1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. NEDD8-activating Enzyme

NEDD8-activating Enzyme

NEDD8-activating Enzyme (NAE) is an essential component of the NEDD8 conjugation pathway that controls the activity of the cullin-RING subtype of ubiquitin ligases, thereby regulating the turnover of a subset of proteins upstream of the proteasome. Substrates of cullin-RING ligases have important roles in cellular processes associated with cancer cell growth and survival pathways.

NEDD8 (neural precursor cell expressed developmentally downregulated protein 8) is the ubiquitin-like protein most homologous to ubiquitin. The covalent binding of NEDD8 to substrate proteins is called “neddylation”, and includes the following steps: mature NEDD8 is activated by NEDD8-activating enzyme E1 (NAE), transferred by NEDD8-conjugating enzyme E2, and conjugated to the substrate protein by a NEDD8-E3 ligase.

NAE is a critical regulator of the neddylation pathway. Inhibition of NAE can inhibit the activity of the cullin-RING ligases (CRLs) and result in accumulation of CRL substrate proteins.

NEDD8-activating Enzyme Related Products (7):

Cat. No. Product Name Effect Purity
  • HY-70062
    Pevonedistat Inhibitor 98.84%
    Pevonedistat (MLN4924) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC50 of 4.7 nM.
  • HY-10484
    Pevonedistat hydrochloride Inhibitor 98.75%
    Pevonedistat hydrochloride (MLN4924 hydrochloride) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor, with an IC50 of 4.7 nM.
  • HY-111505
    NAcM-OPT Inhibitor 98.60%
    NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction.
  • HY-128586
    TAS4464 Inhibitor
    TAS4464 is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM.
  • HY-101790A
    ZM223 hydrochloride Inhibitor 98.00%
    ZM223 hydrochloride is an orally active, potent non-covalent NEDD8 activating enzyme (NAE) inhibitor with excellent anticancer activity.
  • HY-128586A
    TAS4464 hydrochloride Inhibitor
    TAS4464 (hydrochloride) is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM.
  • HY-101790
    ZM223 Inhibitor
    ZM223 is a potent non-covalent NEDD8 activating enzyme (NAE) inhibitor, orally active.
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