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

509704
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₀H₂₁Cl₂NO₆ 1319207-44-7

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      5.09704.0001
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          Glass bottle 10 mg
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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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Huang, H., et al. 2013. Nat. Chem. Biol. 10, 156.
          Ceccarelli, D.F., et al. 2011. Cell 145, 1075.
          Data Sheet

          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 -20°C
          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.
          Toxicity Standard Handling
          ReferencesHuang, H., et al. 2013. Nat. Chem. Biol. 10, 156.
          Ceccarelli, D.F., et al. 2011. Cell 145, 1075.