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MI1013

Chemical Structure : MI1013

CAS No.:

MI1013 (MI-1013)

Catalog No.: PC-24991Not For Human Use, Lab Use Only.

MI1013 is a potent, selective CRBN-base PROTAC degrader of pregnane X receptor (PXR) designed by connecting SPA70 and pomalidomide with PEG linker, has DC50 of 89 nM and Dmax of 82% in HepaRG cells.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

MI1013 is a potent, selective CRBN-base PROTAC degrader of pregnane X receptor (PXR) designed by connecting SPA70 and pomalidomide with PEG linker, has DC50 of 89 nM and Dmax of 82% in HepaRG cells.
The proteasome inhibitor MG132 prevented the MI1013-induced degradation of PXR, confirming the involvement of the proteasome pathway.
MI1013 does not degrade RXRα and GSPT1.
MI1013 demonstrates a concentration-dependent inhibition of PXR activation by rifampicin.

Physicochemical Properties

M.Wt 914.95
Formula C42H46N10O12S
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
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Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(4-((1-(2,5-dimethoxyphenyl)-5-methyl-1H-1,2,3-triazol-4-yl)sulfonyl)phenyl)-3-(2-(2-(2-(4-(((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)methyl)-1H-1,2,3-triazol-1-yl)ethoxy)ethoxy)ethoxy)propanamide

References

1. Kamaraj R, et al. J Med Chem. 2025 Jul 12. doi: 10.1021/acs.jmedchem.4c03134.

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