| Identification | Back Directory | [Name]
NAcM-OPT | [CAS]
2089293-61-6 | [Synonyms]
NAcM-OPT
NAcM-OPT NEW
Urea, N-(1-butyl-4-piperidinyl)-N'-(3,4-dichlorophenyl)-N-(phenylmethyl)- | [Molecular Formula]
C23H29Cl2N3O | [MDL Number]
MFCD31693837 | [MOL File]
2089293-61-6.mol | [Molecular Weight]
434.4 |
| Chemical Properties | Back Directory | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (up to 30 mg/ml) or in Ethanol (up to 20 mg/ml) | [form ]
solid | [color ]
White | [Stability:]
Stable for 1 year as from date of purchase supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| Hazard Information | Back Directory | [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 | [Uses]
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 |
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