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Inhibitor Report for: ALT-PG2

sEH-targeting PROTAC (Proteolysis-targeting chimera) ALT-PG2 degrades this protein at low nanomolar concentration in the human hepatoma-derived Huh-7 cell line and in primary mouse hepatocytes


General
Type Urea derivative, Trifluo, PROTAC, Multitarget
Chemical_Nomenclature
Canonical SMILES C1(=CC=C(C=C1)C(=O)N(CCOCCOCCOCCN(C(=O)COC2=C3C(=CC=C2)C(N(C3=O)C4C(N(C(CC4)=O)[H])=O)=O)[H])[H])O[C@@H]5CC[C@H](CC5)N(C(=O)N(C6=CC=C(C=C6)OC(F)(F)F)[H])[H].CC
InChI InChI=1S/C44H49F3N6O13.C2H6/c45-44(46,47)66-32-14-8-29(9-15-32)51-43(60)50-28-6-12-31(13-7-28)65-30-10-4-27(5-11-30)39(56)49-19-21-62-23-25-63-24-22-61-20-18-48-37(55)26-64-35-3-1-2-33-38(35)42(59)53(41(33)58)34-16-17-36(54)52-40(34)57;1-2/h1-5,8-11,14-15,28,31,34H,6-7,12-13,16-26H2,(H,48,55)(H,49,56)(H2,50,51,60)(H,52,54,57);1-2H3/t28-,31-,34?;
InChIKey CTXVVVILCJCWDW-FBWMZPCKSA-N
Other name(s)
________________________________________________________________________________________________
MW|956.96
Formula|C46H55F3N6O13
CAS_number|
PubChem|
UniChem|CTXVVVILCJCWDW-FBWMZPCKSA-N
IUPHAR|
Wikipedia|

Target
Families | ALT-PG2 ligand of proteins in family: Epoxide_hydrolase
Protein | human-EPHX2

References:
Search PubMed for references concerning: ALT-PG2
    Title: Soluble epoxide hydrolase-targeting PROTAC activates AMPK and inhibits endoplasmic reticulum stress
    Peyman M, Barroso E, Turcu AL, Estrany F, Jr., Smith D, Jurado-Aguilar J, Rada P, Morisseau C, Hammock BD and Vazquez-Carrera M <4 more author(s)>
    Ref: Biomed Pharmacother, 168:115667, 2023 : PubMed

            

    Title: PROTAC-Mediated Selective Degradation of Cytosolic Soluble Epoxide Hydrolase Enhances ER Stress Reduction
    Wang Y, Morisseau C, Takamura A, Wan D, Li D, Sidoli S, Yang J, Wolan DW, Hammock BD, Kitamura S
    Ref: ACS Chemical Biology, :, 2023 : PubMed