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.


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ZM223

ZM223 is a novel non-sulfamide NEDD8 activating enzyme inhibitor that inhibits HCT116 colon cancer cells with an IC50 value of 100 nM.

  • CAS Number: 2031177-48-5
  • MF: C23H17F3N4O2S2
  • MW: 502.53
  • Catalog: NEDD8-activating Enzyme
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MLN4924

MLN4924 is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC50 of 4.7 nM.

  • CAS Number: 905579-51-3
  • MF: C21H25N5O4S
  • MW: 443.519
  • Catalog: NEDD8-activating Enzyme
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 721.0±70.0 °C at 760 mmHg
  • Melting Point: 161-163°C
  • Flash Point: 389.9±35.7 °C

TAS4464

TAS4464 is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM[1].

  • CAS Number: 1848959-10-3
  • MF: C21H23FN6O6S
  • MW: 506.51
  • Catalog: NEDD8-activating Enzyme
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TAS4464 hydrochloride

TAS4464 (hydrochloride) is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM[1].

  • CAS Number: 1848959-11-4
  • MF: C21H24ClFN6O6S
  • MW: 542.97
  • Catalog: NEDD8-activating Enzyme
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MLN4924 (hydrochloride)

Pevonedistat hydrochloride (MLN4924 hydrochloride) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor, with an IC50 of 4.7 nM.

  • CAS Number: 1160295-21-5
  • MF: C21H26ClN5O4S
  • MW: 479.98000
  • Catalog: NEDD8-activating Enzyme
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NAcM-OPT

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

  • CAS Number: 2089293-61-6
  • MF: C23H29Cl2N3O
  • MW: 434.40
  • Catalog: NEDD8-activating Enzyme
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A