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Home >> Signaling Pathways >> Proteases >> 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.

Products for  NEDD8-activating Enzyme

  1. Cat.No. 产品名称 Information
  2. GC64989 NAcM-OPT 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.
  3. GC38156 ZM223 hydrochloride 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。
  4. GC37743 TAS4464 hydrochloride 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。
  5. GC37742 TAS4464 TAS4464 is a potent and highly selective NEDD8 activating enzyme (NAE) inhibitor with IC50 of 0.955 nM. TAS4464 exhibits superior antitumor activity with prolonged target inhibition.
  6. GC15086 MLN4924

    氨基磺酸[(1S,2S,4R)-4-[4-[[(1S)-2,3-二氢-1H-茚-1-基]氨基]-7H-吡咯并[2,3-D]嘧啶-7-基]-2-羟基环戊基]甲基酯,MLN4924

     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）。
  7. GC12175 MLN4924 HCl salt

    氨基磺酸[(1S,2S,4R)-4-[4-[[(1S)-2,3-二氢-1H-茚-1-基]氨基]-7H-吡咯并[2,3-D]嘧啶-7-基]-2-羟基环戊基]甲基酯盐酸盐,MLN 4924 (HCl salt)

     A selective inhibitor of NEDD8-activating enzyme

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