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Heclin is an inhibitor of HECT E3 ubiquitin ligases (IC50s = 6.8, 6.3, and 6.9 μM for Smurf2, Nedd4, and WWP1 HECT ligase domains, respectively).1 It inhibits autoubiquitination of Smurf2 in HEK293 cells expressing the human enzyme (IC50 = 9 μM) and reduces ubiquitination of Dishevelled 2 in HEK293 cells expressing Smurf2, Nedd4, or WWP2. Heclin is cytotoxic to HEK293 cells (IC50 = 45 μM).
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