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LC-MI-3

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

M.Wt 744.77
Formula C39H36N8O8
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Lingfeng Chen, et al. J Med Chem. 2024 May 9. doi: 10.1021/acs.jmedchem.4c00181.

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