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Sulindac sulfide

Catalog No. T13037   CAS 49627-27-2
Synonyms: cis-Sulindac sulfide

Sulindac sulfide (cis-Sulindac sulfide) is a non-steroidal anti-inflammatory compound that has a high affinity for COX-1 and acts as an inhibitor in Ras activation of Raf-1. Sulindac sulfide is a non-competitive inhibitor of gamma-secretase with an IC50 value of 20.2 μM. It is an active metabolite of sulinic acid.

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Sulindac sulfide Chemical Structure
Sulindac sulfide, CAS 49627-27-2
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10 mg In stock $ 31.00
25 mg In stock $ 48.00
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1 mL * 10 mM (in DMSO) In stock $ 79.00
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Purity: 99.68%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Sulindac sulfide (cis-Sulindac sulfide) is a non-steroidal anti-inflammatory compound that has a high affinity for COX-1 and acts as an inhibitor in Ras activation of Raf-1. Sulindac sulfide is a non-competitive inhibitor of gamma-secretase with an IC50 value of 20.2 μM. It is an active metabolite of sulinic acid.
Targets&IC50 γ42-secretase:20.2 μM , γ42-secretase:20.2 μM, COX-1:1.9 µM, COX-2:1.21 µM, Aldose reductase:279 nM
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. 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]
In vivo Sulindac sulfide also inhibits aldose reductase, blocking NADPH-dependent reduction of glucose to sorbitol, and reducing type 2 diabetic complications.[2]
Sulindac sulfide inhibits colorectal cancer growth both in vitro and in vivo.[5]
Synonyms cis-Sulindac sulfide
Molecular Weight 340.41
Formula C20H17FO2S
CAS No. 49627-27-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45.0 mg/mL (132.2 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Takahashi Y, et al. Sulindac sulfide is a noncompetitive gamma-secretase inhibitor that preferentially reduces Abeta 42 generation. J Biol Chem. 2003;278(20):18664-18670. 2. Zheng X, et al. The molecular basis for inhibition of sulindac and its metabolites towards human aldose reductase. FEBS Lett. 2012;586(1):55-59. 3. Warner TD, et al. Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: a full in vitro analysis. Proc Natl Acad Sci U S A. 1999;96(13):7563-7568. 4. Boolbol SK, et al. Cyclooxygenase-2 overexpression and tumor formation are blocked by sulindac in a murine model of familial adenomatous polyposis. Cancer Res. 1996;56(11):2556-2560. 5. Williams CS, et al. Sulindac sulfide, but not sulindac sulfone, inhibits colorectal cancer growth. Neoplasia. 1999;1(2):170-176.

Related compound libraries

This product is contained In the following compound libraries:
Membrane Protein-targeted Compound Library Inhibitor Library Kinase Inhibitor Library Bioactive Compounds Library Max Neurotransmitter Receptor Compound Library Neuronal Signaling Compound Library Anti-Obesity Compound Library Bioactive Compound Library

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Keywords

Sulindac sulfide 49627-27-2 MAPK Neuroscience Others AChR Raf cis-Sulindac sulfide cis-Sulindac Sulfide Sulindac Sulfide inhibitor inhibit

 

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