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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Heat Shock Protein (HSP)-KUNG65
KUNG65

Chemical Structure : KUNG65

CAS No.: 2144469-30-5

KUNG65 (KUNG 65)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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).

    物理化学性质&存储条件

    分子量 414.86
    分子式 C23H20ClFO4
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

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

    参考文献

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

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