Art. -Nr.: HY-B1786

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Sulindac sulfide

(Synonyms: cis-Sulindac sulfide)

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Sulindac sulfide is a noncompetitive γ-secretase inhibitor, with an IC₅₀ of 20.2 μM for γ₄₂-secretase activity.

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Reinheit: 98.10%
CAS. Nr.: 49627-27-2
Formel: C₂₀H₁₇FO₂S
Molecular Weight:340.41

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Sulindac sulfide Chemical Structure

CAS. Nr.: 49627-27-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Sulindac sulfide is a noncompetitive γ-secretase inhibitor, with an IC₅₀ of 20.2 μM for γ₄₂-secretase activity.

IC₅₀ & Target

IC50: 20.2 μM (γ₄₂-secretase)^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	34 μM Compound: 4	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	[PMID: 20503989]
COLO 320	IC₅₀	38.7 μM Compound: c	Cytotoxicity against human COLO320 cells after 72 hrs by WST-1 assay Cytotoxicity against human COLO320 cells after 72 hrs by WST-1 assay	[PMID: 20801552]
HEK293	IC₅₀	45200 nM Compound: Sulindac sulfide	Displacement of [3H]L685458 from human SPP expressed in HEK293 cells Displacement of [3H]L685458 from human SPP expressed in HEK293 cells	[PMID: 17932033]
HEK293	IC₅₀	215 μM Compound: 2	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	[PMID: 20650635]
HEK293	IC₅₀	53 μM Compound: 2	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	[PMID: 20650635]
HEK293	IC₅₀	82.5 μM Compound: 2	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	[PMID: 20650635]
MDA-MB-231	EC₅₀	209 μM Compound: 1b	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	[PMID: 22263894]
MDCK	IC₅₀	180 μM Compound: Sulindac Sulfide	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	[PMID: 11844707]
MDCK	IC₅₀	200 μM Compound: Sulindac Sulfide	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	[PMID: 11844707]
MIA PaCa-2	IC₅₀	146 μM Compound: c	Cytotoxicity against human MIAPaCa2 cells after 72 hrs by WST-1 assay Cytotoxicity against human MIAPaCa2 cells after 72 hrs by WST-1 assay	[PMID: 20801552]
NIH3T3	IC₅₀	350 μM Compound: Sulindac Sulfide	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	[PMID: 11844707]
REF	IC₅₀	200 μM Compound: Sulindac Sulfide	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)	[PMID: 11844707]
SW480	IC₅₀	200 μM Compound: Sulindac Sulfide	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	[PMID: 11844707]
THP-1	IC₅₀	57100 nM Compound: Sulindac sulfide	Displacement of [3H]L685458 from gamma-secretase in human THP1 cells Displacement of [3H]L685458 from gamma-secretase in human THP1 cells	[PMID: 17932033]
THP-1	IC₅₀	332 μM Compound: Sulindac sulfide	Displacement of [3H]IN973 from gamma-secretase in human THP1 cells Displacement of [3H]IN973 from gamma-secretase in human THP1 cells	[PMID: 17932033]

In Vitro

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

CAS. Nr. 49627-27-2
Appearance Solid
Molecular Weight 340.41
Formel C₂₀H₁₇FO₂S
Color Light yellow to yellow
SMILES

O=C(O)CC(C1=C/2C=CC(F)=C1)=C(C)C2=C\C3=CC=C(SC)C=C3
Synonyms

cis-Sulindac sulfide
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Journal Impact Factor

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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9376 mL

14.6882 mL

29.3763 mL

5 mM

0.5875 mL

2.9376 mL

5.8753 mL

10 mM

0.2938 mL

1.4688 mL

2.9376 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (7.34 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.

Protocol 2

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Takahashi Y, et al. Sulindac sulfide is a noncompetitive gamma-secretase inhibitor that preferentially reduces Abeta 42 generation. J Biol Chem. 2003 May 16;278(20):18664-70. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Sulindac sulfide

1 Cited Publications

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Sulindac sulfide

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Publications Citing Use of MedChemExpress (MCE) Sulindac sulfide

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Sulindac sulfide

Metabolism/Protease Compound Library

Neuronal Signaling Compound Library

Stem Cell Signaling Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Neurodegenerative Disease-related Compound Library

Drug Metabolite Library

Human Metabolite Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Mitochondrial Toxicity Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Sulindac sulfide

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Sulindac sulfide Related Classifications

Art. -Nr.: HY-B1786