Soluble Epoxide Hydrolase PROTAC 1a

SKU: orb1980008

Description

Soluble epoxide hydrolase (sEH) PROTAC 1a is a proteolysis-targeting chimera (PROTAC) comprising a cereblon ligand linked to the sEH inhibitor t-TUCB via a linker, promoting selective sEH degradation and inhibiting its hydrolase activity (IC50 = 0.8 nM) significantly more than its phosphatase activity (IC50 = >10,000 nM). This compound preferentially targets cytosolic sEH for lysosomal rather than proteasomal degradation. Furthermore, it mitigates thapsigargin-induced upregulation of phosphorylated inositol-requiring enzyme 1α (IRE1α) and X-box binding protein 1 (XBP1) splicing in HepG2 and 293T cells, thereby reducing endoplasmic reticulum stress.

Key Properties

• MW: 971.00
• Formula: C₄₆H₅₃F₃N₆O₁₄
• SMILES: O=C(N(C1C(NC(CC1)=O)=O)C2=O)C(C2=CC=C3)=C3OCC(NCCOCCOCCOCCOCCNC(C4=CC=C(O[C@H]5CC[C@H](NC(NC6=CC=C(OC(F)(F)F)C=C6)=O)CC5)C=C4)=O)=O
• Target: Others

Storage & Handling

• Storage: -20°C
• Disclaimer: For research use only

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Gene Symbol

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