Sulindac sulfide
Based on 1 publication(s) in Google Scholar
Sulindac sulfide is a noncompetitive γ-secretase inhibitor, with an IC50 of 20.2 μM for γ42-secretase activity.
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- Pureté: 98.10%
- CAS No.: 49627-27-2
- Formule: C20H17FO2S
- Masse moléculaire:340.41
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) Sulindac sulfide
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Activité biologique
IC50: 20.2 μM (γ42-secretase)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
34 μM
Compound: 4
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Modulation of gamma-secretase-mediated cleavage of human APP expressed in CHO cells with human presenilin-1 assessed as inhibition of amyloid beta42 production after 24 hrs by ELISA
Modulation of gamma-secretase-mediated cleavage of human APP expressed in CHO cells with human presenilin-1 assessed as inhibition of amyloid beta42 production after 24 hrs by ELISA
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[PMID: 20503989] |
| COLO 320 | IC50 |
38.7 μM
Compound: c
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Cytotoxicity against human COLO320 cells after 72 hrs by WST-1 assay
Cytotoxicity against human COLO320 cells after 72 hrs by WST-1 assay
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[PMID: 20801552] |
| HEK293 | IC50 |
45200 nM
Compound: Sulindac sulfide
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Displacement of [3H]L685458 from human SPP expressed in HEK293 cells
Displacement of [3H]L685458 from human SPP expressed in HEK293 cells
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[PMID: 17932033] |
| HEK293 | IC50 |
215 μM
Compound: 2
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Inhibition of gamma-secretase in HEK293 cells co-overexpressing APP Swedish mutant assessed as inhibition of amyloid beta 40 production by luciferase reporter gene assay
Inhibition of gamma-secretase in HEK293 cells co-overexpressing APP Swedish mutant assessed as inhibition of amyloid beta 40 production by luciferase reporter gene assay
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[PMID: 20650635] |
| HEK293 | IC50 |
53 μM
Compound: 2
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Inhibition of gamma-secretase in HEK293 cells co-overexpressing NotchdeltaE assessed as inhibition of notch cleavage by luciferase reporter gene assay
Inhibition of gamma-secretase in HEK293 cells co-overexpressing NotchdeltaE assessed as inhibition of notch cleavage by luciferase reporter gene assay
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[PMID: 20650635] |
| HEK293 | IC50 |
82.5 μM
Compound: 2
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Inhibition of gamma-secretase in HEK293 cells co-overexpressing APP Swedish mutant assessed as inhibition of amyloid beta 42 production by luciferase reporter gene assay
Inhibition of gamma-secretase in HEK293 cells co-overexpressing APP Swedish mutant assessed as inhibition of amyloid beta 42 production by luciferase reporter gene assay
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[PMID: 20650635] |
| MDA-MB-231 | EC50 |
209 μM
Compound: 1b
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Cytotoxicity against human MDA-MB-231 cells after 48 hrs by WST1 assay
Cytotoxicity against human MDA-MB-231 cells after 48 hrs by WST1 assay
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[PMID: 22263894] |
| MDCK | IC50 |
180 μM
Compound: Sulindac Sulfide
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Anti-proliferative activity was evaluated by its ability to inhibit proliferation of MDCK cells
Anti-proliferative activity was evaluated by its ability to inhibit proliferation of MDCK cells
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[PMID: 11844707] |
| MDCK | IC50 |
200 μM
Compound: Sulindac Sulfide
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Anti-proliferative activity was evaluated by its ability to inhibit proliferation of MDCK-f3 (Madin-Darby canine kidney f3) cell line
Anti-proliferative activity was evaluated by its ability to inhibit proliferation of MDCK-f3 (Madin-Darby canine kidney f3) cell line
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[PMID: 11844707] |
| MIA PaCa-2 | IC50 |
146 μM
Compound: c
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Cytotoxicity against human MIAPaCa2 cells after 72 hrs by WST-1 assay
Cytotoxicity against human MIAPaCa2 cells after 72 hrs by WST-1 assay
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[PMID: 20801552] |
| NIH3T3 | IC50 |
350 μM
Compound: Sulindac Sulfide
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Anti-proliferative activity was evaluated by its ability to inhibit proliferation of murine NIH3T3 fibroblasts
Anti-proliferative activity was evaluated by its ability to inhibit proliferation of murine NIH3T3 fibroblasts
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[PMID: 11844707] |
| REF | IC50 |
200 μM
Compound: Sulindac Sulfide
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Anti-proliferative activity was evaluated by its ability to inhibit proliferation of rat embryonic fibroblasts (REF)
Anti-proliferative activity was evaluated by its ability to inhibit proliferation of rat embryonic fibroblasts (REF)
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[PMID: 11844707] |
| SW480 | IC50 |
200 μM
Compound: Sulindac Sulfide
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Anti-proliferative activity was evaluated by its ability to inhibit proliferation of SW480 cells
Anti-proliferative activity was evaluated by its ability to inhibit proliferation of SW480 cells
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[PMID: 11844707] |
| THP-1 | IC50 |
57100 nM
Compound: Sulindac sulfide
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Displacement of [3H]L685458 from gamma-secretase in human THP1 cells
Displacement of [3H]L685458 from gamma-secretase in human THP1 cells
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[PMID: 17932033] |
| THP-1 | IC50 |
332 μM
Compound: Sulindac sulfide
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Displacement of [3H]IN973 from gamma-secretase in human THP1 cells
Displacement of [3H]IN973 from gamma-secretase in human THP1 cells
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[PMID: 17932033] |
Treatment with 100 μM of Sulindac sulfide (SSide) causes cell death presumably by inducing apoptosis, resulting in marked decrease in Aβgeneration as well as in total protein expression. The IC50 value for Aβ42 secretion of Sulindac sulfide is 30.6±2.8 μM. SSone and naproxen have no effect either on Aβ40 or Aβ42 secretion as well as on Notch cleavage up to 100 μM. It is observed that an inhibition of γ42-secretase activity by Sulindac sulfide in a dose-dependent manner. The IC50 value of SSide for inhibiting γ42-secretase activity in vitro is 20.2±2.6 μM. A decrease is found in slope by the increase of the concentration of SSide in the plot of rate against the enzyme concentration, suggesting that Sulindac sulfide is not an irreversible or pseudo-irreversible inhibitor. Moreover, when the dialyzed solubilizedγ-secretase fraction is pretreated with Sulindac sulfide against CHAPSO buffer without Sulindac sulfide, γ-secretase activity is almost totally recovered. From these data, it is strongly suggested that the genuine molecular target of Sulindac sulfide is the γ-secretase complex and that Sulindac sulfide works as a reversible γ-secretase inhibitor[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 49627-27-2
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Appearance Solid
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Masse moléculaire 340.41
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Formule C20H17FO2S
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Color Light yellow to yellow
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SMILES
O=C(O)CC(C1=C/2C=CC(F)=C1)=C(C)C2=C\C3=CC=C(SC)C=C3
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Synonyms
cis-Sulindac sulfide
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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J Cancer Res Clin Oncol
Sulindac exhibits anti-proliferative and anti-invasive effects in uterine serous carcinoma cells. [Abstract]2024 Aug 28;150(8):402. PMID: 39198302
Solvant et solubilité
DMSO : 50 mg/mL (146.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.34 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.34 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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 2.9376 mL | 14.6882 mL | 29.3763 mL | 73.4408 mL |
| 5 mM | 0.5875 mL | 2.9376 mL | 5.8753 mL | 14.6882 mL | |
| 10 mM | 0.2938 mL | 1.4688 mL | 2.9376 mL | 7.3441 mL | |
| 15 mM | 0.1958 mL | 0.9792 mL | 1.9584 mL | 4.8961 mL | |
| 20 mM | 0.1469 mL | 0.7344 mL | 1.4688 mL | 3.6720 mL | |
| 25 mM | 0.1175 mL | 0.5875 mL | 1.1751 mL | 2.9376 mL | |
| 30 mM | 0.0979 mL | 0.4896 mL | 0.9792 mL | 2.4480 mL | |
| 40 mM | 0.0734 mL | 0.3672 mL | 0.7344 mL | 1.8360 mL | |
| 50 mM | 0.0588 mL | 0.2938 mL | 0.5875 mL | 1.4688 mL | |
| 60 mM | 0.0490 mL | 0.2448 mL | 0.4896 mL | 1.2240 mL | |
| 80 mM | 0.0367 mL | 0.1836 mL | 0.3672 mL | 0.9180 mL | |
| 100 mM | 0.0294 mL | 0.1469 mL | 0.2938 mL | 0.7344 mL |
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