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509704 Cdc34 Inhibitor, CC0651 - CAS 1319207-44-7 - Calbiochem

A cell-permeable, selective allosteric inhibitor of E2 ubiquitin-conjugating enzyme Cdc34 (IC₅₀ = 2.5 µM in a Sic1-SCFCdc4 assay).

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Synonymes: 4,5-Dideoxy-5-(3ʹ,5ʹ-dichloro-4-biphenylyl)-4-((methoxyacetyl)amino)-L-arabinonic acid, (2R,3S,4S)-5-(3ʹ,5ʹ-Dichloro-(1,1ʹ-biphenyl)-4-yl)-2,3-dihydroxy-4-(2 methoxyacetamido)pentanoic acid, Cdc34A Inhibitor, Ube2R1 Inhibitor, Ubc3 Inhibitor, E2R1 Inhibitor, UbcH3 Inhibitor

Primary Target: E2 ubiquitin-conjugating enzyme Cdc34
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509704
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CAS #Empirical Formula
1319207-44-7C₂₀H₂₁Cl₂NO₆

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      Description
      OverviewA cell-permeable biphenylylpentanoic acid compound that acts as a selective allosteric inhibitor of E2 ubiquitin-conjugating enzyme Cdc34 (IC50 = 2.5 µM in a Sic1-SCFCdc4 assay) without affecting the activities of E1 or E3 ligases. Reported to act by trapping a weak interaction between ubiquitin and the E2 donor ubiquitin-binding site and may serve as a molecular bridge between Cdc34A and ubiquitin. Binds to Cdc34ACAT alone with an EC50 value of 267 µM, but in the presence of ubiquitin, this affinity is significantly increased (EC50 = 19 µM). Does not disrupt the interaction of Cdc34A with the RING domain of Rbx1 and is suggested to even moderately stabilize this interaction. Shown to inhibit p27Kip1 ubiquitination (IC50 = 1.72 µM) and reduce PC-3 cancer cells proliferation (~30 µM).

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number509704
      Brand Family Calbiochem®
      Synonyms4,5-Dideoxy-5-(3ʹ,5ʹ-dichloro-4-biphenylyl)-4-((methoxyacetyl)amino)-L-arabinonic acid, (2R,3S,4S)-5-(3ʹ,5ʹ-Dichloro-(1,1ʹ-biphenyl)-4-yl)-2,3-dihydroxy-4-(2 methoxyacetamido)pentanoic acid, Cdc34A Inhibitor, Ube2R1 Inhibitor, Ubc3 Inhibitor, E2R1 Inhibitor, UbcH3 Inhibitor
      References
      ReferencesHuang, H., et al. 2013. Nat. Chem. Biol. 10, 156.
      Ceccarelli, D.F., et al. 2011. Cell 145, 1075.
      Product Information
      CAS number1319207-44-7
      FormOff-white powder
      Hill FormulaC₂₀H₂₁Cl₂NO₆
      Chemical formulaC₂₀H₂₁Cl₂NO₆
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetE2 ubiquitin-conjugating enzyme Cdc34
      Purity≥98% by HPLC; ≥98% ee
      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 -20°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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      5097040001 04055977241044

      Documentation

      Cdc34 Inhibitor, CC0651 - CAS 1319207-44-7 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Huang, H., et al. 2013. Nat. Chem. Biol. 10, 156.
      Ceccarelli, D.F., et al. 2011. Cell 145, 1075.
      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.

      Revision18-July-2014 JSW
      Synonyms4,5-Dideoxy-5-(3ʹ,5ʹ-dichloro-4-biphenylyl)-4-((methoxyacetyl)amino)-L-arabinonic acid, (2R,3S,4S)-5-(3ʹ,5ʹ-Dichloro-(1,1ʹ-biphenyl)-4-yl)-2,3-dihydroxy-4-(2 methoxyacetamido)pentanoic acid, Cdc34A Inhibitor, Ube2R1 Inhibitor, Ubc3 Inhibitor, E2R1 Inhibitor, UbcH3 Inhibitor
      DescriptionA cell-permeable and aqueous soluble (~ 1 mg/mL or 2.26 mM at pH 7.4) biphenylylpentanoic acid that selectively inhibits human, but not yeast, E2 Ub-conjugating enzyme Cdc34- dependent substrates ubiquitinations in p27kip1-SCFSkp2, Sic1-SCFCdc4 (IC50 = 1.72 & 2.5 µM, respectively), Cyclin E-SCFFbw7, IκBα-SCFβTrCP ubiquitination assays and induces cellular p27kip1 and cyclin E accumulation (30 µM for 16 h in PC-3 cultures), displaying no affinity or inhibitory activity against other E1 (Uba1), E2 (Cdc34B/Ube2R2,Ube2G1, UbeU1), HECT E3 (SMURF 2, UbcH7), or RING E3 (Rnf168) tested. CC0651 is shown to target Ub-bound Cdc34 with a 14-fold higher affinity than the non-Ub-bound Cdc34 via an allosteric binding pocket at the periphery of the Cdc34-Ub interface. In addition to inhibit the reactivity of the Cdc34-Ub complex via direct binding, the CC0651-bound Cdc34-Ub complex itself is reported to exhibit higher affinity toward SCF E3 complex and thereby exhibit a dominant negative effect by effectively competing against functional Cdc34-Ub complex for SCF binding.
      FormOff-white powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1319207-44-7
      Chemical formulaC₂₀H₂₁Cl₂NO₆
      Purity≥98% by HPLC; ≥98% ee
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      -20°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesHuang, H., et al. 2013. Nat. Chem. Biol. 10, 156.
      Ceccarelli, D.F., et al. 2011. Cell 145, 1075.