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KUNG65

Chemical Structure : KUNG65

CAS No.: 2144469-30-5

KUNG65 (KUNG 65)

Catalog No.: PC-49775Not For Human Use, Lab Use Only.

KUNG65 is a potent, selective glucose regulated protein 94 (Grp94) inhibitor with Kd value of 540 nM in fluorescence polarization assays, 73-fold selectivity over Hsp90α.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    KUNG65 is a potent, selective glucose regulated protein 94 (Grp94) inhibitor with Kd value of 540 nM in fluorescence polarization assays, 73-fold selectivity over Hsp90α.
    Treatment with KUNG65 produced 38-40% migration (60% inhibition) at 500 nM after 24 h and exhibited good effects at lower concentrations in metastatic breast (MDA-MB-231) and prostate (PC3-MM2) cell lines.
    KUNG65 also reduced the migratory capabilities aginst metastatic melanoma (SK-MEL-28) cells.
    KUNG65 (2.5 uM) selectively targets Grp94 and induces the degradation of Grp94-specific client proteins without decreasing the levels of proteins that depend upon the cytosolic Hsp90 isoforms in in the metastatic cancer cell lines (MDA-MB-231, PC3-MM2, SK-MEL-28).

    Physicochemical Properties

    M.Wt 414.86
    Formula C23H20ClFO4
    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

    methyl 3-chloro-2-(2-(4-fluorobenzyl)phenethyl)-4,6-dihydroxybenzoate

    References

    1. Crowley VM, et al. Chemistry. 2017 Nov 7;23(62):15775-15782.

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