NEDD8 is an ubiquitin-like protein whose activity is required to activate cullin-RING ubiquitin E3 ligases (CRLs) responsible for the ubiquitination and proteasome-dependent turnover of certain substrates with roles relevant to cellular processes important for cancer cell survival. Neddylation of CRLs is initiated...

Description: Pevonedistat (MLN4924) is a potent and selective NEDD8 activating enzyme (NAE) inhibitor (IC50=4.7 nM) with therapeutic potential for myelodysplastic syndromes (MDS) and antitumor activity. Target: NEDD8, E1/E2/E3 Enzyme. Smiles: NS(=O)(=O)OC[C@@H]1CC(C[C@@H]1O)n1ccc2c(NC3CCc4ccccc34)ncnc12....

MLN4924 acts as a Nedd8-activating enzyme inhibitor, blocking proteasomal cullin protein neddylation by Cullin-RING E3 ubiquitin ligases. As a result, these proteins accumulate, inducing cell cycle arrest, senescence, autophagy, and/or apoptosis in cellular and animal models. This compound's inhibition of...

White solid. Soluble in DMSO (30mg/ml), ethanol (10mg/ml) or DMF (20mg/ml). Insoluble in water. Chemical. CAS: 905579-51-3. Formula: C21H25N5O4S . H2O. MW: 443.5 . 18.0. Adenosine 5'-monophosphate (AMP) analog. Potent, selective and cell permeable inhibitor of Nedd8 E1 Activating Enzyme (NAE) (IC50=4.7nM). NEDD8 is...

Liquid. Potent, selective and cell-permeable inhibitor of Nedd8 E1 Activating Enzyme (NAE), By inhibiting the Neddylation pathway this molecule disrupts cullin-RING ligase activity, leading to inhibition of proliferation or apoptotic death of various human tumor cells through the deregulation of S-phase DNA synthesis.