1-Benzyl-I3C is a NEDD4-1 inhibitor with significant anticancer activity. 1-Benzyl-I3C can directly inhibit the ubiquitination activity of NEDD4-1 with an IC50 of 12.3µM, which is significantly better than its precursor compound I3C of 284µM. 1-Benzyl-I3C and its analogs showed good effects in inhibiting the proliferation of human melanoma cells, which is roughly related to their potency as NEDD4-1 enzyme inhibitors. By combining in vitro ubiquitination experiments and thermal stability analysis, 1-Benzyl-I3C was shown to be able to bind to the catalytic HECT domain of NEDD4-1[1].
Molekulargewicht:
237.30
Reinheit:
99.68
CAS Nummer:
[60941-76-6]
Formel:
C16H15NO
Target-Kategorie:
E1/E2/E3 Enzyme
Anwendungsbeschreibung:
MCE Product type: Natural Products
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