Biological Activity:

Heclin is a selective HECT E3 ubiquitin ligase inhibitor, inhibits Nedd4, Smurf2 and WWP1 with IC50 6.3, 6.8 and 6.9 μM respectively. It is selective for HECT-mediated over RING-mediated ubiquitination. Heclin does not block E2 binding but causes a conformational change that results in oxidation of the active site Cys. It kills HEK293 cells growing in culture, consistent with an essential role for HECT ligase activity in mammalian cells.

How to Use:

In vitro: Heclin was used at 10-30 µM final concentration in various in vitro assays.
In vivo: n/a

Reference:

• 1. Mund T, et al. Peptide and small molecule inhibitors of HECT-type ubiquitin ligases. (2014) Proc Natl Acad Sci USA. 111(47):16736-41.