Licofelone

SKU: orb1300651

Description

Licofelone

Research Area

Cell Biology, Immunology & Inflammation, Metabolism Research, Neuroscience

Key Properties

• CAS Number: 156897-06-2
• MW: 379.88
• Purity: 99.25%
• Formula: C₂₃H₂₂ClNO₂
• SMILES: CC1(C)Cc2c(c(c(CC(O)=O)n2C1)-c1ccc(Cl)cc1)-c1ccccc1
• Target: Lipoxygenase,Apoptosis,COX
• Solubility: Ethanol:10 mg/mL (26.32 mM);DMSO:25 mg/mL (65.81 mM);H2O:< 1 mg/mL (insoluble or slightly soluble) (< 1 mM);10% DMSO+90% Corn Oil:2 mg/mL (5.26 mM)

Bioactivity

• Target IC50:
  5-LOX:0.18 μM|COX:0.21 μM
• In Vitro:
  The dual COX/5-LOX inhibitor licofelone triggers apoptosis in a dose- and time-dependent manner in HCA-7 colon cancer cells. Induction of apoptosis was related to the recruitment of the intrinsic mitochondrial apoptotic pathway, as shown by loss in mitochondrial membrane potential, cytochrome c release, caspase-9 and 3 activation and poly-(ADP-ribose)polymerase-1 cleavage. Moreover, licofelone induced the cleavage of the full-length p21(Bax) into p18(Bax), a more potent inducer of the apoptotic process than the uncleaved form. Pre-treatment of HCA-7 cells with the pan-caspase inhibitor z-VAD-fmk significantly blocked licofelone-induced apoptosis, confirming that this process occurred primarily in a caspase-dependent pathway. Licofelone was able to affect the arachidonic acid (AA) cascade, as it blocked the activity of 5-LOX and COX enzymes, and it induced, through the phosphorylation of cytoplasmic phospholipase A(2) (cPLA(2)), the release of unesterified AA from HCA-7 membrane phospholipids.

Storage & Handling

• Storage: store at low temperature,keep away from moisture | 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

ML 3000, ML3000, ML-3000, inhibit, Licofelone, Lipoxygenase, LOX, Inhibitor, COX, Cyclooxygenase, Apoptosis, 5-LOX

Compound Identifiers

PubChem CID

133021