DTHIB (Direct Targeted HSF1 InhiBitor) is a direct and selective inhibitor of heat shock factor 1 (HSF1) with Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB exhibits potently anticancer activities.
Direct Targeted HSF1 InhiBitor (DTHIB) physically engages HSF1 and selectively stimulates degradation of nuclear HSF1. DTHIB robustly inhibits the HSF1 cancer gene signature and prostate cancer cell proliferation.[1]
DTHIB potently attenuates tumor progression in four therapy-resistant prostate cancer animal models, including an NEPC model, where it causes profound tumor regression.[1]
[1] Bushu Dong, et al. Sci Transl Med. 2020 Dec 16;12(574):eabb5647.