GlpBio

NEDD8-activating Enzyme

NEDD8-activating Enzyme(NEDD8活化酶)

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 相关产品(6)

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

    A selective inhibitor of NEDD8-activating enzyme

  • GC15086 structure
    GC15086MLN4924
    CAS: 905579-51-3
    纯度: >99.50% / >98.00%

    MLN4924 是一种有效的选择性 NEDD8 激活酶 (NAE) 小分子抑制剂 (IC50 = 4 nM) ，并且相对于密切相关的酶 UAE、SAE、UBA6 和 ATG7 具有选择性（ IC50 = 1.5、8.2、1.8 和 >；分别为 10 μM）。

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

    TAS4464是一种高效且选择性的NEDD8激活酶（NAE）抑制剂，IC 50 为0.955nM。

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

    TAS4464 (hydrochloride) 是一种高效选择性的 NEDD8 活化酶 (NAE) 抑制剂，IC50 值为 0.955 nM。

  • GC38156 structure
    GC38156ZM223 hydrochloride
    纯度: >98.50%

    ZM223 hydrochloride 是一种有效的非共价 NEDD8 活化酶 (NAE) 抑制剂，具有口服活性。

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

    NAcM-OPT is a specific, reversible and orally bioavailable inhibitor of cullin neddylation 1 (DCN1) that targets N-Acetyl-UBE2M (E2 conjugating enzyme, UBC12) interaction with DCN1 with IC50 of 79 nM.