Soluble Epoxide Hydrolase PROTAC 1a

Referentie NB-64-44352-5mg

Formaat : 5mg

Merk : Neo Biotech


Soluble Epoxide Hydrolase PROTAC 1a (Synonyms: Soluble Epoxide Hydrolase Proteolysis-targeting Chimera 1a, sEH ...)

Catalog No. T83857 Copy Product Info
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.

Soluble Epoxide Hydrolase PROTAC 1a

Copy Product Info
Synonyms Soluble Epoxide Hydrolase Proteolysis-targeting Chimera 1a, sEH Proteolysis-targeting Chimera 1a, sEH PROTAC 1a

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.

Soluble Epoxide Hydrolase PROTAC 1a

Product Introduction

Bioactivity
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.
SynonymsSoluble Epoxide Hydrolase Proteolysis-targeting Chimera 1a, sEH Proteolysis-targeting Chimera 1a, sEH PROTAC 1a
Chemical Properties
Molecular Weight971.00
FormulaC46H53F3N6O14
SmilesO=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
Storage & Solubility Information
StorageShipping with blue ice/Shipping at ambient temperature.