COX

1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid (Standard) is the analytical standard of 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid (HY-N4226). This product is intended for research and analytical applications. 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid is an AP-1 inhibitor which can be found in Cordyceps bassiana. 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid downregulates the expression of COX-2. 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid can be used for the study of atopic dermatitis.

(E)-Ethyl p-methoxycinnamate (Standard) is the analytical standard of (E)-Ethyl p-methoxycinnamate. This product is intended for research and analytical applications. (E)-Ethyl p-methoxycinnamate is a natural product found in Kaempferia galangal with anti-inflammatory, anti-neoplastic and anti-microbial effects. (E)-Ethyl p-methoxycinnamate inhibits COX-1 and COX-2 in vitro with IC₅₀s of 1.12 and 0.83 μM, respectively.

BPN-37440 is a blood-brain barrier-permeable, selective, and orally active EP2 receptor inhibitor with an IC₅₀ of 53-60 nM. BPN-37440 inhibits the expression of inflammatory mediators IL-1β and COX-2, with an IC₅₀ of 21 nM for IL-1β and 42 nM for COX-2. BPN-37440 reduces microgliosis in key brain regions of mice with pilocarpine (HY-B0726A)-induced status epilepticus and reverses their working memory and recognition memory deficits. BPN-37440 can be used for research on status epilepticus.

Caspase-3/7 activator 4 is a caspase-3 activator and caspase-7 activator. Caspase-3/7 activator 4 inhibits key enzymes in estrogen biosynthesis, including aromatase (IC₅₀ = 38.3 nM) and steroid sulfatase (IC₅₀ = 12.7 µM), and selectively suppresses COX-2 (IC₅₀ = 5.38 µM). Caspase-3/7 activator 4 shows strong antioxidant activity (DPPH: IC₅₀ = 16.26 µM). Caspase-3/7 activator 4 inhibits estrogen synthesis, suppresses estrogen availability, reduces prostaglandin production, increases caspase-3/7 expression, induces G0/G1 cell cycle arrest, induces apoptotic cell death, reduces circulating TNF-α and VEGFR-II levels, restores hepatorenal function markers and histoarchitecture, restores antioxidant defense enzyme activity, reduces lipid peroxidation, exerts antiproliferative activity against breast cancer cells, exerts antitumor activity in the Ehrlich ascites carcinoma models. Caspase-3/7 activator 4 can be used for the research of breast cancer, ehrlich ascites carcinoma.

Metyrosine-¹³C₉,¹⁵N,d₇ is the deuterium, ¹³C-, and 15-labeled Metyrosine. Metyrosine is a selective tyrosine hydroxylase enzyme inhibitor. Metyrosine exerts anti-inflammatory and anti-ulcerative effects. Metyrosine significantly inhibits high COX-2 activity. Metyrosine is a very effective agent for blood pressure control.

TU-100 is a Japanese herbal medicine. TU-100 exhibits anti-cancer effects by regulating cancer-associated fibroblasts (CAFs) in the TME. TU-100 can antagonize the M2 polarization phenotype of macrophages in the tumor microenvironment by suppressing the TLR4/NF-κB/STAT3 axis. TU-100 can inhibit the high expression of MMP-2, COX-2, and VEGF in TAMs.

Hordenine (Standard) (Ordenina (Standard); Peyocactine (Standard)) is the analytical standard of Hordenine (HY-N0113). This product is intended for research and analytical applications. Hordenine (Ordenina; Peyocactine) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine promotes M2 macrophage polarization, restores blood-milk barrier integrity, alleviates oxidative stress by reducing ROS and MDA, and attenuates LPS-induced lung injury and pulmonary edema. Hordenine inhibits cAMP production, CREB phosphorylation, and MITF expression, thereby suppressing melanin synthesis in melanocytes and reconstructed epidermis. Hordenine activates the Wnt/β-catenin signaling pathway, promotes dermal papilla cell proliferation and hair shaft elongation, and accelerates hair regeneration. Hordenine activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine limits alcohol intake, reduces relapse drinking behavior, and modulates alcohol-induced conditioned place preference. Hordenine can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder.

COX-2/NO-IN-1 is an orally active nitric oxide synthase (iNOS), COX-2 expression and NO (IC₅₀ of 3.52 μM) inhibitor. COX-2/NO-IN-1 has anti-inflammatory effects.

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.

Parameritannin A-1 is a tetrameric proanthocyanidin (PAC) that can be isolated from the bark of Parameria laevigata Moldenke (Apocynaceae). Parameritannin A-1 is a COX-2 inhibitor. Parameritannin A-1 also inhibits the activity of phospholipase A₂ (PLA₂).

Justalakonin is an arylnaphthalene glycoside that is found in Justicia purpurea. Justalakonin exhibits no significant inhibitory effects on lipid peroxidation, COX‑1, or the proliferation of various tumor cells, but possesses COX-2 inhibitory activity.

Naproxen (sodium) (Standard) is the analytical standard of Naproxen (sodium). This product is intended for research and analytical applications. Naproxen sodium is a COX-1 and COX-2 inhibitor with IC₅₀s of 8.72 and 5.15 μM, respectively in cell assay.

Ibuprofen-¹³C,d₃ is the ¹³C- and deuterium labeled Ibuprofen. Ibuprofen is an anti-inflammatory agent targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.

Anticancer agent 166 (compound 3) is an anticancer agent with an excellent inhibition activity against Caco-2 (IC₅₀ = 9.6 nM).

4F-PMPH is a COX-II inhibitor with anti-inflammatory activity. 4F-PMPH binds to the active site of COX-II by forming key interactions with residues such as Val102, Tyr341, and Leu338.

COX-2/CA II-1 is an orally active dual selective inhibitor targeting COX-2 and hCA II. COX-2/CA II-1 inhibits COX-2 with an IC₅₀ value of 0.13 μM (SI = 9.25 vs COX-1) and hCA II with a K_i value of 39.1 nM (SI = 933.8 vs hCA I). COX-2/CA II-1 demonstrates significant analgesic and anti-inflammatory effects in animal models, shows improved gastric safety with reduced ulcerogenic liability, and exhibits intraocular pressure (IOP)-lowering effects in rabbit glaucoma models. COX-2/CA II-1 can be used for anti-inflammatory, analgesic and antiglaucoma research.

Ermanin is a flavonoid isolated from Tanacetum microphyllum. Ermanin potently inhibits iNOS, COX-2 activities, and inhibits platelet aggregation. Ermanin has anti-inflammatory, anti-tuberculous and anti-viral/bacterial properties.

Nitroparacetamol (NCX-701) is a nitric oxide (NO) donor-non-steroidal anti-inflammatory agent (NO-NSAID). Nitroparacetamol is formed by the ester linkage of Acetaminophen (HY-66005) and Nitrooxybutyroyl, aiming to combine the analgesic advantage of Acetaminophen with the organ-protective effect of nitric oxide, while expanding its anti-inflammatory activity. The analgesic spectrum of Nitroparacetamol is broader, and it is effective for painful pathological pain, and significantly reduces hepatotoxicity. Nitroparacetamol can reduce the expressions of IL-1β, TNF-α, COX-2, and iNOS.

Indomethacin farnesil is an orally active proagent of Indomethacin. Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC₅₀s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes.

Aspirin calcium is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC₅₀ values of 5 and 210 μg/mL, respectively. Aspirin calcium induces apoptosis. Aspirin calcium inhibits the activation of NF-κB. Aspirin calcium also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis.