2. Vitamin D Related/Nuclear Receptor Apoptosis
  3. Orphan Nuclear Receptor Apoptosis
  4. DHQZ-17

DHQZ-17 is a HNF4A inhibitor. DHQZ-17 triggers apoptosis in head and neck squamous cell carcinoma cells. DHQZ-17 can be used for the research of head & neck squamous cell carcinoma.

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

DHQZ-17

DHQZ-17 Chemical Structure

CAS No. : 2408759-14-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

DHQZ-17 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

DHQZ-17 is a HNF4A inhibitor. DHQZ-17 triggers apoptosis in head and neck squamous cell carcinoma cells. DHQZ-17 can be used for the research of head & neck squamous cell carcinoma[1].

In Vitro

DHQZ-17 (Compound 17) (0.5-50 μM; 24-72 h) potently inhibits the viability of SCC131 oral squamous cell carcinoma cells with an IC50 of 1.75 μM at 72 h, shows lower potency against other cancer cell lines, and is non-toxic to normal human cells and PBMCs at tested concentrations[1].
DHQZ-17 (10 μM; 2 h) does not induce micronuclei formation in human PBMCs, showing no genotoxic effect[1].
DHQZ-17 (2.5-10 μM; 24 h-4 days) alters the morphology of SCC131 cells and reduces viable cell numbers in a concentration-dependent manner over 4 days[1].
DHQZ-17 (2.5-10 μM; 24 h) induces G2/M phase cell cycle arrest and increases Sub G0 phase cell population in SCC131 cells, accompanied by elevated Cyclin B1 levels[1].
DHQZ-17 (2.5-10 μM; 24 h) induces concentration-dependent apoptosis in SCC131 cells via increased ROS generation, DNA damage, and modulation of pro- and anti-apoptotic proteins[1].
DHQZ-17 (2.5-10 μM; 24-48 h) inhibits the tumorigenic potential of SCC131 cells by reducing colony formation and impairing wound healing in a concentration-dependent manner[1].
DHQZ-17 (2.5-5 μM; 24 h) downregulates HNF4A expression in SCC131 cells, and overexpression of HNF4A partially rescues DHQZ-17-induced cytotoxicity and colony inhibition, identifying HNF4A as a target[1].

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

DHQZ-17 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: human peripheral blood mononuclear cells (PBMCs)
Concentration: 0.5 μM; 1 μM; 1.5 μM; 2 μM; 2.5 μM; 3 μM; 3.5 μM; 4 μM; 4.5 μM; 5 μM
Incubation Time: 72 h
Result: Caused no significant cell death in PBMCs treated with up to 5 μM for 72 h.

Cell Proliferation Assay[1]

Cell Line: SCC131 oral squamous cell carcinoma cells
Concentration: 2.5 μM; 5 μM; 10 μM
Incubation Time: 24 h; 4 days
Result: Caused drastic concentration-dependent morphological changes in SCC131 cells compared to DMSO-treated controls.
Reduced viable cell numbers significantly to 430.28×103 cells (5 μM) and 560.75×103 cells (10 μM) by day 4, relative to DMSO-treated cells.

Cell Cycle Analysis[1]

Cell Line: SCC131 oral squamous cell carcinoma cells
Concentration: 2.5 μM; 5 μM; 10 μM
Incubation Time: 24 h
Result: Caused 24.285% of SCC131 cells to arrest at G2/M phase, with 7.55% of cells in Sub G0 phase at 5 μM.
Caused 26.67% of SCC131 cells to arrest at G2/M phase, with 9.54% of cells in Sub G0 phase at 10 μM.
Increased Cyclin B1 protein levels with increasing concentration.

Apoptosis Analysis[1]

Cell Line: SCC131 oral squamous cell carcinoma cells
Concentration: 2.5 μM; 5 μM; 10 μM
Incubation Time: 24 h
Result: Reduced early apoptotic cells to 1.2% and increased late apoptotic cells to 57.83% at 10 μM (compared to 23.07% early and 3.57% late apoptotic cells in DMSO controls).
Induced concentration-dependent DNA fragmentation, nuclear condensation (349 condensed nuclei at 10 μM vs. 6.5 in DMSO), and ROS generation.
Increased levels of cleaved PARP, cleaved caspase-3, caspase-9, and BAX, and decreased levels of BCL2 with increasing concentration.

Real Time qPCR[1]

Cell Line: SCC131 oral squamous cell carcinoma cells
Concentration: 2.5 μM; 5 μM; 10 μM
Incubation Time: 24 h
Result: Downregulated HNF4A expression by 3.36-fold in SCC131 cells at 5 μM.
Reduced the cytotoxic and colony-inhibiting effects of the compound in HNF4A-Flag-transfected cells compared to untransfected cells.
In Vivo

DHQZ-17 (Compound 17) (10.287-41.148 mg/kg; i.p.; single dose) exhibits minimal acute in vivo toxicity in BALB/c mice at doses up to 20.574 mg/kg, with only moderate body weight reduction at the highest tested dose of 41.148 mg/kg[1].
DHQZ-17 (41.148 mg/kg; i.p.; single dose) reduces head and neck squamous cell carcinoma xenograft tumor volume by 22.39% in athymic mice, with no observed organ toxicity[1].

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

Animal Model: BALB/c (female, 4-6 weeks old)[1]
Dosage: 10.287 mg/kg; 20.574 mg/kg; 41.148 mg/kg
Administration: i.p.; single dose
Result: Showed no significant reduction in body weight compared to DMSO-treated controls (10.287 mg/kg and 20.574 mg/kg groups).
Showed a 23% reduction in body weight by day 10, after which body weight stabilized (41.148 mg/kg group).
Observed no changes in solid and liquid feeding behavior across all groups.
Animal Model: nu/nu athymic (female, 4-6 weeks old)[1]
Dosage: 41.148 mg/kg
Administration: i.p.; single dose
Result: Reduced tumor volume by 22.39% compared to DMSO-treated controls on day 7 post-treatment.
Showed no significant change in body weight.
Noted no visual necrosis or organ toxicity upon sacrifice.
Molecular Weight

358.31

Formula

C19H13F3N2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N[C@@H](C2=CC=C(C=CC=C3)C3=C2)NC4=C1C=C(OC(F)(F)F)C=C4
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 (279.09 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 2.7909 mL 13.9544 mL 27.9088 mL
5 mM 0.5582 mL 2.7909 mL 5.5818 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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

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

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (13.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (13.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7909 mL 13.9544 mL 27.9088 mL 69.7720 mL
5 mM 0.5582 mL 2.7909 mL 5.5818 mL 13.9544 mL
10 mM 0.2791 mL 1.3954 mL 2.7909 mL 6.9772 mL
15 mM 0.1861 mL 0.9303 mL 1.8606 mL 4.6515 mL
20 mM 0.1395 mL 0.6977 mL 1.3954 mL 3.4886 mL
25 mM 0.1116 mL 0.5582 mL 1.1164 mL 2.7909 mL
30 mM 0.0930 mL 0.4651 mL 0.9303 mL 2.3257 mL
40 mM 0.0698 mL 0.3489 mL 0.6977 mL 1.7443 mL
50 mM 0.0558 mL 0.2791 mL 0.5582 mL 1.3954 mL
60 mM 0.0465 mL 0.2326 mL 0.4651 mL 1.1629 mL
80 mM 0.0349 mL 0.1744 mL 0.3489 mL 0.8721 mL
100 mM 0.0279 mL 0.1395 mL 0.2791 mL 0.6977 mL
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DHQZ-17 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:

DHQZ-172408759-14-6DHQZ17DHQZ 17Orphan Nuclear ReceptorApoptosisapoptosisPBMCsnormal human cellsSCC131 oral squamous cell carcinoma cellshead and neck squamous cell carcinoma xenograftsHNF4Ahead and neck squamous cell carcinoma cellsG2/M phase cell cycle arrestathymic miceCyclin B1Inhibitorinhibitorinhibit

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