CAY10404

SKU: orb1219804

Description

CAY10404 is a potent and highly selective inhibitor of COX-2 and COX-1. It is also a potent inhibitor of PKB/Akt and MAPK signalling pathways and induces apoptosis in NSCLC cells, with analgesic, anti-inflammatory and anti-cancer activities.Treatment with CAY10404 in the range of 10-100 microM caused dose-dependent growth inhibition, with an average 50% inhibitory concentration (IC(50)) of 60-100 micromol/L, depending on the cell line. Western blot analysis of CAY10404-treated cells showed cleavage of poly (ADP-ribose) polymerase (PARP) and procaspase-3, signifying caspase activity and apoptotic cell death. CAY10404 treatment inhibited the phosphorylation of Akt, glycogen synthase kinase-3beta and extracellular signal-regulated kinases 1/2 in H460 and H358 cells.

Key Properties

• CAS Number: 340267-36-9
• MW: 367.34
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₂F₃NO₃S
• SMILES: CS(=O)(=O)c1ccc(cc1)-c1noc(c1-c1ccccc1)C(F)(F)F
• Target: COX
• Solubility: In Vitro: DMSO : 100 mg/mL (272.23 mM)

Bioactivity

• In Vivo:
  CAY10404 (50 mg/kg/day; ip; for 4 days) decreases lung inflammation in HTV mice and attenuates ventilator-induced lung injury. Animal model: Adult male C57Bl/6J mice weighing 24-30 g. Dosage: 50 mg/kg. Administration: IP; daily; for 4 days. Result: Attenuated cyclooxygenase activity, significantly decreasing BAL PGE2 and 6-keto PGF1α. Decreased lung inflammation in HTV mice (high tidal volume; 20 ml/kg; for 4 hours) and attenuates ventilator-induced lung injury.
• In Vitro:
  CAY10404 (compound 7) exhibits no inhibition of COX-1 (IC50>500 μM). CAY10404 (10-100 μM; for 3 days) inhibits the growth of NSCLC cell lines in a concentration-dependent manner and has an average 50% inhibitory concentration (IC50) of 60-100 μM. CAY10404 (20-100 μM; for 3 days) induces apoptosis in NSCLC cells. CAY10404 (80 μM; for 3 days) induces a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-XL) and pAkt and pGSK-3β. CAY10404 (20, 50, 80, 100 μM; for 14 days) compromises the ability of H460 cells to form colonies in anchorage-independent growth in a concentration-dependent manner. Cell Viability Assay Cell line: Non-small cell lung cancer (NSCLC) cells (H1703, H358, H460). Concentration: 10-100 μM. Incubation time: For 3 days. Result: Inhibited the growth of NSCLC cell lines in a concentration-dependent manner. Apoptosis Analysis Cell line: H460 cells. Concentration: 20, 50, 100 μM. Incubation time: For 3 days. Result: Induced apoptosis. Western blot analysis. Cell line: NSCLC cells (H358, H460). Concentration: 80 μM. Incubation time: For 3 days. Result: Induced a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-XL) and pAkt and pGSK-3β, without changing the level of the pro-apoptotic protein (Bax) and total Akt and GSK-3β protein levels.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T

Quick Database Links

Gene Symbol

COX