MI1013 is a PROTAC PXR degrader with a DC50 of 89 nM and a Dmax of 82%. It degrades PXR in human liver cancer RG cells (HepaRG) and modulates CYP3A4 promoter activity with specificity and safety through PXR degradation. MI1013 influences key genes involved in sulfate conjugation (e.g., SULT1E1), bile acid synthesis (CYP7A1), gluconeogenesis (PCK1), ketogenesis (HMGCS20), and hepatocyte proliferation (MKI67).
Target:
Others|||PROTACs|||Cytochromes P450
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