NAcM-OPT
NEDD8 ligation inhibitor / 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
Biochemicals & reagents
2089293-61-6
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
-20°C
TARGET: Neddylation -- PATHWAY: Degradation -- RESEARCH AREA: Ubiquitin/Proteasome -- DISEASE AREA: Cancer