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COX2 Inhibitor Screening Kit (Fluorometric) (ab283401) offers a rapid, simple, sensitive, and reliable test suitable for high-throughput screening of COX-2 inhibitors.

Individual kit components also available for purchase with a minimum order of 20 units. Contact us to discuss your needs.

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Functional Studies - COX2 Inhibitor Screening Kit (Fluorometric) (AB283401), expandable thumbnail

Publications

Key facts

Detection method

Fluorescent

Sample types

Inhibitor compounds

Target data

Function

Dual cyclooxygenase and peroxidase in the biosynthesis pathway of prostanoids, a class of C20 oxylipins mainly derived from arachidonate, with a particular role in the inflammatory response (PubMed:7947975, PubMed:7592599, PubMed:9261177, PubMed:16373578, PubMed:22942274, PubMed:26859324, PubMed:27226593, PubMed:11939906, PubMed:19540099). The cyclooxygenase activity oxygenates arachidonate (AA, C20:4(n-6)) to the hydroperoxy endoperoxide prostaglandin G2 (PGG2), and the peroxidase activity reduces PGG2 to the hydroxy endoperoxide PGH2, the precursor of all 2-series prostaglandins and thromboxanes (PubMed:7947975, PubMed:7592599, PubMed:9261177, PubMed:16373578, PubMed:22942274, PubMed:26859324, PubMed:27226593). This complex transformation is initiated by abstraction of hydrogen at carbon 13 (with S-stereochemistry), followed by insertion of molecular O2 to form the endoperoxide bridge between carbon 9 and 11 that defines prostaglandins. The insertion of a second molecule of O2 (bis-oxygenase activity) yields a hydroperoxy group in PGG2 that is then reduced to PGH2 by two electrons (PubMed:7947975, PubMed:7592599, PubMed:9261177, PubMed:16373578, PubMed:22942274, PubMed:26859324, PubMed:27226593). Similarly catalyzes successive cyclooxygenation and peroxidation of dihomo-gamma-linoleate (DGLA, C20:3(n-6)) and eicosapentaenoate (EPA, C20:5(n-3)) to corresponding PGH1 and PGH3, the precursors of 1- and 3-series prostaglandins (PubMed:11939906, PubMed:19540099). In an alternative pathway of prostanoid biosynthesis, converts 2-arachidonoyl lysophopholipids to prostanoid lysophopholipids, which are then hydrolyzed by intracellular phospholipases to release free prostanoids (PubMed:27642067). Metabolizes 2-arachidonoyl glycerol yielding the glyceryl ester of PGH2, a process that can contribute to pain response (PubMed:22942274). Generates lipid mediators from n-3 and n-6 polyunsaturated fatty acids (PUFAs) via a lipoxygenase-type mechanism. Oxygenates PUFAs to hydroperoxy compounds and then reduces them to corresponding alcohols (PubMed:11034610, PubMed:11192938, PubMed:9048568, PubMed:9261177). Plays a role in the generation of resolution phase interaction products (resolvins) during both sterile and infectious inflammation (PubMed:12391014). Metabolizes docosahexaenoate (DHA, C22:6(n-3)) to 17R-HDHA, a precursor of the D-series resolvins (RvDs) (PubMed:12391014). As a component of the biosynthetic pathway of E-series resolvins (RvEs), converts eicosapentaenoate (EPA, C20:5(n-3)) primarily to 18S-HEPE that is further metabolized by ALOX5 and LTA4H to generate 18S-RvE1 and 18S-RvE2 (PubMed:21206090). In vascular endothelial cells, converts docosapentaenoate (DPA, C22:5(n-3)) to 13R-HDPA, a precursor for 13-series resolvins (RvTs) shown to activate macrophage phagocytosis during bacterial infection (PubMed:26236990). In activated leukocytes, contributes to oxygenation of hydroxyeicosatetraenoates (HETE) to diHETES (5,15-diHETE and 5,11-diHETE) (PubMed:22068350, PubMed:26282205). During neuroinflammation, plays a role in neuronal secretion of specialized preresolving mediators (SPMs) 15R-lipoxin A4 that regulates phagocytic microglia (By similarity).

Alternative names

What's included?

100 Test
Components
Arachidonic Acid
1 x 1 Vial
COX Assay Buffer
1 x 25 mL
COX Cofactor
1 x 20 µL
Celecoxib (COX-2 Inhibitor)
1 x 100 µL
Human Recombinant COX-2
1 x 1 Vial
NaOH Solution
1 x 500 µL
OxiRed Probe
1 x 200 µL

Recommended products

COX2 Inhibitor Screening Kit (Fluorometric) (ab283401) offers a rapid, simple, sensitive, and reliable test suitable for high-throughput screening of COX-2 inhibitors.

Individual kit components also available for purchase with a minimum order of 20 units. Contact us to discuss your needs.

Alternative names

Key facts

Detection method

Fluorescent

Sample types

Inhibitor compounds

Assay Platform

Microplate (12 x 8 well strips)

Storage

Shipped at conditions

Blue Ice

Appropriate short-term storage conditions

-20°C

Appropriate long-term storage conditions

-20°C

Storage information

-20°C

Notes

COX2 Inhibitor Screening Kit (Fluorometric) (ab283401) offers a rapid, simple, sensitive, and reliable test suitable for high-throughput screening of COX-2 inhibitors.

Cyclooxygenase (COX), also known as prostaglandin-endoperoxide synthase, , is an enzyme that is responsible for the formation of important biological mediators called prostanoids, including prostaglandins, prostacyclin and thromboxane. COX is the central enzyme in the biosynthetic pathway to prostanoids from arachidonic acid. There are two known isoenzymes: COX-1 and COX-2. COX-2 is not expressed under normal conditions in most cells, but elevated levels are found during inflammation.

This assay is based on the fluorometric detection of Prostaglandin G2, the intermediate product generated by the COX enzyme.

This product is manufactured by BioVision, an Abcam company and was previously called K547 COX-2 Inhibitor Screening Kit (Fluorometric). K547-100 is the same size as the 100 test size of ab283401.

Supplementary info

This supplementary information is collated from multiple sources and compiled automatically.

Activity summary

Cyclooxygenase-2 (COX-2) also known as prostaglandin-endoperoxide synthase 2 is an enzyme with a mass of about 72 kDa. It is a vital component in the conversion of arachidonic acid to prostaglandins which are lipid compounds that exhibit a variety of physiological functions. COX-2 is an inducible enzyme meaning its expression can be increased by various factors such as cytokines and growth factors. It is typically present in inflammatory sites as well as in the brain kidney and other tissues under specific conditions.

Biological function summary

COX-2 participates in processes related to inflammation and pain. Although it primarily functions as an individual enzyme it can interact with other proteins in tissue-specific contexts. COX-2 is particularly important in situations requiring an increased prostaglandin production like inflammatory responses and the healing of wounds. It contributes to the regulation of normal physiological functions including renal hemodynamics and the regulation of blood flow within the kidney.

Pathways

The COX-2 enzyme plays a substantial role in the arachidonic acid metabolic pathway. It engages in this pathway by facilitating the biosynthesis of prostaglandins from arachidonic acid. COX-2 operates alongside other proteins such as COX-1 which is its constitutively expressed counterpart as well as other enzymes involved in prostaglandin synthesis like lipoxygenases. This shared pathway highlights the coordinated efforts required in regulating inflammation and maintaining tissue homeostasis.

Associated diseases and disorders

COX-2 has been closely linked to conditions such as arthritis and cancer. In arthritis COX-2 contributes to the chronic inflammation and pain observed in affected joints. In cancer overexpression of COX-2 has been observed in various tumor types where it may promote tumor growth and inhibit apoptosis. Celecoxib a COX-2 inhibitor is often used to reduce disease symptoms by targeting COX-2’s role in these pathological processes. Through its involvement in these disorders COX-2 also interacts indirectly with other critical proteins like nuclear factor kappa B (NF-kB) that participate in inflammatory and tumor pathways.

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1 product image

  • Functional Studies - COX2 Inhibitor Screening Kit (Fluorometric) (ab283401), expandable thumbnail

    Functional Studies - COX2 Inhibitor Screening Kit (Fluorometric) (ab283401)

    COX2 Inhibitor Screening Kit.

    Inhibition of COX2 Activity with Celecoxib. IC50 of Celecoxib was determined to be 0.45 μM.

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Product protocols

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