Sulindac sulfide

SKU: orb1708446

Description

Sulindac sulfide, the active metabolite of sulindac, is a potent COX-1 inhibitor and non-competitive gamma-secretase inhibitor (IC50 = 20.2 µM). It is widely used in research on inflammation, cancer (notably colorectal), and Alzheimer's disease, employing both in vitro and in vivo models to study Ras/Raf signaling and amyloid precursor protein processing.

Research Area

Metabolism Research, Neuroscience, Protein Biochemistry, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 49627-27-2
• MW: 340.41
• Purity: 99.68%
• Formula: C₂₀H₁₇FO₂S
• SMILES: C(=C/1\C=2C(C(CC(O)=O)=C1C)=CC(F)=CC2)\C3=CC=C(SC)C=C3
• Target: Gamma-secretase,AChR,Drug Metabolite,Raf
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.88 mM);DMSO:45 mg/mL (132.19 mM)

Bioactivity

• Target IC50:
  γ42-secretase:20.2 μM |γ42-secretase:20.2 μM|COX-2:1.21 µM|Aldose reductase:279 nM|COX-1:1.9 µM
• In Vivo:
  Sulindac sulfide also inhibits aldose reductase, blocking NADPH-dependent reduction of glucose to sorbitol, and reducing type 2 diabetic complications. Sulindac sulfide inhibits colorectal cancer growth both in vitro and in vivo.
• In Vitro:
  Treatment with 100 μM of Sulindac sulfide (SSide) induces apoptosis leading to significant reduction in Aβ generation and total protein expression. The IC50 for Aβ42 secretion of SSide is 30.6±2.8 μM. SSide inhibits γ42-secretase activity dose-dependently, with an IC50 of 20.2±2.6 μM. Increasing SSide concentration decreases the slope in the rate vs. enzyme concentration plot, indicating SSide is not an irreversible or pseudo-irreversible inhibitor. After pretreatment of the dialyzed solubilized γ-secretase fraction with SSide and subsequent exposure to CHAPSO buffer without SSide, γ-secretase activity almost fully recovers. This strongly suggests that SSide targets the γ-secretase complex as a reversible inhibitor.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

γ42-secretase, Raf-1, mAChR, cis-Sulindac sulfide

Compound Identifiers

PubChem CID

5352624