| 产品详情 |
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| Product Name | MLN4924 |
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| Description | Purity >98%. 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 by NEDD8-activating enzyme (NAE), which has become a novel target in cancer therapeutic research. MLN4924 is an analog of adenosine 5'-monophosphate that selectively inhibits NAE (IC50 = 4.7 nM). At much higher concentrations, MLN4924 inhibits the related enzymes ubiquitin-activating enzyme (UAE) and SUMO-activating enzyme (SAE) with IC50 values of 1.5 and 8.2 µM, respectively. At 0.3 µM, MLN4924 has been shown to disrupt CRL-mediated protein turnover leading to apoptosis in HCT116 cells by deregulating S-phase DNA synthesis. In vivo, 30-60 mg/kg MLN4924 dose-dependently suppresses the growth of human tumor xenografts in mice. |
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| Size | n/a |
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| Concentration | n/a |
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| Applications | n/a |
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| Other Names | sulfamic acid, [(1S,2S,4R)-4-[4-[[(1S)-2,3-dihydro-1H-inden-1-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-2-hydroxycyclopentyl]methyl ester, Pevonedistat |
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| Gene, Accession, CAS # | CAS: 905579-51-3 |
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| Catalog # | LS-H8772 |
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| Order / More Info | MLN4924 from LIFESPAN BIOSCIENCES INC. |
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| Product Specific References | n/a |
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