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SEW84

Chemical Structure : SEW84

CAS No.: 259089-67-3

SEW84 (SEW04784, SEW 04784, SEW 84)

Catalog No.: PC-38267Not For Human Use, Lab Use Only.

SEW84 (SEW04784) is a first-in-class, specific inhibitor of the Aha1-stimulated Hsp90 (ASH) ATPase activity (IC50=0.3 uM) without inhibiting basal Hsp90 ATPase.

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    Biological Activity

    SEW84 (SEW04784) is a first-in-class, specific inhibitor of the Aha1-stimulated Hsp90 (ASH) ATPase activity (IC50=0.3 uM) without inhibiting basal Hsp90 ATPase.
    SEW84 binds to the C-terminal domain of Aha1 (Kd=1.7 uM) to weaken its asymmetric binding to Hsp90.
    SEW84 inhibited the GR- and AR-dependent luciferase expression with IC50 of 1.3 uM and 0.7 uM respectively.
    SEW84 blocks Aha1-dependent Hsp90 chaperoning activities, including the in vitro and in vivo refolding of firefly luciferase, and the transcriptional activity of the androgen receptor in cell-based models of prostate cancer.
    SEW84 promotes the clearance of phosphorylated tau in cellular and tissue models of neurodegenerative tauopathy.

    Physicochemical Properties

    M.Wt 422.402
    Formula C19H14F4N4OS
    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

    2-(1-(4-fluorophenyl)-1H-pyrrole-2-carbonyl)-N-(3-(trifluoromethyl)phenyl)hydrazine-1-carbothioamide

    References

    1. Jay K Singh, et al. Cell Chem Biol. 2020 Mar 19;27(3):292-305.e6.

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