DTHIB

DTHIB is an inhibitor of heat shock factor 1 (Hsf1). 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.Formal Name: N-(4-chloro-3-nitrophenyl)-N'-(4-fluorophenyl)-urea. CAS Number: 897326-30-6. Synonyms: Direct Targeted Heat Shock Factor 1 Inhibitor, Direct Targeted Hsf1 Inhibitor. Molecular Formula: C13H9ClFN3O3. Formula Weight: 309.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble, Methanol: Soluble. lambdamax: 256 nm. SMILES: O=C(NC1=CC=C(C([N+]([O-])=O)=C1)Cl)NC2=CC=C(C=C2)F. InChi Code: InChI=1S/C13H9ClFN3O3/c14-11-6-5-10(7-12(11)18(20)21)17-13(19)16-9-3-1-8(15)2-4-9/h1-7H,(H2,16,17,19). InChi Key: DWVIOMKFHSRQQM-UHFFFAOYSA-N.