Formulation: A solid
Formal Name: N-(1-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)-2-oxo-6,9,12,15-tetraoxa-3-azaheptadecan-17-yl)-4-(((1r,4r)-4-(3-(4-(trifluoromethoxy)phenyl)ureido)cyclohexyl)oxy)benzamide
Purity: ≥95%
Formula Markup: C46H53F3N6O14
Formula Weight: 971
Shelf life (days): 1095
Notes: 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.{51387} 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.
English
Deutsch
