and DCN1-UBC12 protein-protein interactions, with IC50 values of 338.79 nM and 14.81 nM, respectively. It exhibits anticancer properties, causing cell cycle arrest, DNA damage, and inducing apoptosis (apoptosis). WS-384 can be applied in research on non-small cell lung cancer (NSCLC).

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.