DI-1548 is a potent, selective, and irreversible covalent inhibitor of DCN1 (IC50 = 4.6 nM). DI-1548 potently and selectively inhibits cullin 3 neddylation at nanomolar concentrations, and exhibits no obvious effect on the neddylation of other cullin members (including cullin 1, 2, 4A, 4B, and 5). DI-1548 exhibits no cytotoxicity. DI-1548 covalently binds to DCN1, disrupting the DCN1-UBC12 interaction, causing the collapse of the neddylation complex, inactivating CRL3, leading to NRF2 accumulation and upregulation of its target genes, and ultimately protecting mice from liver damage. DI-1548 can be used in liver injury research[1].
Molekulargewicht:
597.81
CAS Nummer:
[2247060-97-3]
Formel:
C32H47N5O4S
Target-Kategorie:
E1/E2/E3 Enzyme,Keap1-Nrf2
Anwendungsbeschreibung:
MCE Product type: Reference compound
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