DI-1548
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].
Product Specifications
CAS Number
2247060-97-3
UNSPSC
12352005
Target
E1/E2/E3 Enzyme; Keap1-Nrf2
Related Pathways
Metabolic Enzyme/Protease; NF-κB
Applications
Metabolism-protein/nucleotide metabolism
Field of Research
Metabolic Disease
Smiles
C=C(CN1CCOCC1)C(NC[C@H](C2CCCCC2)NC([C@@H](NC(CC)=O)CC(SC3=C4)=NC3=CC=C4C(C)C)=O)=O
Molecular Formula
C32H47N5O4S
Molecular Weight
597.81
References & Citations
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Frequently Asked Questions
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