SEW84 is a potent and selective inhibitor of the Aha1-stimulated Hsp90 ATPase activity without inhibition of basal Hsp90 ATPase. It binds to the C-terminal domain of Aha1 and weakens the Hsp90-Aha1 interaction. SEW84 inhibits Aha1-dependent Hsp90 chaperoning activities including refolding of denatured firefly luciferase (in vitro) and in vivo transcriptional activity of the glucocorticoid receptor and AR androgen receptor in prostate cancer cell-based models. SEW84 preferentially clears Alzheimer disease related phosphorylated aggregation-prone Tau in primary rat cortical neurons.
potent and selective inhibitor of the Aha1-stimulated Hsp90 ATPase activity
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Cell chemical biology, 27(3), 292-305 (2020-02-06)
Hsp90 plays an important role in health and is a therapeutic target for managing misfolding disease. Compounds that disrupt co-chaperone delivery of clients to Hsp90 target a subset of Hsp90 activities, thereby minimizing the toxicity of pan-Hsp90 inhibitors. Here, we
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