COX (Cyclooxygenase)

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

click to view more

Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S1261

Celecoxib

Celecoxib is a selective COX-2 inhibitor with IC50 of 40 nM in Sf9 cells.

S1255

Nepafenac

Nepafenac is a prodrug of amfenac that acts as an inhibitor of COX-1 and COX-2 activity, used in the treatment of pain and inflammation associated with cataract surgery.

S1638

Ibuprofen

Ibuprofen (Dolgesic) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively.

S1723

Indomethacin

Indomethacin is a nonselective COX1 and COX2 inhibitor with IC50 of 0.1 μg/mL and 5 μg/mL, respectively, used to reduce fever, pain, stiffness, and swelling.

S2007

Sulindac

Sulindac is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions.

S8433New

NS-398 (NS398)

NS-398 is a selective inhibitor of cyclooxygenase-2 (COX-2). The IC50 values for human recombinant COX-1 and -2 are 75 and 1.77 μM, respectively.

S1634New

Acetaminophen

Acetaminophen is a COX inhibitor for COX-1 and COX-2 with IC50 of 113.7 μM and 25.8 μM, respectively.

S4686New

Vitamin E

Vitamin E is a fat-soluble vitamin with potent antioxidant properties. It is a potent peroxyl radical scavenger and inhibits noncompetitively cyclooxygenase activity in many tissues, also inhibits angiogenesis and tumor dormancy through suppressing vascular endothelial growth factor (VEGF) gene transcription.

S4651New

Etoricoxib

Etoricoxib is a new COX-2 selective inhibitor with anti-inflammatory, antipyretic, analgesic, and potential antineoplastic properties.

S4682New

Loxoprofen

Loxoprofen is a non-steroidal anti-inflammatory drug in the propionic acid derivatives group.

S4609New

Diflunisal

Diflunisal is a difluorophenyl derivate of salicylic acid and a nonsteroidal anti-inflammatory drug (NSAID) with antipyretic, analgesic and anti-inflammatory properties. The mechanism of action of diflunisal is as a Cyclooxygenase Inhibitor.

S4656New

Parecoxib

Parecoxib is a selective COX2 inhibitor.

S4628New

(+/-)-Sulfinpyrazone

Sulfinpyrazone is one of the most studied platelet COX inhibitors, also a uricosuric agent that competitively inhibits uric acid reabsorption in kidney proximal tubules.

S4539New

Salicylic acid

Salicylic acid is a beta hydroxy acid that occurs as a natural compound in plants which is an inhibitor of ethylene biosynthesis and cyclooxygenase activity.

S4526New

Fenbufen

Fenbufen is an orally active phenylalkanoic derivative with anti-inflammatory, analgesic and antipyretic activity. It is a non-steroidal anti-inflammatory drug.

S3043

Rofecoxib

Rofecoxib is a COX-2 inhibitor with IC50 of 18 nM.

S1734

Meloxicam

Meloxicam is a selective COX inhibitor, used to relieve pain and fever effects.

S3023

Bufexamac

Bufexamac is a COX inhibitor for IFN-α release with EC50 of 8.9 μM.

S3017

Aspirin

Aspirin is a salicylate, and irreversible COX1 and COX2 inhibitor, used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication.

S1761

Suprofen

Suprofen is a dual COX-1/COX-2 inhibitor, used as a non-steroidal anti-inflammatory analgesic and antipyretic.

S1713

Piroxicam

Piroxicam is a non-selective COX inhibitor, used in the treatment of rheumatoid and osteoarthritis.

S1328

Etodolac

Etodolac is a nonsteroidal anti-inflammatory drug (NSAID) and a COX inhibitor, used for the treatment of inflammation and pain.

S1645

Ketoprofen

Ketoprofen is a dual COX1/2 inhibitor, used as a nonsteroidal anti-inflammatory drug to treat arthritis-related inflammatory pains.

S1903

Diclofenac Sodium

Diclofenac Sodium is a non-selective COX inhibitor with IC50 of 0.5 μg/ml and 0.5 μg/ml for COX-1 and -2 in intact cells, respectively, used as a nonsteroidal anti-inflammatory drug (NSAID) to relieve pain and reduce swelling in flammation.

S1518

Ibuprofen Lysine

Ibuprofen Lysine is a non-steroidal anti-inflammatory drug.

S2047

Lornoxicam

Lornoxicam is a non-steroidal COX-1/COX-2 inhibitor, used as an anti-inflammatory drug to treat pain, osteoarthritis, and rheumatoid arthritis.

S1646

Ketorolac

Ketorolac (Ketorolac tromethamine) is a non-selective COX inhibitor of COX-1 and COX-2 with IC50 of 1.23 μM and 3.50 μM, respectively.

S1626

Naproxen Sodium

Naproxen Sodium is a COX inhibitor for COX-1 and COX-2 with IC50 of 8.7 μM and 5.2 μM, respectively.

S2903

Lumiracoxib

Lumiracoxib is a novel, selective COX-2 inhibitor with IC50 and Ki of 0.14 μM and 0.06 μM, exhibits 515-fold selectivity over COX-1. Phase 4.

S2531

Asaraldehyde

Asaraldehyde is a natural COX-2 inhibitor, exhibiting 17-fold selectivity over COX-1.

S1960

Pranoprofen

Pranoprofen is a non-steroidal COX inhibitor, used as an anti-inflammatory drug in ophthalmology.

S3008

Zaltoprofen

Zaltoprofen is an inhibitor of Cox-1 and Cox-2 for treatment of arthritis.

S2602

Acemetacin

Acemetacin is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor.

S1959

Tolfenamic Acid

Tolfenamic Acid is a COX-2 inhibitor with IC50 of 0.2 μM.

S4049

Valdecoxib

Valdecoxib is a potent and selective inhibitor of COX-2 with IC50 of 5 nM.

S2577

Phenacetin

Phenacetin is a non-opioid analgesic without anti-inflammatory properties.

S2040

Nimesulide

Nimesulide is a relatively COX-2 selective inhibitor with IC50 of 26 μM.

S4149

Amfenac Sodium Monohydrate

Amfenac Sodium monohydrate is a non-steroidal analgesic anti-inflammatory drug with acetic acid moiety.

S4248

Bromfenac Sodium

Bromfenac Sodium is a nonsteroidal anti-inflammatory drug (NSAID), which has anti-inflammatory activity and may block prostaglandin synthesis by inhibiting cyclooxygenase 1 and 2.

S4051

Nabumetone

Nabumetone is a non-steroidal anti-inflammatory drug and its active metabolite inhibits the COX.

S3018

Niflumic acid

Niflumic acid is an inhibitor of cyclooxygenase-2 used for joint and muscular pain.

S4011

Ampiroxicam

Ampiroxicam is a nonselective cyclooxygenase inhibitor uesd as anti-inflammatory drug.

S4136

Carprofen

Carprofen inhibits canine COX2 with IC50 of 30 nM.

S4078

Mefenamic Acid

Mefenamic Acid is a competitive inhibitor of COX-1 and COX-2.

S4230

Oxaprozin

Oxaprozin is a non-narcotic, non-steroidal anti-inflammatory drug (NSAID) used to relieve the inflammation, swelling, stiffness, and joint pain associated with osteoarthritis and rheumatoid arthritis.

S7889

Xanthohumol

Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Phase 1.

S2108

Flunixin Meglumin

Flunixin Meglumin is a potent inhibitor of the enzyme cyclooxygenase used as analgesic agent with anti-inflammatory and antipyretic activity.

S4295

Meclofenamate Sodium

Meclofenamate Sodium is a dual COX-1/COX-2 inhibitor with IC50 of 40 nM and 50 nM, respectively, used in the treatment of joint, muscular pain, arthritis and dysmenorrhea.

Catalog No. Information Product Use Citations Product Validations
S1261

Celecoxib

Celecoxib is a selective COX-2 inhibitor with IC50 of 40 nM in Sf9 cells.

S1255

Nepafenac

Nepafenac is a prodrug of amfenac that acts as an inhibitor of COX-1 and COX-2 activity, used in the treatment of pain and inflammation associated with cataract surgery.

S1638

Ibuprofen

Ibuprofen (Dolgesic) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively.

S1723

Indomethacin

Indomethacin is a nonselective COX1 and COX2 inhibitor with IC50 of 0.1 μg/mL and 5 μg/mL, respectively, used to reduce fever, pain, stiffness, and swelling.

S2007

Sulindac

Sulindac is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions.

S8433New

NS-398 (NS398)

NS-398 is a selective inhibitor of cyclooxygenase-2 (COX-2). The IC50 values for human recombinant COX-1 and -2 are 75 and 1.77 μM, respectively.

S1634New

Acetaminophen

Acetaminophen is a COX inhibitor for COX-1 and COX-2 with IC50 of 113.7 μM and 25.8 μM, respectively.

S4686New

Vitamin E

Vitamin E is a fat-soluble vitamin with potent antioxidant properties. It is a potent peroxyl radical scavenger and inhibits noncompetitively cyclooxygenase activity in many tissues, also inhibits angiogenesis and tumor dormancy through suppressing vascular endothelial growth factor (VEGF) gene transcription.

S4651New

Etoricoxib

Etoricoxib is a new COX-2 selective inhibitor with anti-inflammatory, antipyretic, analgesic, and potential antineoplastic properties.

S4682New

Loxoprofen

Loxoprofen is a non-steroidal anti-inflammatory drug in the propionic acid derivatives group.

S4609New

Diflunisal

Diflunisal is a difluorophenyl derivate of salicylic acid and a nonsteroidal anti-inflammatory drug (NSAID) with antipyretic, analgesic and anti-inflammatory properties. The mechanism of action of diflunisal is as a Cyclooxygenase Inhibitor.

S4656New

Parecoxib

Parecoxib is a selective COX2 inhibitor.

S4628New

(+/-)-Sulfinpyrazone

Sulfinpyrazone is one of the most studied platelet COX inhibitors, also a uricosuric agent that competitively inhibits uric acid reabsorption in kidney proximal tubules.

S4539New

Salicylic acid

Salicylic acid is a beta hydroxy acid that occurs as a natural compound in plants which is an inhibitor of ethylene biosynthesis and cyclooxygenase activity.

S4526New

Fenbufen

Fenbufen is an orally active phenylalkanoic derivative with anti-inflammatory, analgesic and antipyretic activity. It is a non-steroidal anti-inflammatory drug.

S3043

Rofecoxib

Rofecoxib is a COX-2 inhibitor with IC50 of 18 nM.

S1734

Meloxicam

Meloxicam is a selective COX inhibitor, used to relieve pain and fever effects.

S3023

Bufexamac

Bufexamac is a COX inhibitor for IFN-α release with EC50 of 8.9 μM.

S3017

Aspirin

Aspirin is a salicylate, and irreversible COX1 and COX2 inhibitor, used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication.

S1761

Suprofen

Suprofen is a dual COX-1/COX-2 inhibitor, used as a non-steroidal anti-inflammatory analgesic and antipyretic.

S1713

Piroxicam

Piroxicam is a non-selective COX inhibitor, used in the treatment of rheumatoid and osteoarthritis.

S1328

Etodolac

Etodolac is a nonsteroidal anti-inflammatory drug (NSAID) and a COX inhibitor, used for the treatment of inflammation and pain.

S1645

Ketoprofen

Ketoprofen is a dual COX1/2 inhibitor, used as a nonsteroidal anti-inflammatory drug to treat arthritis-related inflammatory pains.

S1903

Diclofenac Sodium

Diclofenac Sodium is a non-selective COX inhibitor with IC50 of 0.5 μg/ml and 0.5 μg/ml for COX-1 and -2 in intact cells, respectively, used as a nonsteroidal anti-inflammatory drug (NSAID) to relieve pain and reduce swelling in flammation.

S1518

Ibuprofen Lysine

Ibuprofen Lysine is a non-steroidal anti-inflammatory drug.

S2047

Lornoxicam

Lornoxicam is a non-steroidal COX-1/COX-2 inhibitor, used as an anti-inflammatory drug to treat pain, osteoarthritis, and rheumatoid arthritis.

S1646

Ketorolac

Ketorolac (Ketorolac tromethamine) is a non-selective COX inhibitor of COX-1 and COX-2 with IC50 of 1.23 μM and 3.50 μM, respectively.

S1626

Naproxen Sodium

Naproxen Sodium is a COX inhibitor for COX-1 and COX-2 with IC50 of 8.7 μM and 5.2 μM, respectively.

S2903

Lumiracoxib

Lumiracoxib is a novel, selective COX-2 inhibitor with IC50 and Ki of 0.14 μM and 0.06 μM, exhibits 515-fold selectivity over COX-1. Phase 4.

S2531

Asaraldehyde

Asaraldehyde is a natural COX-2 inhibitor, exhibiting 17-fold selectivity over COX-1.

S1960

Pranoprofen

Pranoprofen is a non-steroidal COX inhibitor, used as an anti-inflammatory drug in ophthalmology.

S3008

Zaltoprofen

Zaltoprofen is an inhibitor of Cox-1 and Cox-2 for treatment of arthritis.

S2602

Acemetacin

Acemetacin is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor.

S1959

Tolfenamic Acid

Tolfenamic Acid is a COX-2 inhibitor with IC50 of 0.2 μM.

S4049

Valdecoxib

Valdecoxib is a potent and selective inhibitor of COX-2 with IC50 of 5 nM.

S2577

Phenacetin

Phenacetin is a non-opioid analgesic without anti-inflammatory properties.

S2040

Nimesulide

Nimesulide is a relatively COX-2 selective inhibitor with IC50 of 26 μM.

S4149

Amfenac Sodium Monohydrate

Amfenac Sodium monohydrate is a non-steroidal analgesic anti-inflammatory drug with acetic acid moiety.

S4248

Bromfenac Sodium

Bromfenac Sodium is a nonsteroidal anti-inflammatory drug (NSAID), which has anti-inflammatory activity and may block prostaglandin synthesis by inhibiting cyclooxygenase 1 and 2.

S4051

Nabumetone

Nabumetone is a non-steroidal anti-inflammatory drug and its active metabolite inhibits the COX.

S3018

Niflumic acid

Niflumic acid is an inhibitor of cyclooxygenase-2 used for joint and muscular pain.

S4011

Ampiroxicam

Ampiroxicam is a nonselective cyclooxygenase inhibitor uesd as anti-inflammatory drug.

S4136

Carprofen

Carprofen inhibits canine COX2 with IC50 of 30 nM.

S4078

Mefenamic Acid

Mefenamic Acid is a competitive inhibitor of COX-1 and COX-2.

S4230

Oxaprozin

Oxaprozin is a non-narcotic, non-steroidal anti-inflammatory drug (NSAID) used to relieve the inflammation, swelling, stiffness, and joint pain associated with osteoarthritis and rheumatoid arthritis.

S7889

Xanthohumol

Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Phase 1.

S2108

Flunixin Meglumin

Flunixin Meglumin is a potent inhibitor of the enzyme cyclooxygenase used as analgesic agent with anti-inflammatory and antipyretic activity.

S4295

Meclofenamate Sodium

Meclofenamate Sodium is a dual COX-1/COX-2 inhibitor with IC50 of 40 nM and 50 nM, respectively, used in the treatment of joint, muscular pain, arthritis and dysmenorrhea.