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533572 HECT Ligase Inhibitor, Heclin - Calbiochem

HECT Ligase Inhibitor, Heclin, is a cell-permeable reversible, broadly specific inhibitor of HECT ligases (IC₅₀ = 6.8, 6.3, 6.9 mM for Smurf2, Nedd4, and WWP, respectively).

HECT Ligase Inhibitor, Heclin - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: HECT Ligase Inhibitor, Compound III

Primary Target: HECT ligases
533572
  
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₇H₁₇NO₃
Description
Overview

This product has been discontinued.



A 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
Global Trade Item Number
Catalogue Number GTIN
533572 0

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 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 3 months at -20°C.
Toxicity Standard Handling
ReferencesMund, T., et al. 2014. Proc. Natl. Acad. Sci. USA. 111, 16736.