DTHIB is a direct and selective heat shock factor 1 (HSF1) inhibitor with a Kd of 160 nM. DTHIB physically engages HSF1 and selectively stimulates degradation of nuclear HSF1. DTHIB robustly inhibited the HSF1 cancer gene signature and prostate cancer cell proliferation. In addition, it potently attenuated tumor progression in four therapy-resistant prostate cancer animal models, including an NEPC model, where it caused profound tumor regression.
CAS Number: 897326-30-6
Molecular Weight: 309.68
Chemical Name: 1-(4-chloro-3-nitrophenyl)-3-(4-fluorophenyl)urea
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO.
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
- 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[J]. Science Translational Medicine, 2020, 12(574):eabb5647.
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