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NEDD8-activating Enzyme

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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.

Products Related to NEDD8-activating Enzyme(7)

  • GC12175 structure
    GC12175MLN4924 HCl salt
    CAS: 1160295-21-5
    Purity: >98.00%

    A selective inhibitor of NEDD8-activating enzyme

  • GC15086 structure
    GC15086MLN4924
    CAS: 905579-51-3
    Purity: >98.00%

    MLN4924 is a potent and selective small-molecule inhibitor of NEDD8-activating enzyme (NAE) (IC50 = 4 nM), and is selective relative to the closely related enzymes UAE, SAE, UBA6 and ATG7 (IC50 = 1.5, 8.2, 1.8 and >10 µM, respectively).

  • GC37742 structure
    GC37742TAS4464
    CAS: 1848959-10-3
    Purity: >98.00%

    TAS4464 is a highly potent and selective inhibitor of NEDD8-activating enzyme (NAE), with an IC 50 of 0.955nM.

  • GC37743 structure
    GC37743TAS4464 hydrochloride
    CAS: 1848959-11-4
    Purity: >98.50%

    TAS4464 (hydrochloride) is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM.

  • GC38156 structure
    GC38156ZM223 hydrochloride
    Purity: >98.50%

    ZM223 hydrochloride is an orally active, potent non-covalent NEDD8 activating enzyme (NAE) inhibitor with excellent anticancer activity.

  • GC64989 structure
    GC64989NAcM-OPT
    CAS: 2089293-61-6
    Purity: >99.00%

    NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction.

  • GC81683 structure
    GC81683AM9053
    CAS: 157469-21-1
    Purity: >98.00%

    AM9053 is a selective, effective and slowly reversible inhibitor of N-acyl ethanolamine acid amidease ( NAAA ) ( IC 50 = 30 nM).