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) [1].
Product Specifications
UNSPSC
12352005
Target
Cytochrome P450; Pregnane X Receptor (PXR) ; PROTACs
Related Pathways
Metabolic Enzyme/Protease; PROTAC; Vitamin D Related/Nuclear Receptor
Applications
Metabolism-sugar/lipid metabolism
Field of Research
Metabolic Disease
Purity
95.48
Smiles
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
Molecular Formula
C42H46N10O12S
Molecular Weight
914.94
References & Citations
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Cereblon; CYP3
Available Sizes
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