2. Signaling Pathways
  3. Immunology/Inflammation
  4. COX

COX

Cyclooxygenase

COX

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Cyclooxygenase (COX), officially known as prostaglandin-endoperoxide synthase (PTGS), is an enzyme that is responsible for formation of important biological mediators called prostanoids, including prostaglandins, prostacyclin and thromboxane. Pharmacological inhibition of COX can provide relief from the symptoms of inflammation and pain. Drugs, like Aspirin, that inhibit cyclooxygenase activity have been available to the public for about 100 years. Two cyclooxygenase isoforms have been identified and are referred to as COX-1 and COX-2. Under many circumstances the COX-1 enzyme is produced constitutively (i.e., gastric mucosa) whereas COX-2 is inducible (i.e., sites of inflammation). Non-steroidal anti-inflammatory drugs (NSAID), such as aspirin and ibuprofen, exert their effects through inhibition of COX. The main COX inhibitors are the non-steroidal anti-inflammatory drugs (NSAIDs).

COX Isoform Specific Products:

COX Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B1279AS
    Metamizole-d3 sodium
    Metamizole-d3 sodium is the deuterium labeled Metamizole sodium. Metamizole sodium is a non-opioid compound with excellent analgesic and antipyretic effects. Metamizole sodium is a cyclooxygenase-3 (COX-3) inhibitor.
    Metamizole-d<sub>3</sub> sodium
  • HY-106093
    Eltenac
    		Inhibitor
    Eltenac, a non-steroidal anti-inflammatory drug (NSAID), is a COX inhibitor. Eltenac shows IC50 of 0.03 μM for both COX-1 and COX-2 in isolated human whole blood.
    Eltenac
  • HY-179439
    Multi-kinase-IN-8
    		Inhibitor
    Multi-kinase-IN-8 is a muti-kinase inhibitor. Multi-kinase-IN-8 inhibits COX-1 (IC50 of 12.6 μM), COX-2 (IC50 of 0.05 μM) and VEGFR-2 (IC50 of 0.12 nM). Multi-kinase-IN-8 inhibits tumor-associated carbonic anhydrases (CA IX and CA XII with Ki of 31.5 nM and 386.9 nM, respectively). Multi-kinase-IN-8 triggers cell cycle arrest and apoptosis through upregulation of Caspase 9 and Bax along with downregulation of Bcl 2. Multi-kinase-IN-8 suppresses PGE2, p-VEGFR-2, MMP-9 and HIF-1α and exhibits growth-inhibitory activity against breast cancer, lung cancer, and colorectal adenocarcinoma.
    Multi-kinase-IN-8
  • HY-105667
    Butanixin
    		Inhibitor
    Butanixin (2-[(4-Butylphenyl)amino]-3-pyridinecarboxylic acid) is a cyclooxygenase (COX) inhibitor. It exerts anti-inflammatory and analgesic activity by reducing prostaglandin production. It is used in the research of musculoskeletal disorders.
    Butanixin
  • HY-B1888AS
    Bromfenac-d4 sodium
    		Inhibitor
    Bromfenac-d4 (sodium) is deuterium labeled Bromfenac (sodium). Bromfenac sodium is a potent and orally active inhibitor of COX, with IC50s of 5.56 and 7.45 nM for COX-1 and COX-2, respectively. Bromfenac sodium is a brominated non-steroidal anti-inflammatory/analgesic agent (NSAID), and it is commonly used for the research of postoperative inflammation and pain following cataract surgery, and pseudophakic cystoid macular edema (CME).
    Bromfenac-d<sub>4</sub> sodium
  • HY-N19723
    Buddlejasaponin I
    		Inhibitor
    Buddlejasaponin I (Verbascosaponin B) is an inhibitor of COX and 5-LOX. Buddlejasaponin I inhibits the production of COX metabolites PGE2, TXB2, and the 5-LOX metabolite LTC4. Buddlejasaponin I reduces ear swelling in mice. Buddlejasaponin I is applicable to inflammation-related research.
    Buddlejasaponin I
  • HY-N13238
    White Willow Bark Extract
    		Inhibitor
    White Willow Bark Extract is the extract of White Willow Bark, with content of 15% , 25% , 50% Salicin.
    White Willow Bark Extract
  • HY-N18025
    Kaempferol 3-O-(2G-glucosylrutinoside)-7-O-glucoside
    		Inhibitor
    Kaempferol 3-O-(2G-glucosylrutinoside)-7-O-glucoside is an anti-inflammatory agent. Kaempferol 3-O-(2G-glucosylrutinoside)-7-O-glucoside exerts significant anti-inflammatory effects in LPS (HY-D1056)-induced RAW 264.7 macrophages by inhibiting the NF-κB, MAPK and Akt signaling pathways, thereby reducing the production of inflammatory mediators (NO, PGE2) and pro-inflammatory cytokines (TNF-α, IL-1β, IL-6).
    Kaempferol 3-O-(2G-glucosylrutinoside)-7-O-glucoside
  • HY-179021
    COX-2/15-LOX-IN-7
    		Inhibitor
    COX-2/15-LOX-IN-7 is a potent, selective and orally active dual inhibitor of COX-2 and 15-LOX with IC50 values of 0.022 and 1.19 μM. COX-2/15-LOX-IN-7 also inhibits COX-1 with an IC50 value of 28.081μM. COX-2/15-LOX-IN-7 has low cytotoxicity against human colorectal cancer HT-29 and HCT116 cell lines (IC50 >100 μM for both). COX-2/15-LOX-IN-7 exhibits non-ulcerogenic performance. COX-2/15-LOX-IN-7 can be used for the research of cancer.
    COX-2/15-LOX-IN-7
  • HY-165394
    Melafolone
    		Inhibitor
    Melafolone is a potent dual COX-2/EGFR inhibitor with IC50s of 13.2 μM (COX-2) and 17.4 μM (EGFR). Melafolone enhances the effect of anti-PD-1 through vascular normalization and PD-L1 downregulation via the PI3K/Akt pathway in Lewis lung carcinoma (LLC) and CMT167 models. Melafolone can be used for lung cancer research.
    Melafolone
  • HY-B0227S2
    Ketoprofen-13C,d3
    		Inhibitor
    Ketoprofen-13C,d3 is the 13C- and deuterium labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively.
    Ketoprofen-<sup>13</sup>C,d<sub>3</sub>
  • HY-105874
    Tomoxiprole
    		Inhibitor
    Tomoxiprole (MDL 035) is a new analgesic antiinflammatory agent. Tomoxiprole selectively inhibits cyclooxygenase-2 (IC50 = 7 nM) .
    Tomoxiprole
  • HY-115921
    Anti-inflammatory agent 9
    Anti-inflammatory agent 9 (compound 28) is a tilomisole-based benzimidazothiazole derivative. Anti-inflammatory agent 9 expresses activity on COX-2 enzyme more than COX-1. Anti-inflammatory agent 9 is orally active.
    Anti-inflammatory agent 9
  • HY-174159
    COX-2-IN-54
    		Inhibitor
    COX-2-IN-54 (Compound 7y) is an orally active COX-2 inhibitor with an IC50 of 4.15 μM. COX-2-IN-54 has a strong protective effect against DSS-induced ulcerative colitis and can significantly reduce tissue damage. COX-2-IN-54 has anti-inflammatory activity.
    COX-2-IN-54
  • HY-155753
    Anti-inflammatory agent 50
    		Inhibitor
    Anti-inflammatory agent 50 (compound a1) is a Fusidic acid derivative with anti-inflammatory effects. Anti-inflammatory agent 50 inhibits inflammatory factor NO, IL-6 and TNF-α. Anti-inflammatory agent 50 alleviates acute lung injury by regulating inflammatory mediators and suppressing the MAPK, NF-κB and NLRP3 inflammasome signaling pathways.
    Anti-inflammatory agent 50
  • HY-14670R
    Firocoxib (Standard)
    		Inhibitor
    Firocoxib (Standard) is the analytical standard of Firocoxib. This product is intended for research and analytical applications. Firocoxib (ML 1785713) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 0.13 μM. Firocoxib shows 58-fold more selective for COX-2 than COX-1 (IC50 of 7.5 μM). Firocoxib has anti-inflammatory effects.
    Firocoxib (Standard)
  • HY-N10009
    Cudraflavone B
    		Inhibitor
    Cudraflavone B is a prenylated flavonoid with anti-inflammatory and anti-tumor properties. Cudraflavone B is also a dual inhibitor of COX-1 and COX-2. Cudraflavone B blocks the translocation of nuclear factor κB (NF-κB) from the cytoplasm to the nucleus in macrophages. Thus, Cudraflavone B inhibits tumor necrosis factor α (TNFα) gene expression and secretion. Cudraflavone B also triggers the mitochondrial apoptotic pathway, activates NF-κB, the MAPK p38, and ERK, and induced the expression of SIRT1. Thus Cudraflavone B inhibits the growth of human oral squamous cell carcinoma cells.
    Cudraflavone B
  • HY-N6189
    MBL-1
    		Inhibitor
    MBL-1 is an orally active anti-inflammatory agent. MBL-1 can be isolated from the fermentation broth of Aspergillus sp. derived from gorgonians. MBL-1 inhibits the activity of the hCOX-2 protein with an IC50 of 5.77 μM. MBL-1 reduces the production of key pro-inflammatory mediators such as NO, ROS, IL-1β and IL-18 by inhibiting the MAPK/NF-κB and NLRP3 signaling pathways. MBL-1 exerts a protective effect against DSS-induced colitis. MBL-1 can be used for the research of ulcerative colitis.
    MBL-1
  • HY-N3631
    Ethoxycoronarin D
    		Inhibitor
    Ethoxycoronarin D is a labdane diterpenes compound isolated from rhizomes. Ethoxycoronarin D selectively inhibits COX-1 with an IC50 of 3.8 µM.
    Ethoxycoronarin D
  • HY-155780
    Anti-inflammatory agent 52
    		Inhibitor
    Anti-inflammatory agent 52 (compound 7j) is an orally active selective COX-2 inhibitor. Anti-inflammatory agent 52 has anti-HT29 transfer activity, which leads to periodic arrest in G2/M phase. Anti-inflammatory agent 52 has safety, moderate ability to suppress inflammation. Anti-inflammatory agent 52 has a rare property of suppressing the development of tumor in mouse model, showing anti-cancer activity.
    Anti-inflammatory agent 52
Cat. No. Product Name / Synonyms Application Reactivity
COX Isoform Comparison

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