1. Apoptosis
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  3. LCS3

LCS3 is a reversible and uncompetitive glutathione disulfide reductase (GSR) and thioredoxin reductase 1 (TXNRD1) inhibitor (IC50=3.3 µM and 3.8 µM, respectively). LCS3 shows anti-tumor activity, and induces apoptosis. LCS3 can be used in lung adenocarcinoma (LUAD) research.

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

LCS3 Chemical Structure

LCS3 Chemical Structure

CAS No. : 109844-92-0

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

LCS3 is a reversible and uncompetitive glutathione disulfide reductase (GSR) and thioredoxin reductase 1 (TXNRD1) inhibitor (IC50=3.3 µM and 3.8 µM, respectively). LCS3 shows anti-tumor activity, and induces apoptosis. LCS3 can be used in lung adenocarcinoma (LUAD) research[1].

Cellular Effect
Cell Line Type Value Description References
HCC1806 IC50
5.1 μM
Compound: 2c
Cytotoxicity against human HCC1806 cells assessed as reduction in cell viability incubated for 3 days by cell-titer-Glo reagent based assay
Cytotoxicity against human HCC1806 cells assessed as reduction in cell viability incubated for 3 days by cell-titer-Glo reagent based assay
[PMID: 26116180]
HeLa EC50
> 20 μM
Compound: 22i
Cytotoxicity against human HeLa cells after 65 hrs by Alamar blue assay
Cytotoxicity against human HeLa cells after 65 hrs by Alamar blue assay
[PMID: 23281892]
Vero CC50
1.5 μM
Compound: 7
Cytotoxicity against African green monkey Vero cells after 48 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells after 48 hrs by MTT assay
[PMID: 30600207]
In Vitro

LCS3 (5 nM-10 µM; 96 h) inhibits lung cancer cell lines, but not non-transformed lung cells[1].
LCS3 (3 µM; 3, 6, and 12 h) induces ROS and NRF2 pathway activation in sensitive lung adenocarcinoma (LUAD) cells[1].
LCS3 (3 µM; 96 h) selectively kills lung adenocarcinoma (LUAD) cell lines, in part through the induction of apoptosis[1].

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

Cell Viability Assay[1]

Cell Line: Non-small cell lung cancer (NSCLC) cells and non-transformed lung cells
Concentration: 5 nM-10 µM
Incubation Time: 96 hours
Result: Inhibited the growth of 24/25 NSCLC cell lines at low micromolar concentrations (IC50<5 µM), both of the non-transformed lung cell lines were relatively insensitive (IC50>10 µM).

Cell Viability Assay[1]

Cell Line: H23 and H1650 cells
Concentration: 3 µM
Incubation Time: 3, 6, and 12 hours
Result: Responded to LCS3 by accumulating ROS and activating the NRF2 transcription program.

Apoptosis Analysis[1]

Cell Line: lung adenocarcinoma (LUAD) cells
Concentration: 3 µM
Incubation Time: 96 hours
Result: Increased cleavage of caspase 3, caspase 7 and/or PARP1 in all LCS3-sensitive LUAD cell lines.

Western Blot Analysis[1]

Cell Line: H23 and H1650 cells
Concentration: 3 µM
Incubation Time: 24 hours
Result: Increased the protein levels of NRF2 and of the products of selected downstream targets of NRF2 in both cell lines.
Molecular Weight

266.64

Formula

C11H7ClN2O4

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=C([N+]([O-])=O)O1)NC2=CC=C(Cl)C=C2

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 : 125 mg/mL (468.80 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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7504 mL 18.7519 mL 37.5037 mL
5 mM 0.7501 mL 3.7504 mL 7.5007 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.

  • Molarity Calculator

  • 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)

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.5 mg/mL (9.38 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.
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 3.7504 mL 18.7519 mL 37.5037 mL 93.7594 mL
5 mM 0.7501 mL 3.7504 mL 7.5007 mL 18.7519 mL
10 mM 0.3750 mL 1.8752 mL 3.7504 mL 9.3759 mL
15 mM 0.2500 mL 1.2501 mL 2.5002 mL 6.2506 mL
20 mM 0.1875 mL 0.9376 mL 1.8752 mL 4.6880 mL
25 mM 0.1500 mL 0.7501 mL 1.5001 mL 3.7504 mL
30 mM 0.1250 mL 0.6251 mL 1.2501 mL 3.1253 mL
40 mM 0.0938 mL 0.4688 mL 0.9376 mL 2.3440 mL
50 mM 0.0750 mL 0.3750 mL 0.7501 mL 1.8752 mL
60 mM 0.0625 mL 0.3125 mL 0.6251 mL 1.5627 mL
80 mM 0.0469 mL 0.2344 mL 0.4688 mL 1.1720 mL
100 mM 0.0375 mL 0.1875 mL 0.3750 mL 0.9376 mL
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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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LCS3
Cat. No.:
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