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Chemical Structure : KUNG65
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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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).
| M.Wt | 414.86 | |
| Formula | C23H20ClFO4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Crowley VM, et al. Chemistry. 2017 Nov 7;23(62):15775-15782.
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