Formulation: A solid
Formal Name: N-(4-chloro-3-nitrophenyl)-N′-(4-fluorophenyl)-urea
Purity: ≥98%
Formula Markup: C13H9ClFN3O3
Formula Weight: 309,7
Shelf life (days): 1460
CAS Number: 897326-30-6
Notes: DTHIB is an inhibitor of heat shock factor 1 (Hsf1).{69510} It binds to the DNA-binding domain of Hsf1 (Kd = 160 nM) and inhibits heat-induced increases in the Hsf1 target proteins heat shock protein 27 (Hsp27) and Hsp70 levels in mouse embryonic fibroblasts (MEFs) when used at a concentration of 10 µM. It decreases nuclear but not cytoplasmic levels of Hsf1 in C4-2 prostate cancer cells, an effect that can be blocked by the proteasome inhibitor MG132. DTHIB decreases the viability of 22Rv1, C4-2, and PC3 prostate cancer cells (EC50 = 1.6, 1.2, and 3 µM, respectively) and induces cell cycle arrest at the G1 phase in C4-2 cells. In vivo, DTHIB (5 mg/kg) induces tumor regression in a TRAMP-C2 murine prostate cancer model.
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