NEDD8-activating Enzyme

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.

Targets for NEDD8-activating Enzyme

Products for NEDD8-activating Enzyme

Cat.No. Nombre del producto Información
GC15086 MLN4924

Pevonedistat
MLN4924 es un potente y selectivo inhibidor de pequeñas moléculas de la enzima activadora de NEDD8 (NAE) (IC₅₀ = 4 nM), y es selectivo en comparación con las enzimas estrechamente relacionadas UAE, SAE, UBA6 y ATG7 (IC₅₀ = 1,5, 8,2, 1,8 y >10 µM, respectivamente).
GC12175 MLN4924 HCl salt A selective inhibitor of NEDD8-activating enzyme
GC64989 NAcM-OPT NAcM-OPT es un inhibidor de cullin neddylation 1 (DCN1) biodisponible por vÍa oral, que inhibe de forma potente la interacciÓn DCN1-UBE2M.
GC37742 TAS4464
TAS4464 es un inhibidor altamente potente y selectivo de la enzima activadora de NEDD8 (NAE), con un IC50 de 0,955 nM.
GC37743 TAS4464 hydrochloride TAS4464 (clorhidrato) es un inhibidor muy potente y selectivo de la enzima activadora de NEDD8 (NAE), con una IC50 de 0,955 nM.
GC38156 ZM223 hydrochloride El clorhidrato de ZM223 es un potente inhibidor de la enzima activadora de NEDD8 (NAE) no covalente activo por vÍa oral con excelente actividad anticancerÍgena.