NEDD8-activating enzyme (NAE) is upstream of the 20S proteasome in the ubiquitin/proteasome pathway and catalyzes the first step in the neddylation pathway. In order to control the activity of the cullin-RING subtype of ubiquitin ligases, which in turn controls the activity of a subset of proteins upstream of the proteasome, NAE is a crucial part of the NEDD8 conjugation pathway. Cullin-RING ligase substrates play significant roles in cellular processes connected to pathways for cancer cell growth and survival.
A crucial signaling molecule associated with cell homeostasis and functional maintenance is the ubiquitin-like protein NEDD8. Many human diseases, including cancer, involve dysregulation of this process. The sole activation enzyme of the neddylation pathway, NEDD8-activating enzyme E1 (NAE), has thus emerged as a promising anticancer target.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V113752 | NAE-IN-3 | 951950-33-7 | NAE-IN-3 (compound 1) is a highly potent and selective non-covalently competitive inhibitor of NEDD8 activator (NAE) (IC50 = 0.8 μM). |
|
V2786 | Pevonedistat (TAK924; MLN4924) | 905579-51-3 | Pevonedistat (previously known as MLN-4924; TAK-924) is a potent and selective small molecule inhibitor of Nedd8 (Neural precursor cell expressed, developmentally down-regulated 8) activating enzyme (NAE) with anticancer activity. |
|
V3202 | Pevonedistat HCl (MLN-4924; TAK-924) | 1160295-21-5 | Pevonedistat HCl (MLN4924; TAK924), the hydrochloride salt ofPevonedistat,is an inhibitor of Nedd8 (Neural precursor cell expressed, developmentally down-regulated 8) activating enzyme (NAE) with IC50 of 4 nM. |
|
V31900 | ZM223 | 2031177-48-5 | ZM223 is a potent, non-covalent NEDD8 activating enzyme (NAE) inhibitor (antagonist) with oral activity. |
|
V73273 | ZM223 hydrochloride | 2438679-27-5 | ZM223 HCl is a potent non-covalent NEDD8 activating enzyme (NAE) inhibitor (antagonist) with oral activity. |
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