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BC-DXI-495

Chemical Structure : BC-DXI-495

CAS No.: 2421117-94-2

BC-DXI-495

Catalog No.: PC-73120Not For Human Use, Lab Use Only.

BC-DXI-495 is a specific small molecule inhibitor of AIMP2-DX2-HSP70 interaction, specifically reduced the levels of DX2 (IC50=4.2 uM) but not AIMP2-F, and the viability of lung cancer cells (EC50=14 uM).

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    Biological Activity

    BC-DXI-495 is a specific small molecule inhibitor of AIMP2-DX2-HSP70 interaction, specifically reduced the levels of DX2 (IC50=4.2 uM) but not AIMP2-F, and the viability of lung cancer cells (EC50=14 uM).
    BC-DXI-495 bound to DX2 with KD of 14 uM.
    BC-DXI-495 specifically reduced the levels of endogenous DX2 protein but not of AIMP2-F , affected the DX2 protein level, but not mRNA level.
    BC-DXI-495 inhibited DX2-dependent cell growth, significantly diminished tumor growth in a xenograft model of H460 cells, with little effect on body weigh.
    BC-DXI-495 significantly suppressed the growth and weight of tumors expressing DX2 WT, but not L80A mutant.

    Physicochemical Properties

    M.Wt 518.632
    Formula C28H30N4O4S
    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

    (S)-3-(1H-Indol-3-yl)-2-((4-methylphenyl)sulfonamido)-N-(4-morpholinophenyl)propanamide

    References

    1. Lim S, et al. Nat Chem Biol. 2020 Jan;16(1):31-41.

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