LC-MI-3

Chemical Structure : LC-MI-3

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货号: 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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25 mg		Get quote
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100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	744.77
分子式	C39H36N8O8
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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

LC-MI-3

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LC-MI-3

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