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505477 NAE Inhibitor, MLN4924 - CAS 951950-33-7 - Calbiochem

NAE Inhibitor, MLN4924, CAS 951950-33-7, is an AMP mimetic that forms a NAE-catalyzed NEDD8 adduct, which acts as a tight-binding, ATP-competitive NAE inhibitor (IC50 = 4.7 nM).

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Synonymes: 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

Primary Target: NEDD8-Activating Enzyme
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505477
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CAS #Empirical Formula
951950-33-7C₂₁H₂₅N₅O₄S

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      Description
      OverviewA 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 = 4.7 nM), 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 = 90 nM in HCT-116 cultures in 24 h), resulting in cullin-RING ligases substrates elevation. Shown to inhibit the growth of various cancer cells both in cultures (IC50 from 50 nM to 1.03 µM) in vitro and in murine xenograft models (30 to 60 mg/kg via s.c.) in vivo via apoptosis induction.
      Catalogue Number505477
      Brand Family Calbiochem®
      SynonymsNEDD8-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
      References
      ReferencesMilhollen, M.A., et al. 2010. Blood 116, 1515.
      Brownell, J.E., et al. 2010. Mol. Cell 37, 102.
      Soucy, T.A., et al. 2009. Nature 458, 73.
      Product Information
      CAS number951950-33-7
      FormLight beige solid
      Hill FormulaC₂₁H₂₅N₅O₄S
      Chemical formulaC₂₁H₂₅N₅O₄S
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationNAE Inhibitor, MLN4924, CAS 951950-33-7, is an AMP mimetic that forms a NAE-catalyzed NEDD8 adduct, which acts as a tight-binding, ATP-competitive NAE inhibitor (IC50 = 4.7 nM).
      Biological Information
      Primary TargetNEDD8-Activating Enzyme
      Primary Target IC<sub>50</sub>4.7 nM)
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      5054770001 04055977243857

      Documentation

      NAE Inhibitor, MLN4924 - CAS 951950-33-7 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Milhollen, M.A., et al. 2010. Blood 116, 1515.
      Brownell, J.E., et al. 2010. Mol. Cell 37, 102.
      Soucy, T.A., et al. 2009. Nature 458, 73.
      Fiche technique

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision11-October-2013 JSW
      SynonymsNEDD8-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
      DescriptionA 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 = 4.7 nM), exhibiting much reduced or little potency against Ub-activating enzyme UAE/UBA1, Ub-like modifier activating enzyme UBA6/UBE1L2, SUMO activating enzyme SAE, Ub-like modifier activating enzyme ATG7 (IC50 = 1.5, 1.8, 8.2, and >10 µM, respectively), adenosine receptors A1/A2A/A2B/A3, or a panel of 12 cellular kinases (IC50 >10 µM). Selectively reduces cellular Ubc12-NEDD8, but not Ubc9-SUMO or Ubc10-Ub, thioester formation (ICmax = 90 nM in HCT-116 cultures in 24 h), resulting in build-up of CRLs (cullin-RING ligases) substrates CDT1, NFE2L2/NRF2, and p27, without affecting overall cellular protein turnover. Shown to inhibit the growth of cancers of various origins both in cultures (IC50 from 50 nM to 1.03 µM) in vitro and in murine xenograft models (30 to 60 mg/kg; q.d. or b.i.d via s.c.) in vivo via apoptosis induction.
      FormLight beige solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number951950-33-7
      Chemical formulaC₂₁H₂₅N₅O₄S
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
      Toxicity Standard Handling
      ReferencesMilhollen, M.A., et al. 2010. Blood 116, 1515.
      Brownell, J.E., et al. 2010. Mol. Cell 37, 102.
      Soucy, T.A., et al. 2009. Nature 458, 73.