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UCI-LC0023

Chemical Structure : UCI-LC0023

CAS No.: 1357615-72-5

UCI-LC0023 (UCI-LC 0023)

Catalog No.: PC-49216Not For Human Use, Lab Use Only.

UCI-LC0023 is a small molecule that restores mutant p53 activity by targeting the cryptic L1/S3 pocket of p53, directly binds to mutant p53 and restores wild-type-like conformation of mutant p53R175H.

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    Biological Activity

    UCI-LC0023 is a small molecule that restores mutant p53 activity by targeting the cryptic L1/S3 pocket of p53, directly binds to mutant p53 and restores wild-type-like conformation of mutant p53R175H.
    Treatment of TOV112D cells with UCI-LC0023 increased the detection with wild-type specific antibodies and decreased the p53R175H mutant specific signal.
    UCI-LC0023 restores DNA binding of p53 mutants (R175H, Y220C, R248W, R282W, R273H, G245S) in vitro and in vivo and induces p53 target gene expression.
    UCI-LC0023 is sufficient to correct the DNA binding defect of p53R175H.
    UCI-LC0023 induces restoration of site-specific DNA binding of the p53R175H mutant to the promoters of the p53-dependent genes p21 and PUMA in TOV112D cells as demonstrated by ChIP.

    Physicochemical Properties

    M.Wt 293.282
    Formula C16H11N3O3
    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

    (E)-1-(1H-benzo[d]imidazol-2-yl)-3-(3-nitrophenyl)prop-2-en-1-one

    References

    1. Geetha Durairaj, et al. Cell Chem Biol. 2022 Aug 9;S2451-9456(22)00275-6.

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