DI-1548

• Description:

  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].

• 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:

  [1]Zhou H, et al. Selective inhibition of cullin 3 neddylation through covalent targeting DCN1 protects mice from acetaminophen-induced liver toxicity. Nat Commun. 2021 May 11;12 (1) :2621.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• CAS Number:

  [2247060-97-3]