Application

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.

Packaging

5, 25 mg in glass bottle