NAcM-OPT, NEDD8 ligation inhibitor (TBI1636)

Description

Product Details

Formal Name: 1-Benzyl-1-(1-butylpiperidin-4-yl)-3-(3,4-dichlorophenyl)urea

Molecular Formula: C₂₃H₂₉Cl₂N₃O

Formula Weight: 434.40

CAS Number: 2089293-61-6

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 30 mg/ml) or in Ethanol (up to 20 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

NEDD8 ligation inhibitor

Functions

A potent and selective NEDD8 ligation inhibitor, IC50=80 nM (in vitro). 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. 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.

Application Procedures

First dissolved in DMSO (up to 30 mg/ml) or in Ethanol (up to 20 mg/ml), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.