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Inhibitor Report for: SR-4559

Directly binds ABHD5 and stimulate lipolysis by releasing it from PLIN, thereby mimicking the effects of extracellular signaling in the absence of PKA-dependent phosphorylation of HSL and PLIN ABHD5 IC50 2.379 microM relatively good inhibitor


General
Type Piperazine, Sulfur Compound, Sulfonamide, Benzofuran
Chemical_Nomenclature 1-[4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)piperazin-1-yl]-2-(6-methyl-1-benzofuran-3-yl)ethanone
Canonical SMILES CC1=CC2=C(C=C1)C(=CO2)CC(=O)N3CCN(CC3)S(=O)(=O)C4=CC5=C(C=C4)OCCO5
InChI InChI=1S/C23H24N2O6S/c1-16-2-4-19-17(15-31-21(19)12-16)13-23(26)24-6-8-25(9-7-24)32(27,28)18-3-5-20-22(14-18)30-11-10-29-20/h2-5,12,14-15H,6-11,13H2,1H3
InChIKey HJVYLFAPJPGKEE-UHFFFAOYSA-N
Other name(s) SR-01000604559 ; SR4559 ; MLS000863888 ; SMR000068843 ; AC1MBBZL ; BDBM94640 ; CHEMBL1312711 ; ZINC3557087
________________________________________________________________________________________________
MW|456.5
Formula|C23H24N2O6S
CAS_number|847939-23-5
PubChem|2674365
UniChem|HJVYLFAPJPGKEE-UHFFFAOYSA-N
IUPHAR|
Wikipedia|

Target
Families | SR-4559 ligand of proteins in family: CGI-58_ABHD5_ABHD4
Protein | human-ABHD5, mouse-abhd5

References:
Search PubMed for references concerning: SR-4559
    Title: Molecular Modeling of ABHD5 Structure and Ligand Recognition
    Shahoei R, Pangeni S, Sanders MA, Zhang H, Mladenovic-Lucas L, Roush WR, Halvorsen G, Kelly CV, Granneman JG, Huang YM
    Ref: Front Mol Biosci, 9:935375, 2022 : PubMed

            

    Title: Novel Pharmacological Probes Reveal ABHD5 as a Locus of Lipolysis Control in White and Brown Adipocytes
    Rondini EA, Mladenovic-Lucas L, Roush WR, Halvorsen GT, Green AE, Granneman JG
    Ref: Journal of Pharmacology & Experimental Therapeutics, 363:367, 2017 : PubMed

            

    Title: Endogenous and Synthetic ABHD5 Ligands Regulate ABHD5-Perilipin Interactions and Lipolysis in Fat and Muscle
    Sanders MA, Madoux F, Mladenovic L, Zhang H, Ye X, Angrish M, Mottillo EP, Caruso JA, Halvorsen G and Granneman JG <3 more author(s)>
    Ref: Cell Metab, 22:851, 2015 : PubMed