2. Signaling Pathways
  3. Vitamin D Related/Nuclear Receptor
  4. Pregnane X Receptor (PXR)
  5. Pregnane X Receptor (PXR) Degrader

Pregnane X Receptor (PXR) Degrader

Pregnane X Receptor (PXR) Degraders (3):

Cat. No. Product Name Effect Purity
  • HY-175266
    MI1013
    		Degrader 99.10%
    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).
  • HY-169264
    SJYHJ-026
    		Degrader
    SJYHJ-026 (compound 37) is a pregnane X receptor (PXR) PROTAC degrader with the DC50 of 86.6 nM and maximal degradation of 66.4%. SJYHJ-026 shows cell cytotoxic aganist SNU-C4 HiBiT-PXR KI cells with the IC50 values of 97.4 μM (24 h) and 99.5 μM (72 h) (Blue: VHL ligand HY-125845,Black: linker HY-43048；Pink: PXR inhibitor HY-169277).
  • HY-169279
    PROTAC SMARCA2/4-degrader-34
    		Degrader
    PROTAC SMARCA2/4-degrader-34 (compound 38) is a potent is a potent SMARCA2 and SMARCA4 PROTAC degrader. PROTAC SMARCA2/4-degrader-34 shows PXR binding affinity with DC50 value of 85.1 nM. PROTAC SMARCA2/4-degrader-34 decreases the protein expression of 3xFLAG-PXR. (Pink: Ligand for target protein (HY-169280); Black: Linker (HY-43048); Blue: Ligand for E3 ligase (HY-125845).