| Identification | Back Directory | [Name]
Urea, N-(4-chloro-3-nitrophenyl)-N'-(4-fluorophenyl)- | [CAS]
897326-30-6 | [Synonyms]
DTHIB
1-(4-Chloro-3-nitrophenyl)-3-(4-fluorophenyl)urea
Urea, N-(4-chloro-3-nitrophenyl)-N'-(4-fluorophenyl)-
degradation,HSP27,Inhibitor,inhibit,HSP70,HSF1,HSP,DTHIB,HSP90,cancer,nuclear,anticancer,Heat shock proteins,prostate | [Molecular Formula]
C13H9ClFN3O3 | [MDL Number]
MFCD05080987 | [MOL File]
897326-30-6.mol | [Molecular Weight]
309.68 |
| Chemical Properties | Back Directory | [Boiling point ]
347.2±42.0 °C(Predicted) | [density ]
1.565±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (322.91 mM; Need ultrasonic) | [form ]
Solid | [pka]
12.61±0.70(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
DTHIB is a direct and selective heat shock factor 1 (HSF1) inhibitor with a Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB inhibits HSF1 cancer gene signature (HSF1 CaSig) and selectively stimulates degradation of nuclear HSF1. DTHIB has potently anticancer activities and can be used for prostate cancer research[1]. | [in vivo]
DTHIB (5 mg/kg; intraperitoneal injection; daily; for 3 weeks) treatment potently attenuates tumor progression in a C4-2 xenograft mouse model[1]. | Animal Model: | Nude mice (6 weeks of age) injected with C4-2 cells[1] | | Dosage: | 5 mg/kg | | Administration: | Intraperitoneal injection; daily; for 3 weeks | | Result: | Showed no visible tumor growth over a 3-week period and a 40% reduction in median tumor volume. |
| [References]
[1] Bushu Dong, et al. 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 |
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