PROTAC PXR degrader-1
PROTAC PXR degrader-1 is a PROTAC degrader targeting PXR, with a DC50 value of 49.8 nM in SNU-C4 3xFLAG-PXR KI cells. PROTAC PXR degrader-1 exhibits selectivity towards CAR, VDR, FXR, LXRα and LXRβ. PROTAC PXR degrader-1 induces the formation of a ternary complex with PXR and VHL, triggering proteasomal degradation of PXR. PROTAC PXR degrader-1 reduces both agonist-induced and basal PXR-mediated CYP3A4 promoter activation, and decreases the expression of endogenous CYP3A4 gene in cancer cells. PROTAC PXR degrader-1 enhances the cytotoxic effect of paclitaxel on cancer cells. PROTAC PXR degrader-1 can be used for the research of colorectal cancer.
(Pink: Pregnane X Receptor (PXR) ligand (HY-169280); Blue: VHL ligand (HY-125845); Black: linker (HY-43048)).
For research use only. We do not sell to patients.
- Formula: C58H78N8O13S
- Molecular Weight:1127.35
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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PXR 49.8 nM (DC50) |
PROTAC PXR degrader-1 (compound 38) (0.05-0.085 μM; 24 h) potently degrades endogenous PXR in SNU-C4 HiBiT-PXR KI cells with an approximate DC50 of 85 nM and ~65% maximal degradation, and in SNU-C4 3xFLAG-PXR KI cells with an approximate DC50 of 50 nM and ~80% maximal degradation[1].
PROTAC PXR degrader-1 binds to the PXR ligand binding domain with higher affinity than most tested PROTAC analogs, though binding affinity does not fully correlate with its PXR degradation activity[1].
PROTAC PXR degrader-1 (10 μM; 24 h) shows no detectable off-target protein degradation in SNU-C4 cells when tested at 10 μM for 24 hours[1].
PROTAC PXR degrader-1 inhibits agonist-induced and basal PXR transcriptional activity in SNU-C4 cells, reducing CYP3A4 promoter activity and endogenous CYP3A4 gene expression[1].
PROTAC PXR degrader-1 induces PXR degradation via the expected mechanism of CRL2(VHL) recruitment and proteasomal degradation[1].
PROTAC PXR degrader-1 enhances the anticancer activity of paclitaxel in SNU-C4 cells by 3.3-fold[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 1127.35
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Formula C58H78N8O13S
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SMILES
O=C(C1=CC=C(C(NC(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)=O)=C1)O[C@@H](CC)CCC)OC
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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)
PROTAC PXR degrader-1 Related Classifications
HY-169279 Related Classifications
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