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A452

Chemical Structure : A452

CAS No.: 798543-42-7

A452 (HDAC6 inhibitor A452)

Catalog No.: PC-38796Not For Human Use, Lab Use Only.

A452 is a potent and selective HDAC6 inhibitor, effectively inhibits the cell growth and viability of various cancer cell types, irrespective of p53 status.

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    Biological Activity

    A452 is a potent and selective HDAC6 inhibitor, effectively inhibits the cell growth and viability of various cancer cell types, irrespective of p53 status.
    A452 induced apoptosis by activated caspase 3 and PARP, increased Bak and Bax and decreased Bcl-xL.
    A452 increased wild-type p53 levels by destabilizing MDM2, but decreased mutant p53 by inducing MDM2 and inhibiting Hsp90-mutant p53 complex formation.
    A452 blocked HDAC6 nuclear localization, resulting in increased levels of acetylated p53 at Lys381/382.
    A452 disrupted the HDAC6-Hsp90 chaperone machinery via Hsp90 acetylation and degradation.
    A452 chemosensitized cancer cells to the Hsp90 inhibitor 17-AAG.

    Physicochemical Properties

    M.Wt 338.407
    Formula C20H22N2O3
    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

    N-hydroxy-3-(1-(3-(naphthalen-2-yl)propyl)-2-oxo-2,5-dihydro-1H-pyrrol-3-yl)propanamide

    References

    1. Ryu HW, et al. Planta Med. 2015 Feb;81(3):222-7.

    2. Ryu HW, et al. Cancer Lett. 2017 Apr 10;391:162-171.

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