2. NF-κB Immunology/Inflammation
  3. NF-κB PD-1/PD-L1
  4. Sulindac

Sulindac (MK-231) is an orally active nonsteroidal anti-inflammatory agent. Sulindac also is an immunomodulatory agent. Sulindac can be used for the research of arthritis of the spine, gouty arthritis and kinds of cancer including colorectal cancer (CRC) and lung cancer.

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

Sulindac Chemical Structure

Sulindac Chemical Structure

CAS No. : 38194-50-2

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

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Sulindac Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Sulindac (MK-231) is an orally active nonsteroidal anti-inflammatory agent. Sulindac also is an immunomodulatory agent. Sulindac can be used for the research of arthritis of the spine, gouty arthritis and kinds of cancer including colorectal cancer (CRC) and lung cancer[1][2].

IC50 & Target[1]

COX-2

 

Autophagy

 

In Vitro

Sulindac (MK-231) (500 μM, 48 h) is effective in preventing TGF-β1-induced EMT, as indicated by upregulation of the epithelial marker, E-cadherin, and downregulation of mesenchymal markers and transcription factors[1].
Sulindac (500 μM, 48 h) can inhibit TGF-β1-enhanced migration and invasion of A549 cells[1].
Sulindac (500 μM, 48 h) enhances the reversal of TGF-β1-induced EMT by sulindac and SIRT1 upregulation promoted TGF-β1-induced EMT[1].

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

Sulindac Related Antibodies

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 500 μM
Incubation Time: 48 h
Result: Inhibit transforming growth factor (TGF)-β1-induced epithelial-mesenchymal transition in A549 cells.

Immunofluorescence[1]

Cell Line: A549 cells
Concentration: 500 μM
Incubation Time: 48 h
Result: Reversed SIRT-1 expression by TGF-β1 and inhibited the TGF-β1-induced cadherin switch.

Cell Migration Assay [1]

Cell Line: A549 cells
Concentration: 500 μM
Incubation Time: 48 h
Result: Inhibited migration, decreased resistance co-treatment with TGF-β1.

Cell Invasion Assay[1]

Cell Line: A549 cells
Concentration: 500 μM
Incubation Time: 40 h; 48 h
Result: Could effectively inhibit the TGF- β1-induced increase in invasion by lung cancer cells.
In Vivo

Sulindac (MK-231) (15 mg/kg, p.o., bid (sulindac alone); 7.5 mg/kg p.o., bid (sulindac combination with PD-L1)) shows a significant reduction in tumor volume and increases infiltration of CD8+ T lymphocytes in the tumor tissues when treated with combination therapy[2].
Sulindac (15 mg/kg, p.o., bid (sulindac alone); 7.5 mg/kg p.o., bid (sulindac combination with PD-L1)) can downregulate PD-L1 by blocking NF-κB signaling, which in turn led to a decrease in exosomal P[2].
Sulindac (15 mg/kg, p.o., bid (sulindac alone); 7.5 mg/kg p.o., bid (sulindac combination with PD-L1)) leads to increased availability of PD-L1 Ab by downregulating PD-L1 in combination therapy[2].
Sulindac (15 mg/kg, p.o., bid (sulindac alone); 7.5 mg/kg p.o., bid (sulindac combination with PD-L1)) has not a systemic inhibitory effect on prostaglandin E2 (PGE2) in low-dose[2].

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

Animal Model: CT26 syngeneic mouse tumor model[2]
Dosage: 15 mg/kg; 7.5 mg/kg
Administration: 15 mg/kg, p.o., bid (sulindac alone); 7.5 mg/kg p.o., bid (sulindac combination with PD-L1)
Result: Downregulated PD-L1 through the blockade of NF-κB signaling and modulate the response of pMMR CRC to anti-PD-L1 immunotherapy.
Cound effectively inhibit PD-L1 with no significant systematic toxicity.
Clinical Trial
Molecular Weight

356.41

Formula

C20H17FO3S
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(CC(C1=C2C=CC(F)=C1)=C(/C2=C/C3=CC=C(C=C3)S(C)=O)C)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 : 50 mg/mL (140.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8058 mL 14.0288 mL 28.0576 mL
5 mM 0.5612 mL 2.8058 mL 5.6115 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
=
Concentration
×
Volume
×
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 (7.01 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 (7.01 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).
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: 99.81%

COA (254 KB) LCMS (98 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 2.8058 mL 14.0288 mL 28.0576 mL 70.1439 mL
5 mM 0.5612 mL 2.8058 mL 5.6115 mL 14.0288 mL
10 mM 0.2806 mL 1.4029 mL 2.8058 mL 7.0144 mL
15 mM 0.1871 mL 0.9353 mL 1.8705 mL 4.6763 mL
20 mM 0.1403 mL 0.7014 mL 1.4029 mL 3.5072 mL
25 mM 0.1122 mL 0.5612 mL 1.1223 mL 2.8058 mL
30 mM 0.0935 mL 0.4676 mL 0.9353 mL 2.3381 mL
40 mM 0.0701 mL 0.3507 mL 0.7014 mL 1.7536 mL
50 mM 0.0561 mL 0.2806 mL 0.5612 mL 1.4029 mL
60 mM 0.0468 mL 0.2338 mL 0.4676 mL 1.1691 mL
80 mM 0.0351 mL 0.1754 mL 0.3507 mL 0.8768 mL
100 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.7014 mL
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Sulindac 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:

Sulindac38194-50-2MK-231MK231MK 231NF-κBPD-1/PD-L1Nuclear factor-κBNuclear factor-kappaBPD-1/Programmed death-ligand 1oralnonsteroidalanti-inflammatoryimmunomodulatory agentFDANSAIDcolorectal cancer (CRC)pMMRTGF-β1epithelial-mesenchymal transition (EMT)SIRT1lung cancermigrationinvasionInhibitorinhibitorinhibit

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