DTHIB

DTHIB is an inhibitor of heat shock factor 1 (Hsf1).¹ It binds to the DNA-binding domain of Hsf1 (K_d = 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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1. Dong, B., Jaeger, A.M., Hughes, P.F., et al. Targeting therapy-resistant prostate cancer via a direct inhibitor of the human heat shock transcription factor 1. Sci. Transl. Med. 12(574), eabb5647 (2020).