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NJH-2-057

Chemical Structure : NJH-2-057

CAS No.: 2858812-70-9

NJH-2-057 (DUBTAC NJH-2-057)

Catalog No.: PC-72837Not For Human Use, Lab Use Only.

NJH-2-057 is a novel CFTR DUBTAC via linking the OTUB1 recruiter EN523 to the CFTR chaperone lumacaftor with C5 alkyl linkers.

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    Biological Activity

    NJH-2-057 is a novel CFTR DUBTAC via linking the OTUB1 recruiter EN523 to the CFTR chaperone lumacaftor with C5 alkyl linkers.
    NJH-2-057 robustly stabilizes ΔF508-CFTR protein levels, leading to improved chloride channel conductance in human cystic fibrosis bronchial epithelial cells.
    Deubiquitinase-targeting chimeras (DUBTACs), heterobifunctional small molecules consisting of a deubiquitinase recruiter linked to a protein-targeting ligand, to stabilize the levels of specific proteins degraded in a ubiquitin-dependent manner.

    Physicochemical Properties

    M.Wt 810.856
    Formula C43H44F2N6O8
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    O=C(NCCCCCNC(CCC1=CC=C(N2C(CN(C(C=C)=O)CC2)=O)O1)=O)C3=CC=CC(C4=NC(NC(C5(C6=CC=C(OC(F)(F)O7)C7=C6)CC5)=O)=CC=C4C)=C3

    References

    1. Henning NJ, et al. Nat Chem Biol. 2022 Feb 24. doi: 10.1038/s41589-022-00971-2.

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