MI1013

MI1013 is a PROTAC PXR degrader (DC50 = 89 nM, Dmax = 82%). MI1013 degrades PXR in human hepatocellular carcinoma RG cells (HepaRG). MI1013 specifically and safely regulates CYP3A4 promoter activity through PXR degradation. MI1013 affects several key genes involved in sulfate conjugation (e.g., SULT1E1), bile acid synthesis (CYP7A1), gluconeogenesis (PCK1), ketone synthesis (HMGCS20), and hepatocyte proliferation (MKI67). (Pink: PXR ligand 3: HY-175267, Blue: Pomalidomide-propargyl ligand: HY-W410002, Pink + Black: PXR ligand-Linker Conjugate 1: HY-175268).

C42H46N10O12S

914.94

O=C(NC1=CC=C(S(=O)(C2=C(C)N(C3=CC(OC)=CC=C3OC)N=N2)=O)C=C1)CCOCCOCCOCCN4N=NC(CNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)=C4

Cytochrome P450; Pregnane X Receptor (PXR) ; PROTACs

Cereblon; CYP3

95.48

-20°C, 3 years; 4°C, 2 years (Powder)

Room Temperature