Heclin has been used as a HECT-type ubiquitin E3 ligase inhibitor in human embryonic kidney (HEK293) cells. It has also been used to test its effect on dandelion-induced chloride channel protein (ClC-Ka) inhibition in HEK293 cells and fibroblast-like COS-7 cell line.
Biochem/physiol Actions
Heclin is not effective in inhibiting E1 or E2 proteins.
Heclin is a selective reversible inihbitor of HECT E3 ubiquitin ligases. Heclin inhibited Nedd4, Smurf2 and WWP1 with IC50 values of 6.3 µM, 6.8 µM and 6.9 µM, respectively, and inhibited autoubiquitination of the Smurf2 HECT domain in vivo with an IC50 value of 9 µM. Heclin had no effect on the auto-ubiquitination of the RING domain ligase Mdm2.