Chemical Structure : LC-MI-3
CAS No.:
LC-MI-3
Catalog No.: PC-22314Not For Human Use, Lab Use Only.
LC-MI-3 is a potent, selective and orally bioavailable PROTAC degrader of interleukin-1 receptor-associated kinase 4 (IRAK4) with DC50 of 47.3 nM in RAW264.7 cells, Dmax of 91%.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
LC-MI-3 is a potent, selective and orally bioavailable PROTAC degrader of interleukin-1 receptor-associated kinase 4 (IRAK4) with DC50 of 47.3 nM in RAW264.7 cells, Dmax of 91%.
LC-MI-3-induced CRBN recruitment promotes IRAK4 ubiquitination and degradation, via the ubiquitin/proteasome system.
LC-MI-3 does not degrader RIOK1 IKZF1, IKZF3, and SALL4.
LC-MI-3 treatment shows potency to normalize LPS-induced interleukin-6 (IL-6) and tumor necrosis factor α (TNFα) mRNA expression as well as cytokine production in macrophages.
LC-MI-3 (20 mg/kg) suppresses lung injury in the LPS-induced mouse ALI model, attenuates Escherichia coli-induced inflammatory reaction and sepsis, suppresses the TLR7-mediated inflammatory reaction in the TLR7-driven psoriasis model.
Physicochemical Properties
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M.Wt
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744.77
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Formula
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C39H36N8O8
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(4-(4-(3-((3-(2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)prop-2-yn-1-yl)oxy)propanoyl)piperazin-1-yl)-2-methoxyphenyl)-6-(1H-pyrazol-5-yl)picolinamide
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References
1. Lingfeng Chen, et al. J Med Chem. 2024 May 9. doi: 10.1021/acs.jmedchem.4c00181.
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