Description
An Hsf1 inhibitor; binds to the DNA-binding domain of Hsf1 (Kd = 160 nM); inhibits heat-induced increases in Hsp27 and Hsp70 levels in MEFs at 10 µM; decreases nuclear but not cytoplasmic levels of Hsf1 in C4-2 cells, an effect that can be blocked by MG132; decreases the viability of 22Rv1, C4-2, and PC3 cells (EC50 = 1.6, 1.2, and 3 µM, respectively) and induces cell cycle arrest at the G1 phase in C4-2 cells; induces tumor regression in a TRAMP-C2 murine prostate cancer model at 5 mg/kg