2247061-09-0
Chemical Structure
DI-1859
- CAS No.: 2247061-09-0
- Formula:C30H45N5O3S
- Molecular Weight:555.78
IUPAC Name: (4-amino-3-bromo-5-fluorophenyl)methanol
InChIKey: HNIUOJXOXQUOMN-LOSJGSFVSA-N
SMILES: CN(C)CC(C(NC[C@H](C1CCCCC1)NC([C@@H](NC(CC)=O)CC(SC2=C3)=NC2=CC=C3C(C)C)=O)=O)=C
Biological Activity: DI-1859 is a DCN1 and cullin 3 inhibitor with a Ki of <1 nM against human DCN1. DI-1859 forms a covalent bond with Cys115 of DCN1, cleaves its dimethylamino group, disrupts the DCN1-UBC12 interaction, and selectively inhibits the neddylation modification of cullin 3 relative to other cullins. DI-1859 inactivates CRL3, promotes the accumulation of NRF2 and SLC7A11, upregulates the expression of HO-1 and NQO1, reduces reactive oxygen species (ROS) levels, enhances insulin signaling, promotes insulin secretion, activates RhoA, regulates the phosphorylation of AKT, without completely blocking the neddylation modification of cullin 3 or restoring the expression of IRS-1. DI-1859 can be used in the research of Acetaminophen (HY-66005)-induced hepatotoxicity, hyperglycemia, metabolic dysfunction-associated steatotic liver disease, insulin resistance, breast cancer and lung cancer[1][2][3][4].
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DI-1859 | 99.62% | DI-1859 is a DCN1 and cullin 3 inhibitor with a Ki of <1 nM against human DCN1. DI-1859 forms a covalent bond with Cys115 of DCN1, cleaves its dimethylamino group, disrupts the DCN1-UBC12 interaction, and selectively inhibits the neddylation modification of cullin 3 relative to other cullins. DI-1859 inactivates CRL3, promotes the accumulation of NRF2 and SLC7A11, upregulates the expression of HO-1 and NQO1, reduces reactive oxygen species (ROS) levels, enhances insulin signaling, promotes insulin secretion, activates RhoA, regulates the phosphorylation of AKT, without completely blocking the neddylation modification of cullin 3 or restoring the expression of IRS-1. DI-1859 can be used in the research of Acetaminophen (HY-66005)-induced hepatotoxicity, hyperglycemia, metabolic dysfunction-associated steatotic liver disease, insulin resistance, breast cancer and lung cancer. | ||||||||||||||||||||
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References
- [1]. Zhou H, et al. Selective inhibition of cullin 3 neddylation through covalent targeting DCN1 protects mice from acetaminophen-induced liver toxicity. Nature communications. 2021 May 11;12(1):2621. [Content Brief]
- [2]. Gu L, et al. A selective Cullin 3 RING E3 ligase inhibitor attenuates hyperglycemia via dual insulin sensitizing and insulinotropic action. bioRxiv [Preprint]. 2026 Feb 1:2026.01.28.702366. [Content Brief]
- [3]. Upadhyay KK, et al. The inner nuclear membrane protein SUN1 regulates cullin-3 neddylation to maintain insulin signaling. bioRxiv [Preprint]. 2026 Apr 20:2026.04.16.718478. [Content Brief]
- [4]. Zhou Q, et al. The CRL3 ubiquitin ligase-USP18 axis coordinately regulates cystine uptake and ferroptosis by modulating SLC7A11. Proceedings of the National Academy of Sciences of the United States of America. 2024 Jul 09;121(28):e2320655121. [Content Brief]
