NAcM-OPT

Description

NAcM-OPT (2089293-61-6) is a potent and selective NEDD8 ligation inhibitor, IC50=80 nM (in vitro).1? It inhibits the N-terminal acetyl-dependent interaction between the E2 conjugating enzyme UBE2M/UBC12 and DCN1, a subunit of a multiprotein E3 ligase for the ubiquitin-like protein NEDD8, an interaction which is essential for assembly of the multiprotein ligation complex.2 NAcM-OPT inhibits NEDD8 ligation in vitro and in cells (IC50=10 μM) and suppresses anchorage-independent growth of HCC95 cells and is highly selective with respect to other N-terminal acetyl protein binding sites.1

The Uses of NAcM-OPT

NAcM-OPT inhibits N-Acetyl-mediated interaction between BE2M (E2 conjugating enzyme) and DCN1 (a component of E3 ligase complex). Also has inhibitory action on DCN2 and NEDD8 ubiquitin-like protein. Reduces anchorage-independent growth in DCN1-amplified cell line.

Definition

ChEBI: 1-Benzyl-1-(1-butyl-4-piperidinyl)-3-(3,4-dichlorophenyl)urea is a member of ureas.

References

1) Scott et al. (2017), Blocking an N-terminal acetylation-dependent protein interaction inhibits an E3 ligase; Nat. Chem. Biol., 13 850 2) Scott et al. (2011), N-terminal acetylation acts as an avidity enhancer within an interconnected multiprotein complex; Science, 334 674