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

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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10 mM * 1 mL in DMSO
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10 mg USD 130 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

DTHIB Related Antibodies

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

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  • Purity & Documentation

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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].

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

DTHIB Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

Light yellow to yellow

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (322.91 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (6.72 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.08 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2291 mL 16.1457 mL 32.2914 mL 80.7285 mL
5 mM 0.6458 mL 3.2291 mL 6.4583 mL 16.1457 mL
10 mM 0.3229 mL 1.6146 mL 3.2291 mL 8.0728 mL
15 mM 0.2153 mL 1.0764 mL 2.1528 mL 5.3819 mL
20 mM 0.1615 mL 0.8073 mL 1.6146 mL 4.0364 mL
25 mM 0.1292 mL 0.6458 mL 1.2917 mL 3.2291 mL
30 mM 0.1076 mL 0.5382 mL 1.0764 mL 2.6909 mL
40 mM 0.0807 mL 0.4036 mL 0.8073 mL 2.0182 mL
50 mM 0.0646 mL 0.3229 mL 0.6458 mL 1.6146 mL
60 mM 0.0538 mL 0.2691 mL 0.5382 mL 1.3455 mL
80 mM 0.0404 mL 0.2018 mL 0.4036 mL 1.0091 mL
100 mM 0.0323 mL 0.1615 mL 0.3229 mL 0.8073 mL
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DTHIB Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DTHIB897326-30-6HSPHeat shock proteinsHSF1prostatecanceranticancernucleardegradationHSP27HSP70HSP90Inhibitorinhibitorinhibit

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