Description
Soluble epoxide hydrolase (sEH) PROTAC 1a is a proteolysis-targeting chimera (PROTAC) that contains cereblon ligand 1 (Item No. 21589) connected to the sEH inhibitor t-TUCB (Item No. 36384) by a linker region.1 It drives sEH degradation and selectively inhibits the hydrolase activity of sEH (IC50 = 0.8 nM) over its phosphatase activity (IC50 = >10,000 nM). sEH PROTAC 1a is also selective for the degradation of cytosolic over peroxisomal sEH and drives its degradation via the lysosome rather than the proteasome. It reduces thapsigargin-induced increases in phosphorylated inositol-requiring enzyme 1α (IRE1α) levels and X-box binding protein 1 (XBP1) splicing in HepG2 and 293T cells, indicating a reduction in ER stress.WARNING This product is not for human or veterinary use.
