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AIMP2-DX2 inhibitor 1

Chemical Structure : AIMP2-DX2 inhibitor 1

CAS No.: 125105-17-1

AIMP2-DX2 inhibitor 1 (Compound 1)

Catalog No.: PC-72704Not For Human Use, Lab Use Only.

AIMP2-DX2 inhibitor 1 (Compound 1) is a specific chemical probe that can inhibit the tumor-promoting interaction between AIMP2-DX2 and HSP70 (IC50=2.9 uM).

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    Biological Activity

    AIMP2-DX2 inhibitor 1 (Compound 1) is a specific chemical probe that can inhibit the tumor-promoting interaction between AIMP2-DX2 and HSP70 (IC50=2.9 uM).
    Compound 1 showed no inhibition of PRKACA and PRKAR2A PPI at 100 uM.
    Compound 1 suppressed DX2-dependent cell proliferation in a DX2-inducible system.
    Compound 1 caused degradation of DX2 via inhibition of binding with HSP70.
    Compound 1 inhibited of proliferation cells with the highest levels of DX2, H460 and H358 with IC50 of 0.97 and 1.29 uM, respectively, with no effect on cells with lowest level of DX2.
    Compound 1 (5 and 10 mg/kg, i.p.) significantly reduced tumor size in a dose-dependent manner in vivo via a xenograft model using H460 cells, with little effect on body weight.

    Physicochemical Properties

    M.Wt 280.323
    Formula C18H16O3
    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

    ethyl (Z)-2-benzoyl-3-phenylacrylate

    References

    1. Dae Gyu Kim, et al. J Pharmacol Exp Ther. 2021 Dec;379(3):358-371.

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