For research use only. Not for therapeutic Use.
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.
| Catalog Number | I026578 |
| CAS Number | 897326-30-6 |
| Synonyms | DTHIB |
| Molecular Formula | C13H9ClFN3O3 |
| Purity | 98% |
| Target | Metabolic Enzyme/Protease |
| Solubility | Soluble in DMSO |
| Appearance | Solid powder |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| IUPAC Name | 1-(4-chloro-3-nitrophenyl)-3-(4-fluorophenyl)urea |
| InChI | 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) |
| InChIKey | DWVIOMKFHSRQQM-UHFFFAOYSA-N |
| SMILES | O=C(NC1=CC=C(F)C=C1)NC2=CC=C(Cl)C([N+]([O-])=O)=C2 |
| Reference | Dong B, Jaeger AM, Hughes PF, Loiselle DR, Hauck JS, Fu Y, Haystead TA, Huang J, Thiele DJ. Targeting therapy-resistant prostate cancer via a direct inhibitor of the human heat shock transcription factor 1. Sci Transl Med. 2020 Dec 16;12(574):eabb5647. doi: 10.1126/scitranslmed.abb5647. PMID: 33328331. |
