533572 HECT Ligase Inhibitor, Heclin - Calbiochem

533572
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₇H₁₇NO₃

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      Description
      OverviewA cell-permeable acrylamide compound that acts as a rapid, reversible, and broadly specific inhibitor of HECT ligases (IC50 = 6.8, 6.3, 6.9 µM for Smurf2, Nedd4, and WWP1, respectively). Does not affect the activity of RING domain ligases, hence allows clear distinction between RING and HECT-mediated ubiquitination. Binds to the HECT domain and disturbs the orientation of the C lobe, which allows reversible oxidation of the active site cysteine to the highly reactive sulfenic acid form. Does not inhibit other cysteine-containing enzymes such as the E1 or E2 proteins. Shown to kill HEK293 cells growing in culture at higher concentration and during prolonged exposure.

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number533572
      Brand Family Calbiochem®
      SynonymsHECT Ligase Inhibitor, Compound III
      References
      ReferencesMund, T., et al. 2014. Proc. Natl. Acad. Sci. USA. 111, 16736.
      Product Information
      FormOff-white solid
      Hill FormulaC₁₇H₁₇NO₃
      Chemical formulaC₁₇H₁₇NO₃
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetHECT ligases
      Primary Target IC<sub>50</sub>6.8, 6.3 and 6.9 µ
      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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      HECT Ligase Inhibitor, Heclin - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Mund, T., et al. 2014. Proc. Natl. Acad. Sci. USA. 111, 16736.
      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.

      Revision20-November-2015 JSW
      SynonymsHECT Ligase Inhibitor, Compound III
      DescriptionA cell-permeable acrylamide compound that acts as a rapid, reversible, and broadly specific inhibitor of HECT ligases (IC50 = 6.8, 6.3, 6.9 µM for Smurf2, Nedd4, and WWP1, respectively). Does not affect the activity of RING domain ligases, hence allows clear distinction between RING and HECT-mediated ubiquitination. Binds to the HECT domain and disturbs the orientation of the C lobe, which allows reversible oxidation of the active site cysteine to the highly reactive sulfenic acid form. Does not inhibit other cysteine-containing enzymes such as the E1 or E2 proteins. Shown to kill HEK293 cells growing in culture at higher concentration and during prolonged exposure.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₇H₁₇NO₃
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage +2°C to +8°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
      ReferencesMund, T., et al. 2014. Proc. Natl. Acad. Sci. USA. 111, 16736.