1. Cytoskeleton
  2. Arp2/3 Complex
  3. Benproperine phosphate

Benproperine phosphate is an orally active, potent actin-related protein 2/3 complex subunit 2 (ARPC2) inhibitor. Benproperine phosphate attenuates the actin polymerization rate of action polymerization nucleation by impairing Arp2/3 function. Benproperine phosphate has the potential for a cough suppressant and suppresses cancer cell migration and tumor metastasis.

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Benproperine phosphate Chemical Structure

Benproperine phosphate Chemical Structure

CAS No. : 19428-14-9

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of Benproperine phosphate:

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  • Biological Activity

  • Purity & Documentation

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Description

Benproperine phosphate is an orally active, potent actin-related protein 2/3 complex subunit 2 (ARPC2) inhibitor. Benproperine phosphate attenuates the actin polymerization rate of action polymerization nucleation by impairing Arp2/3 function. Benproperine phosphate has the potential for a cough suppressant and suppresses cancer cell migration and tumor metastasis[1].

In Vitro

Benproperine phosphate (20-120 μM; for 24 hours) inhibits cell viability in a dose-dependent manner[1].
Benproperine phosphate (10 μM; for 24 hours) significantly inhibits the migration of various types of cancer cells and inhibits the migration and invasion of DLD-1, AsPC-1 cells with IC50 values of 1-2 μM. Benproperine phosphate (10 μM; for 24 hours) does not affect cortactin-rich lamellipodium in MCF-10A cells[1].

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

Cell Viability Assay[1]

Cell Line: DLD-1, AsPC-1, CFPAC-1, A375P, A375P, MDA-MB-231, DU145, DU145 cancer cells
Concentration: 20, 40, 60, 80, 100, 120 μM
Incubation Time: For 24 hours
Result: Inhibited cell viability in a dose-dependent manner.
In Vivo

Benproperine phosphate (50, 100 mg/kg; oral gavage; 5 days per week for 4 weeks) inhibits primary pancreatic tumor growth[1].
Benproperine phosphate shows a marked decrease in the lung metastasis of AsPC-1 cells (56.1% inhibition) in mouse. Benproperine phosphate significantly suppressed the liver metastasis of HCT-116 cells by 78.9% and DLD-1 cells by 78.2%[1].

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

Animal Model: Female BALB/c nude mice of 6-week-old with AsPC-1 cells[1]
Dosage: 50, 100 mg/kg
Administration: Oral gavage; 5 days per week for 4 weeks
Result: Inhibited primary pancreatic tumor growth compared to the vehicle control (47.7% inhibition) without body weights change.
Molecular Weight

407.44

Formula

C21H30NO5P

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(N1CCCCC1)COC2=CC=CC=C2CC3=CC=CC=C3.O=P(O)(O)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (306.79 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 100 mg/mL (245.43 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4543 mL 12.2717 mL 24.5435 mL
5 mM 0.4909 mL 2.4543 mL 4.9087 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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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

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Volume (start)

V1

=
Concentration (final)

C2

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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: ≥ 2.08 mg/mL (5.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.35%

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 (sealed storage, away from moisture). 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
H2O / DMSO 1 mM 2.4543 mL 12.2717 mL 24.5435 mL 61.3587 mL
5 mM 0.4909 mL 2.4543 mL 4.9087 mL 12.2717 mL
10 mM 0.2454 mL 1.2272 mL 2.4543 mL 6.1359 mL
15 mM 0.1636 mL 0.8181 mL 1.6362 mL 4.0906 mL
20 mM 0.1227 mL 0.6136 mL 1.2272 mL 3.0679 mL
25 mM 0.0982 mL 0.4909 mL 0.9817 mL 2.4543 mL
30 mM 0.0818 mL 0.4091 mL 0.8181 mL 2.0453 mL
40 mM 0.0614 mL 0.3068 mL 0.6136 mL 1.5340 mL
50 mM 0.0491 mL 0.2454 mL 0.4909 mL 1.2272 mL
60 mM 0.0409 mL 0.2045 mL 0.4091 mL 1.0226 mL
80 mM 0.0307 mL 0.1534 mL 0.3068 mL 0.7670 mL
100 mM 0.0245 mL 0.1227 mL 0.2454 mL 0.6136 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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.

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Benproperine phosphate
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