2. Stem Cell/Wnt
  3. Wnt β-catenin
  4. QPH-FR

QPH-FR is a LGR5 inhibitor. QPH-FR competitively binds to LGR5 and prevents the formation of the LGR5/RSPO1 complex. QPH-FR promotes RNF43/ZNRF3-mediated ubiquitination of FZD receptors, inhibits the Wnt β-catenin signaling pathway, and reduces the stemness of colorectal cancer cells. QPH-FR is applicable to relevant research on colorectal cancer.

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Custom Peptide Synthesis

QPH-FR

QPH-FR Chemical Structure

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Based on 1 publication(s) in Google Scholar

QPH-FR Related Antibodies

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Description

QPH-FR is a LGR5 inhibitor. QPH-FR competitively binds to LGR5 and prevents the formation of the LGR5/RSPO1 complex. QPH-FR promotes RNF43/ZNRF3-mediated ubiquitination of FZD receptors, inhibits the Wnt β-catenin signaling pathway, and reduces the stemness of colorectal cancer cells. QPH-FR is applicable to relevant research on colorectal cancer[1].

In Vitro

QPH-FR binds to an overlapping site on LGR5 with RSPO1, with a binding energy of -7.0 kcal/mol, indicating potential competitive inhibition of LGR5/RSPO1 complex formation[1].
QPH-FR directly binds to endogenous LGR5 protein in HCT-8 and DLD1 human colorectal cancer cells[1].
QPH-FR (50 μg/mL; 24 h) enhances the chemosensitivity of HCT-8 and DLD1 human colorectal cancer cells to 5-FU, reducing the 5-FU IC50 to 11.27 μM and 15.30 μM, respectively[1].
QPH-FR (50 μg/mL; 24 h) inhibits tumor sphere formation, a marker of stemness, in HCT-8 and DLD1 human colorectal cancer cells by targeting LGR5, and blocks LiCl-induced Wnt pathway activation and sphere formation[1].
QPH-FR (20-60 μg/mL) disrupts the formation of the LGR5/RSPO1 complex in a dose-dependent manner in HCT-8 and DLD1 human colorectal cancer cells, with reduced RSPO1 binding to LGR5 at concentrations of 20, 40, and 60 μg/mL[1].
QPH-FR (50 μg/mL; 24 h) inhibits nuclear accumulation of β-catenin, a key mediator of Wnt signaling, in HCT-8 and DLD1 human colorectal cancer cells by targeting LGR5, and blocks LiCl-induced β-catenin nuclear translocation[1].
QPH-FR (50 μg/mL; 24 h) reduces the expression of stemness markers CD133, CD44, and ALDH1A1 at both the protein and mRNA levels in HCT-8 and DLD1 human colorectal cancer cells by targeting LGR5[1].

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

QPH-FR Related Antibodies

Cell Viability Assay[1]

Cell Line: Human colorectal cancer HCT-8 and DLD1 cells
Concentration: 50 μg/mL (co-incubated with 5-FU)
Incubation Time: 24 h (co-incubation with 5-FU)
Result: Reduced the IC50 of 5-FU in HCT-8 cells from 49.57 μM to 11.27 μM.
Reduced the IC50 of 5-FU in DLD1 cells from 47.62 μM to 15.30 μM, indicating enhanced chemosensitivity of cells to 5-FU.

Western Blot Analysis[1]

Cell Line: Human colorectal cancer HCT-8 and DLD1 cells
Concentration: 50 μg/mL; 10 mM LiCl (co-incubated with QPH-FR)
Incubation Time: 24 h (QPH-FR treatment; QPH-FR + LiCl co-treatment)
Result: Reduced nuclear β-catenin levels to near control levels when co-treated with LiCl, which alone increased total and nuclear β-catenin levels.
Lost inhibitory effect on nuclear β-catenin accumulation when LGR5 was knocked down.
Molecular Weight

1862.01

Formula

C81H124N26O25
Appearance

Solid

Color

White to off-white

Sequence

Phe-Lys-Glu-Asp-Val-Trp-Ser-Arg-Pro-Gly-Gly-Gly-Gly-Gly-Gly-Ile-Ser-Arg
Sequence Shortening

FKEDVWSRPGGGGGGISR
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (13.43 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 0.5371 mL 2.6853 mL 5.3705 mL
5 mM 0.1074 mL 0.5371 mL 1.0741 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (1.34 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (1.34 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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 (sealed storage, away from moisture). 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 0.5371 mL 2.6853 mL 5.3705 mL 13.4264 mL
5 mM 0.1074 mL 0.5371 mL 1.0741 mL 2.6853 mL
10 mM 0.0537 mL 0.2685 mL 0.5371 mL 1.3426 mL
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QPH-FR 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:

QPH-FRWntβ-cateninBeta cateninLGR5RNF43/ZNRF3DLD1RSPO1FZD receptorWnt β-catenin signaling pathwayHCT-8colorectal cancer cellsLGR5/RSPO1 complexInhibitorinhibitorinhibit

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