533572 Sigma-AldrichHECT Ligase Inhibitor, Heclin - Calbiochem

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.