2. Others Immunology/Inflammation Stem Cell/Wnt Metabolic Enzyme/Protease MAPK/ERK Pathway Neuronal Signaling NF-κB
  3. Keap1-Nrf2 Reactive Oxygen Species Cholinesterase (ChE) MMP Insecticide ERK
  4. Propoxur

Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests.

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

Propoxur Chemical Structure

Propoxur Chemical Structure

CAS No. : 114-26-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
Solid
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Other Forms of Propoxur:

Propoxur Related Antibodies

Top Publications Citing Use of Products

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AChE BChE

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8

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ERK ERK1 ERK2 ERK5 ERK8

  • Biological Activity

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Description

Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests[1][2][3].

IC50 & Target

MMP-2

 

AChE

 

In Vitro

Propoxur (0.01-100 μM; 48 h) promotes cell migration and invasion in human breast cancer MCF-7 and MDA-MB-231 cells in a concentration-dependent manner, enhances MMP-2 protein expression, increases intracellular ROS levels, and activates ERK1/2 phosphorylation and Nrf2 nuclear translocation[1]. The intracellular regulatory activity of Propoxur could be reversed by PD98059 (HY-12028)[1].
Propoxur (10 μg/mL; 24 h) induces lipid peroxidation in hamster ovary CHO-K1 cells, significantly increases MDA production, decreases GSH content and GSH/GSSG ratio, and activates GR, GPx, and GST antioxidant enzyme activities. BSO pretreatment further aggravated oxidative damage[2].

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

Propoxur Related Antibodies

Cell Viability Assay[1]

Cell Line: Human breast cancer MCF-7 and MDA-MB-231 cells
Concentration: 0, 0.01, 1, 100 μM
Incubation Time: 48 h
Result: Unchanged cell viability across concentrations, and reduced migration/invasion.
Dose-dependent increases in migration and invasion in Wound healing and Transwell assays, with 110.8-406.0% higher invasion compared to control.

Western Blot Analysis[1]

Cell Line: Human breast cancer MCF-7 and MDA-MB-231 cells
Concentration: 0, 0.01, 1, 100 μM
Incubation Time: 48 h
Result: Increased MMP-2 protein expression without changes in MMP-9.
Dose-dependently increased phosphorylated ERK1/2 and nuclear Nrf2 levels, and the effects reversed by PD98059 (HY-12028), which suppressed MMP-2 overexpression.

Immunofluorescence[1]

Cell Line: MCF-7 & MDA-MB-231cells
Concentration: 0, 0.01, 1, 100 μM
Incubation Time: 48 h
Result: Resulted significant ROS accumulation in Flow cytometry and immunofluorescence.
In Vivo

Propoxur (8.51 mg/kg/day; oral; 30 days) induces oxidative stress in brain regions (cerebellum, cortex, hippocampus) in rats, manifestes by lipid peroxidation (increased MDA), protein carbonylation (increased PCC), decreases GSH levels and decreased activities of antioxidant enzymes (SOD, CAT, GSH-Px, GST), while inhibiting acetylcholinesterase (AChE) activity. Pretreatment with essential oil extracted from Nigella sativa significantly improves the above indicators[3].

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

Animal Model: Male Sprague-Dawley rats (250-300 g) with propoxur-induced neurotoxicity model[3]
Dosage: 8.51 mg/kg
Administration: Oral gavage, daily for 30 days
Result: Significantly decreased body weight and weights of cerebellum, cortex, and hippocampus by 24%, 24%, 44%, respectively. AChE activity was reduced by 50% in cerebellum, 39% in cortex, and 54% in hippocampus.
Significantly decreased activities of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-Px), and glutathione-S-transferase (GST).
Molecular Weight

209.24

Formula

C11H15NO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)OC1=CC=CC=C1OC(NC)=O
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 (477.92 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.7792 mL 23.8960 mL 47.7920 mL
5 mM 0.9558 mL 4.7792 mL 9.5584 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
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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: ≥ 2.08 mg/mL (9.94 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 (9.94 mM); Suspended solution

    This protocol yields a suspended solution of ≥ 2.08 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

    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

Purity: 99.43%

SDS (623 KB)

COA (251 KB) HNMR (163 KB) LCMS (88 KB)

Handling Instructions (2659 KB)
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 4.7792 mL 23.8960 mL 47.7920 mL 119.4800 mL
5 mM 0.9558 mL 4.7792 mL 9.5584 mL 23.8960 mL
10 mM 0.4779 mL 2.3896 mL 4.7792 mL 11.9480 mL
15 mM 0.3186 mL 1.5931 mL 3.1861 mL 7.9653 mL
20 mM 0.2390 mL 1.1948 mL 2.3896 mL 5.9740 mL
25 mM 0.1912 mL 0.9558 mL 1.9117 mL 4.7792 mL
30 mM 0.1593 mL 0.7965 mL 1.5931 mL 3.9827 mL
40 mM 0.1195 mL 0.5974 mL 1.1948 mL 2.9870 mL
50 mM 0.0956 mL 0.4779 mL 0.9558 mL 2.3896 mL
60 mM 0.0797 mL 0.3983 mL 0.7965 mL 1.9913 mL
80 mM 0.0597 mL 0.2987 mL 0.5974 mL 1.4935 mL
100 mM 0.0478 mL 0.2390 mL 0.4779 mL 1.1948 mL
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Propoxur 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:

Propoxur114-26-1Keap1-Nrf2Reactive Oxygen SpeciesCholinesterase (ChE)MMPInsecticideERKMatrix metalloproteinasesExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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