| 产品详情 |
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| Product Name | NAE Inhibitor, MLN4924 |
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| Description | Purity ~98% (HPLC). A cell-permeable AMP mimetic that targets the NEDD8-activating E1 enzyme NAE nucleotide-binding site and undergoes a NAE-catalyzed covalent NEDD8 adduct formation, the adduct in turn acts as a tight-binding, ATP-competitive NAE inhibitor (IC50 = 4.7nM), exhibiting much reduced or little potency against UAE/UBA1, UBA6/UBE1L2, SAE, ATG7, adenosine receptors A1/A2A/A2B/A3, or a panel of 12 cellular kinases. Selectively reduces cellular Ubc12-NEDD8, but not Ubc9-SUMO or Ubc10-Ub, thioester formation (ICmax = 90nM in HCT-116 cultures in 24h), resulting in cullin-RING ligases substrates elevation. Shown to inhibit the growth of various cancer cells both in cultures (IC50 from 50nM to 1.03uM) in vitro and in murine xenograft models (30 to 60mg/kg via s.c.) in vivo via apoptosis induction. Solubility: DMSO (100mg/ml). Use only fresh DMSO for reconstitution. Water by CHN (mol): ≥0.0mol Elemental Analysis: Calculated: %C: 54.00-57.00 %H: 5.50-7.50 %N: 13.50-16.50 |
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| Size | 5mg |
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| Concentration | n/a |
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| Applications | n/a |
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| Other Names | NAE Inhibitor, MLN4924 (NEDD8-Activating Enzyme Inhibitor, ((1S,2S,4R)-4-(4-((1S)-2,3-Dihydro-1H-inden-1-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl}-2-hydroxycyclopentyl)methyl Sulphamate) |
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| Gene, Accession, CAS # | n/a |
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| Catalog # | 217578 |
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| Order / More Info | NAE Inhibitor, MLN4924 from UNITED STATES BIOLOGICAL |
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| Product Specific References | n/a |
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