COX-2-IN-5 (compound 11a) is a potent COX-2 inhibitor with an IC50 value of 0.65 µM. COX-2-IN-5 has the potential for the research of inflammation[1].
Desoxo-narchinol A is an orally active and potent anti-inflammatory agent. Desoxo-narchinol A can be isolated from the roots and rhizomes of Nardostachys jatamansi. Desoxo-narchinol A can be used for septic shock and inflammatory diseases research[1][2][3].
Ocarocoxib, a potent COX-2 (cyclooxygenase-2) inhibitor, is a non-steroidal anti-inflammatory for veterinary use[1].
γ-Tocopherol (D-γ-Tocopherol) is a potent cyclooxygenase (COX) inhibitor. γ-Tocopherol is a naturally occurring form of Vitamin E in many plant seeds, such as corn oil and soybeans. γ-Tocopherol possesses antiinflammatory properties and anti-cancer activity[1].
AG-024322 is a potent ATP-competitive pan-CDK inhibitor against cell cycle kinases CDK1, CDK2, and CDK4 with Ki values in the 1-3 nM range[1]. AG-024322 displays broad-spectrum anti-tumor activity and clear target modulation in vivo. AG-024322 induces cell apoptosis[3].
Tazofelone (LY 213829) is a cyclooxygenase-II (COX-II) inhibitor. Tazofelone transform into sulfoxide and quinol metabolites is primarily mediated by CYP3A. Tazofelone can be used for the research of inflammatory bowel disease[1][2].
CAY10404 is a potent and highly selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM. CAY10404 exhibits no inhibition of COX-1 (IC50>500 µM)[1]. CAY10404 is a potent inhibitor of PKB/Akt and MAPK signaling pathways and induces apoptosis in NSCLC cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities[2][3].
Guaiacol-13C6 is the 13C labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Ketorolac (RS37619) hemicalcium is a non-steroidal anti-inflammatory drug (NSAID), acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2. Ketorolac tromethamine is used as 0.5% ophthalmic solution for the research of allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and postoperative ocular inflammation and pain. Ketorola chemicalcium is also a DDX3 inhibitor that can be used for cancer research[1][4].
Harpagoside is isolated from Harpagophytum procumbens (Hp). Harpagoside has inhibitory effects on COX-1 and COX-2 activity and inhibits NO production[1].
Isoxicam is an orally active, long-acting, non-steroidal anti-inflammatory agent for the research of arthritis[1]. Isoxicam is a nonselective inhibitor of COX-1 and COX-2[2].
Dehydrodiisoeugenol is isolated from Myristica fragrans Houtt, shows anti-inflammatory and anti-bacterial actions[1]. Dehydrodiisoeugenol inhibits LPS- stimulated NF-κB activation and cyclooxygenase (COX)-2 gene expression in murine macrophages[2].
COX-2-IN-17 (compound 10) is a potent and BBB-penetrated COX-2 (cyclooxygenase-2) inhibitor, with an IC50 of 0.02 μM. COX-2-IN-17 shows anti-inflammatory and analgesic activities. COX-2-IN-17 attenuates hyperalgesia in the neurogenic phase as well as the inflammatory phase[1].
Celecoxib is a selective COX-2 inhibitor with an IC50 of 40 nM.
Licofelone-d6 is the deuterium labeled Licofelone[1]. Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins[2][3][4].
Oxaprozin potassium 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 potassium also inhibits the activation of NF-κB. Oxaprozin potassium induces cell apoptosis. Oxaprozin potassium shows anti-inflammatory activity. Oxaprozin potassium-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties[1][2].
Carprofen-13C,d3 is the deuterium and 13C labeled Carprofen[1]. Carprofen is a nonsteroid anti-inflammatory agent, acts as a multi-target FAAH/COX inhibitor, with IC50s of 3.9 μM, 22.3 μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively[2][3][4].
Benoxaprofen (LRCL 3794) is a potent and long-acting anti-inflammatory and antipyretic compound. Benoxaprofen is a relatively weak inhibitor of cyclooxygenase in in vitro systems, inhibits lipoxygenase in other systems, and inhibits monocyte migration in some animal models of inflammation[1][2].
Plantanone B is a moderate antioxidant-agent with an IC50 of 169.8±5.2 μM. Plantanone B shows significant ovine COX-1 and moderate COX-2 inhibitory activities. Plantanone B has the potential for inflammation-related diseases research[1].
PPOH, a fatty acid derivative, is a selective cyclooxygenase (COX) inhibitor that inhibits arachidonic acid cyclooxygenase activity in renal cortical microsomes. In addition, PPOH acts on CYP4A2 and CYP4A3 with the IC50 values of 22 μM and 6.5 μM, respectively[1].
Hamaudol is a chromone isolated from Saposhnikovia divaricata. Hamaudol shows significant inhibitory activity on cyclooxygenase (COX)-1 and COX-2 activities with IC50 values of 0.30, 0.57 mM, respectively, and has potent analgesia and anti-inflammary effects[1][2].
Buddlejasaponin IV (BS‐IV) exerts anti-inflammatory and cytotoxic effects against cancer cells[1].
COX-2-IN-36 (compound 1) is a very potent and specific COX-2 inhibitor, with an IC50 of 0.4 μM[1][2].
PTUPB is a novel dual acting COX-2/sEH inhibitor with IC50 of 1.26 uM/0.9 nM,does not inhibits COX-1 (IC50>100 uM); reduces kidney injury parameters, decreases inflammatory and oxidative stress markers in ZDF rats; exhibits more effective than the same dose of either COX-2 inhibitor (celecoxib) or sEH inhibitor (t-AUCB) alone, shows in vivo antiallodynic activity in vivo; also suppresses glioblastoma growth by targeting EGFR and hyaluronan mediated motility receptor, potentiates the antitumor efficacy of cisplatin.
Pentagamavunon-1 (PGV-1), a Curcumin analog with oral activity, targets on several molecular mechanisms to induce apoptosis including inhibition of angiogenic factors cyclooxygenase-2 (COX-2) and vascular endothelial growth factor (VEGF). PGV-1 inhibits NF-κB activation[1].
Phenacetin is a non-opioid analgesic without anti-inflammatory properties, inhibits COX-3 activity.Target: COXPhenacetin is a pain-relieving and fever-reducing drug, Phenacetin was withdrawn from the Canadian market in June 1973 due to concerns regarding nephropathy. the clinical and laboratory data were compatible with "phenacetin nephritis" as described in Europe and Australia and recently in the United States and Canada. This report evaluates the findings in the 23 cases and cautions against the use of phenacetin, particularly in patients with impaired renal function [1]. Phenacetin has been linked to renal papillary necrosis in human beings [2, 3].
(S)-Flurbiprofen is an active enantiomer of Flurbiprofen, with IC50 values of 0.48 μM and 0.47 μM for COX-1 and COX-2, respectively[1].
COX-2-IN-24 is an orally active inhibitor of COX-2 with IC50 value of 0.17 μM, shows anti-inflammatory and low ulcerogenic activities.
COX-2-IN-16 (compound 2b) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 102 µM. COX-2-IN-16 inhibits the NO production. COX-2-IN-16 shows anti-inflammatory activity[1].
Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 µM, 1.47 µM, and 1.06 µM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.