Oxaprozin

Oxaprozin is an orally active and potent COX inhibitor, with IC₅₀ values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB. Oxaprozin induces cell apoptosis. Oxaprozin shows anti-inflammatory activity. Oxaprozin-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties^[1][2]. IC50 & Target: IC50: 2.2 μM (COX-1), 36 μM (COX-2)，NF-κB^[1] In Vitro: Oxaprozin induces apoptosis in a dose-dependent manner. Oxaprozin increases caspase-3 activity in the activated but not in the resting condition. NF-κB activation is inhibited by Oxaprozin (50 μM). Oxaprozin inhibits activation of the IKK system induced by the reagent IκBα^[1].
Oxaprozin (100 μM) induces the strongest proapoptotic effect and significantly increases CD40L-treated monocyte apoptosis. Oxaprozin treatment inhibits CD40L-induced Akt and NF-κB (p65) phosphorylation^[2].