Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | 35 days | $ 575.00 | |
5 mg | 35 days | $ 2,580.00 |
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. |
Synonyms | sEH Proteolysis-targeting Chimera 1a, Soluble Epoxide Hydrolase Proteolysis-targeting Chimera 1a, sEH PROTAC 1a |
Molecular Weight | 971.00 |
Formula | C46H53F3N6O14 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Soluble Epoxide Hydrolase PROTAC 1a sEH Proteolysis-targeting Chimera 1a Soluble Epoxide Hydrolase Proteolysis-targeting Chimera 1a sEH PROTAC 1a inhibitor inhibit