KRIBB11
An Hsf1 inhibitor (IC50 = 1.2 μM in a luciferase reporter assay); blocks heat shock-induced Hsp70, Hsp40, and Hsp27 mRNA expression and down-regulates protein expression of the Hsf1 target proteins Hsp70 and Hsp27 in HCT116 cells in a dose-dependent manner; specifically binds to Hsf1 over other Hsf1-associated proteins, lacking activity at Hsp90, Hsf2, and Cdk9 in an in vitro pull-down assay; inhibits growth of cancer cell lines (IC50s = 3-8 μM) via induction of cell cycle arrest at the G2/M phase and apoptosis; decreases tumor growth in a mouse HCT116 xenograft model; attenuates dengue virus progression and reduces mortality in infected mice
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Reference:
9002528-10
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