PROTAC sEH degrader-2
PROTAC sEH degrader-2 is a soluble epoxide hydrolase (sEH) PROTAC degrader, with pIC50 values of 8.37 and 7.12 against hsEH-H and msEH-H, respectively. PROTAC sEH degrader-2 induces targeted degradation of sEH via the ubiquitin-proteasome system, thereby completely blocking its dual functions as an epoxide hydrolase and a lipid phosphatase by bridging the short-branch exit of sEH with the CRBN E3 ubiquitin ligase. PROTAC sEH degrader-2 can be used in the research of neuroinflammation and Alzheimer's disease.
(Pink: sEH ligand (HY-174225); Blue: Cereblon ligand (HY-103597); Black: linker).
For research use only. We do not sell to patients.
- Formula: C54H57F4N9O13S
- Molecular Weight:1148.14
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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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hsEH-H 8.37 (pIC50) |
msEH-H 7.12 (pIC50) |
PROTAC sEH degrader-2 (Compound 23) (3 nM-3 μM; 1-24 h) induces dose- and time-dependent degradation of sEH in HeLasEH-HiBiT cells[1].
PROTAC sEH degrader-2 (3 μM; 3 h) significantly reduces the conversion of 14 (15)-, 11 (12)-, and 8 (9)-EpETrE into their corresponding DiHETrE metabolites in HeLasEH-HiBiT cell homogenates[1].
PROTAC sEH degrader-2 (300 nM; 18 h) significantly reduces sEH expression levels in LPS (HY-D1056)- and IFNγ-activated human M1 macrophages, primary mouse hepatocytes, and precision-cut lung slices (PCLS)[1].
PROTAC sEH degrader-2 (up to 50 μM; 72 h) does not induce significant cytotoxicity in HepG2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human M1 macrophages (activated by LPS and IFNγ)
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Concentration:300 nM
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Incubation Time:18 h
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Result:Successfully triggered sEH degradation in primary human M1 macrophages.
Significantly downregulating sEH expression levels (approx. 10% residual expression) compared to the untreated group, while the inactive control 31 was ineffective.
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Cell Line:Primary murine hepatocytes
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Concentration:300 nM
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Incubation Time:18 h
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Result:Elicited significant degradation of sEH protein in primary murine hepatocytes (approx. 60% residual expression), though the degradation efficiency was lower than that observed in human macrophages.
Chemical Information
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Molecular Weight 1148.14
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Formula C54H57F4N9O13S
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SMILES
O=C(NCC1=C(C=C(C=C1)NS(=O)(CCCC2=CN(N=N2)CCOCCOCCOCCOCCNC(COC3=C(C(N(C4C(NC(CC4)=O)=O)C5=O)=O)C5=CC=C3)=O)=O)C(F)(F)F)C6=CC=C7N(C=CC7=C6)CC8=CC=CC(F)=C8
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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 sEH degrader-2
- PROTAC sEH degrader2
- PROTAC sEH degrader 2
- PROTACs
- Epoxide Hydrolase
- primary mouse hepatocytes
- soluble epoxide hydrolase
- ubiquitinylation
- HepG2 cells
- precision-cut lung slices
- HeLasEH-HiBiT cells
- rat liver microsomes
- human M1 macrophages
- cereblon
- mouse liver microsomes
- Inhibitor
- inhibitor
- inhibit