COX-2/5-LOX-IN-3 (compound 5b) is a potent and dual COX-2/5-LOX inhibitor with IC50 values of 45.73, 5.45 and 4.33 μM for COX-1, COX-2, and 5-LOX, respectively. COX-2/5-LOX-IN-3 has the potential for the research of inflammation diseases[1].
Ibuprofen impurity 1 is an Ibuprofen impurity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively[1].
Etoricoxib-d3 is the deuterium labeled Etoricoxib[1]. Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood[2][3][4].
LM-4108 (N-(2-Phenylethyl)-indomethacin amide) is a selective and orally active COX-2 inhibitor with an IC50 of 0.06 μM for purified human COX-2. LM-4108 shows anti-inflammatory activity and may be effective in prevention of cancer. Half-lives for the disappearance of 10 μM LM-4108 in rat, human, and mouse liver microsomes were 11 min, 21 min, and 51 min, respectively[1].
K-80001 is an RXRα-binder and COX-1/2 inhibitor, with IC50s of with an IC50 of 82.9μM, 3.4μM, 1.2μM for RXRα, COX-1 and COX-2, respectively[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.
α-Chaconine, isolated from a Solanum tuberosum L. cv Jayoung, inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects[1].
Atractylochromene is a potent dual inhibitor of 5-LOX/COX-1 with IC50s of 0.6 and 3.3 μM, respectively[1].
3,3'-Diiodo-L-thyronine-13C6 is the 13C labeled 3,3'-Diiodo-L-thyronine[1]. 3,3'-Diiodo-L-thyronine (3,3'-T2) is an endogenous metabolite of thyroid hormone. 3,3'-Diiodo-L-thyronine significantly enhances COX activity[2][3].
COX-2-IN-18 (Compound 3) is a potent inhibitor of COX-2. COX-2-IN-18 possesses good COX-2 inhibitory activity (IC50 = 0.775 μM) compared to the reference drug, Celecoxib (IC50 = 0.153 μM). COX-2-IN-18 has the potential for the research of cancer diseases[1].
(Rac)-γ-Tocopherol (DMPBQ) is a Vitamin E isoform, which is converted by tocopherol cyclase to γ-Tcopherol[1].
Roburic acid, a tetracyclic triterpenoid found in Gentiana macrophylla, acts as an inhibitor of COX, with IC50s of 5 and 9 μM for COX-1 and COX-2, respectively[1].
COX-2-IN-11 (compound 7b2) is a potent and selective inhibitor of COX-2. COX-2-IN-11 has the potential for the research of inflammation diseases[1].
(±)-Catechin (rel-Cianidanol) is the racemate of Catechin. (±)-Catechin has two steric forms of (+)-Catechin and its enantiomer (-)-Catechin. (+)-Catechin inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM. Anticancer, anti-obesity, antidiabetic, anticardiovascular, anti-infectious, hepatoprotective, and neuroprotective effects[1].
COX-1/2-IN-2 is a potent COX1/2 inhibitor. COX-1/2-IN-2 exhibits significant inhibitory effect against COX-1 and COX-2 inhibitor with IC50 values of 13.9 ± 3.21 µM and 6.4±0.74 µM, respectively[1].
Hirsutanonol ((5S)-Hirsutanonol) is a diarylheptanoid that can be isolated from the bark of Alnus hirsute var. sibirica. Hirsutanonol inhibits cyclooxygenase-2 (COX-2) expression. Hirsutanonol has anti-filarial with an IC50 value of 44.11 μg/mL for microfilariae[1].
Amtolmetin guacil is an effective nonsteroidal anti-Inflammatory agent with pain-relieving effects. Amtolmetin guacil inhibits prostaglandin synthesis and cyclooxygenase (COX). Amtolmetin guacil can stimulate capsaicin receptors present on the gastrointestinal wall and also releases gastroprotective nitric oxide (NO). Amtolmetin guacil can be used to research knee osteoarthritis[1][2].
Ampyrone-d3-1 is the deuterium labeled Ampyrone. Ampyrone is a reagent for glucose determination in the presence of peroxidase and phenol.
Vedaprofen (Quadrisol) is a COX-1 selective nonsteroidal anti-inflammatory drug (NSAID) for serum TxB2 and exudate PGE2 inhibition [1]. Vedaprofen is a Escherichia coli (E. coli) sliding clamp (SC) inhibitor with the IC50 of 222 μM[2].
N-Acetyl-2-carboxybenzenesulfonamide is an orally active COX-1 and COX-2 inhibitor with IC50s of 0.06 μM and 0.25 μM, respectively. N-Acetyl-2-carboxybenzenesulfonamide shows anti-inflammatory activity[1].
Paradol is a pungent phenolic substance found in ginger and other Zingiberaceae plants. Paradol is an effective inhibitor of tumor promotion in mouse skin carcinogenesis, binds to cyclooxygenase (COX)-2 active site.
β-Elemonic acid is a triterpene isolated from Boswellia papyrifera. β-Elemonic acid induces cell apoptosis, reactive oxygen species (ROS) and COX-2 expression and inhibits prolyl endopeptidase. β-Elemonic acid exhibits anticancer and anti-inflammatory effects[1][2].
Hydrangenol is an orally active antiphotoaging compound. It can be isolated from Hydrangea serrata leaves. Hydrangenol prevents wrinkle formation by reducing MMP and inflammatory cytokine expression and increasing moisturizing factors and antioxidant genes level[1].
Lumiracoxib-d6 (COX-189-d6) is the deuterium labeled Lumiracoxib. Lumiracoxib is a potent,selective and orally active COX-2 inhibitor with a Ki value of 0.06 μM[1]. Lumiracoxib acts as a nonselective NSAID with anti-inflammatory, analgesic and antipyretic activities. Lumiracoxib can be used for osteoarthritis and bone cancer research[1][2].
COX-1/2-IN-3 (Compound 7a) is a COX-1 and COX-2 inhibitor. COX-2-IN-15 shows anti-inflammatory activity with low toxicity[1].
COX-2-IN-23 (compound 9a) is a selective COX-2 inhibitor with IC50 values of 0.28 and 20.14 μM for COX-2 and COX-1. COX-2-IN-23 has anti-inflammatory activity and low ulcerogenic activity.
Flufenamic acid-13C6 is the 13C6 labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
COX-2-IN-28 is a potent and selective COX-2 inhibitor with IC50 values of 0.054, 2.14, 13.21 µM for COX-2, 15-LOX, COX-1,respectively[1].
Benzoylgomisin O isolated from Schisandra rubriflora, has inhibitory activity against 15-LOX, COX-1 and COX-2 enzymes and anti-inflammatory activity[1].
Flufenamic acid-d4 is deuterium labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.