1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
  2. HSP
  3. DTHIB

DTHIB 

Cat. No.: HY-138280 Purity: 98.34%
Handling Instructions

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.

For research use only. We do not sell to patients.

DTHIB Chemical Structure

DTHIB Chemical Structure

CAS No. : 897326-30-6

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Based on 1 publication(s) in Google Scholar

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Description

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].

IC50 & Target

Kd: 160 nM (DTHIB binding to the HSF1 DNA binding domain)[1]

In Vitro

DTHIB (5 μM; 48 hours) treatment of C4-2 cells induces cell cycle arrest, with accumulation in the G1 phase. DTHIB stimulates C4-2 PCa cell entry into senescence[1].
DTHIB (0.5-5 μM; 48 hours; C4-2 prostate cancer) treatment reduces steady-state protein abundance of the molecular chaperones P23, HSP27, HSP70, and HSP90-all bona fide HSF1 targets in C4-2 cells[1].
DTHIB dose-dependently reduces the clonal expansion of both C4-2 and PC-3 PCa cells with EC50 values of 1.2 μM and 3.0 μM, respectively[1].
In mouse embryonic fibroblasts (MEFs), DTHIB (0.5-10 μM) attenuates the robust acute heat shock induction of the HSP70 and HSP25 molecular chaperones in a dose-dependent manner. DTHIB attenuates the heat shock response by reducing the steady-state transcript abundance of multiple molecular chaperones[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: C4-2 cells
Concentration: 5 μM
Incubation Time: 48 hours
Result: Induced cell cycle arrest.

Western Blot Analysis[1]

Cell Line: C4-2 prostate cancer (PCa) cells
Concentration: 0.5 μM, 1 μM, 2.5 μM, 5 μM
Incubation Time: 48 hours
Result: Dose-dependently inhibited expression of molecular chaperones in C4-2 PCa cells.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

309.68

Formula

C₁₃H₉ClFN₃O₃

CAS No.

897326-30-6

SMILES

O=C(NC1=CC=C(F)C=C1)NC2=CC=C(Cl)C([N+]([O-])=O)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (322.91 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2291 mL 16.1457 mL 32.2914 mL
5 mM 0.6458 mL 3.2291 mL 6.4583 mL
10 mM 0.3229 mL 1.6146 mL 3.2291 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

DTHIBHSPHeat shock proteinsHSF1prostatecanceranticancernucleardegradationHSP27HSP70HSP90Inhibitorinhibitorinhibit

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DTHIB
Cat. No.:
HY-138280
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