SJYHJ-026
SJYHJ-026 is a PROTAC degrader targeting PXR, with a DC50 of 86.6 nM in SNU-C4 HiBiT-PXR KI cells. SJYHJ-026 shows higher selectivity for PXR over CAR, VDR, FXR, LXRα and LXRβ, and can bind to VHL to form a PXR-SJYHJ-026-VHL complex, inducing proteasomal degradation of PXR. SJYHJ-026 blocks agonist-induced PXR-mediated gene expression (including CYP3A4) and reduces basal PXR activity at the CYP3A4 promoter. SJYHJ-026 can be used for the research of colorectal cancer.
(Pink: Pregnane X Receptor (PXR) ligand (HY-169277); Blue: VHL ligand (HY-125845); Black: linker (HY-43048)).
For research use only. We do not sell to patients.
- Formula: C60H84N8O11S
- Molecular Weight:1125.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
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PXR 86.6 nM (DC50) |
SJYHJ-026 (dose-response range; 24 h) potently induces degradation of endogenous PXR in SNU-C4 HiBiT-PXR KI cells with a DC50 of 86.6 nM and 66.4% maximal degradation, and exhibits no significant cytotoxicity at concentrations up to 30 μM[1].
SJYHJ-026 (dose-response range; 24 h) potently induces degradation of endogenous PXR in SNU-C4 3xFLAG-PXR KI cells with a DC50 of ~50 nM and ~80% maximal degradation, as measured by western blot[1].
SJYHJ-026 (10 μM; 24 h) exhibits high specificity for PXR, with no off-target protein degradation detected in SNU-C4 cells treated with 10 μM for 24 h as measured by TMT-MS[1].
SJYHJ-026 does not degrade CAR, VDR, FXR, LXRα, or LXRβ, demonstrating selectivity for PXR among related nuclear receptors[1].
SJYHJ-026 binds to the PXR ligand binding pocket with higher affinity than most tested PROTAC analogs, supporting its potent PXR degradation activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SNU-C4 3xFLAG-PXR KI cells
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Concentration:dose-response range
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Incubation Time:24 h
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Result:Induced potent PXR degradation, with a DC50 of ~50 nM and a Dmax of ~80% as measured by western blot, representing improved degradation parameters compared to the HiBiT assay.
Chemical Information
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Molecular Weight 1125.42
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Formula C60H84N8O11S
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SMILES
O=C(NC1=CC(C(C)(C)C)=CC=C1O[C@@H](CC)CCC)C2=C(N(N=N2)C3=CC(OC)=C(C=C3OC)OCCCCCCOCCOCC(N[C@H](C(N4[C@@H](C[C@H](C4)O)C(NCC5=CC=C(C=C5)C6=C(N=CS6)C)=O)=O)C(C)(C)C)=O)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)