3053823-69-8
Chemical Structure
LC-MI-3
- CAS No.: 3053823-69-8
- Formula:C39H36N8O8
- Molecular Weight:744.75
InChIKey: DUEGKYWYMGQGDW-UHFFFAOYSA-N
SMILES: O=C1N(C(C2=C1C=C(C=C2)C#CCOCCC(N3CCN(CC3)C4=CC=C(C(OC)=C4)NC(C5=CC=CC(C6=CC=NN6)=N5)=O)=O)=O)C7CCC(NC7=O)=O
Biological Activity: LC-MI-3 is an orally active IRAK4 degrader with an IC50 of 57.2 nM and high selectivity among human protein kinases[1][2].LC-MI-3 eliminates IRAK4 kinase and scaffolding functions via the cereblon E3 ubiquitin ligase and ubiquitin-proteasome systems[1][2].LC-MI-3 inhibits downstream nuclear factor-κB and IRAK4-mediated inflammatory signaling pathways[1][2].LC-MI-3 exerts anti-inflammatory activity in lipopolysaccharide-, Escherichia coli-, TLR4-, and TLR7-induced inflammatory models[1][2].LC-MI-3 can be used for the research of acute lung injury, sepsis, psoriasis, and inflammatory diseases[1][2][3].
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LC-MI-3 | LC-MI-3 is an orally active IRAK4 degrader with an IC50 of 57.2 nM and high selectivity among human protein kinases.LC-MI-3 eliminates IRAK4 kinase and scaffolding functions via the cereblon E3 ubiquitin ligase and ubiquitin-proteasome systems.LC-MI-3 inhibits downstream nuclear factor-κB and IRAK4-mediated inflammatory signaling pathways.LC-MI-3 exerts anti-inflammatory activity in lipopolysaccharide-, Escherichia coli-, TLR4-, and TLR7-induced inflammatory models.LC-MI-3 can be used for the research of acute lung injury, sepsis, psoriasis, and inflammatory diseases. | |||||||||||||||||||||
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- [1]. Chen L, et al. Discovery of LC-MI-3: A Potent and Orally Bioavailable Degrader of Interleukin-1 Receptor-Associated Kinase 4 for the Treatment of Inflammatory Diseases. Journal of medicinal chemistry. 2024 May 23;67(10):8060-8076. [Content Brief]
- [2]. Lin Y, et al. Interleukin-1 Receptor-Associated Kinase 4 (IRAK4) Degraders for Treating Inflammatory Diseases: Advances and Prospects. Journal of medicinal chemistry. 2025 Jan 23;68(2):902-914. [Content Brief]
- [3]. Fan Y, et al. Discovery of Rigid Linker-Based IRAK4 PROTACs with Improved Metabolic Stability for the Treatment of Inflammatory Diseases. Journal of medicinal chemistry. 2025 Aug 28;68(16):17874-17896. [Content Brief]
Keywords
