E0226New |
Chebulagic acid
|
Chebulagic acid, isolated form Terminalia chebula Retz, is a reversible and non-competitive inhibitor of maltase with a Ki value of 6.6 μM. Chebulagic acid shows potent anti-inflammatory effects in LPS-stimulated RAW 264.7 cells. Chebulagic acid also shows potent COX–LOX dual inhibition activity with IC50 values of 15 μM, 0.92 μM and 2.1 μM for COX-1, COX-2 and 5-LOX respectively.
|
|
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E0500New |
Firocoxib (ML 1785713)
|
Firocoxib (ML 1785713) is a cyclooxygenase (COX)-2 inhibitor and a nonsteroidal anti-inflammatory drug. In vitro firocoxib inhibits COX-1 and COX-2 with an IC50 of 7.5 mM and 0.13 mM respectively in feline blood. |
|
|
S0759 |
FPL 62064
|
FPL 62064 is a potent dual inhibitor of 5-lipoxygenase (5-LOX) and prostaglandin synthetase (cyclooxygenase, COX) with IC50 of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and seminal vesicle prostaglandin synthetase, respectively. FPL 62064 has potent anti-inflammatory activity. |
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S0761 |
Desmethyl Celecoxib
|
Desmethyl Celecoxib (compound 3b), an analog of Celecoxib with the optimal yield of 75%, is a selective inhibitor of cyclooxygenase-2 (COX-2) with anti-inflammatory activities. |
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S0766 |
RHC 80267
|
RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL, DAG lipase) with IC50 of 4 μM for cholinesterase activity. RHC 80267 inhibits cyclooxygenase (COX) activity, phospholipase C (PLC) activity and the hydrolysis of phosphatidylcholine (PC). |
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S0821 |
Pamicogrel
|
Pamicogrel (KBT3022) is an inhibitor of cyclooxygenase (COX) with platelet anti-aggregatory properties. |
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S0931 |
Jaceosidin
|
Jaceosidin, a flavonoid isolated from Artemisia vestita, possesses anti-tumor and anti-proliferative activities in many cancer cells. Jaceosidin induces apoptosis, activates Bax and down-regulates Mcl-1 and c-FLIP expression. Jaceosidin inhibits COX-2 expression and NF-κB activation. |
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S1204 |
Melatonin (NSC 113928)
|
Melatonin (NSC 113928, NSC 56423, N-Acetyl-5-methoxytryptamine) is a MT receptor agonist, used as a dietary supplement. Melatonin is a selective ATF-6 inhibitor and downregulates COX-2. Melatonin enhances mitophagy and regulates the homeostasis of apoptosis and autophagy. |
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Cell Chem Biol, 2021, S2451-9456(21)00442-6
-
Int J Mol Sci, 2021, 22(11)5649
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Int Immunopharmacol, 2021, 96:107787
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S1255 |
Nepafenac
|
Nepafenac (AHR 9434, AL 6515) 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. |
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Adv Sci (Weinh), 2020, 7(21):2001018
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S1261 |
Celecoxib (SC 58635)
|
Celecoxib (SC 58635) is a selective COX-2 inhibitor with IC50 of 40 nM in Sf9 cells. |
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Nat Commun, 2022, 13(1):1487
-
Hypertens Res, 2022, 10.1038/s41440-022-00889-1
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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S1328 |
Etodolac
|
Etodolac is a nonsteroidal anti-inflammatory drug (NSAID) and a COX inhibitor, used for the treatment of inflammation and pain. |
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Genome Med, 2021, 13(1):168
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|
S1396 |
Resveratrol (SRT501)
|
Resveratrol (SRT501, trans-Resveratrol) has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis. |
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Placenta, 2022, 122:56-65
-
Int Immunopharmacol, 2022, 103:108489
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Eur J Neurosci, 2022, 10.1111/ejn.15596
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S1518 |
Ibuprofen Lysine
|
Ibuprofen Lysine is a non-steroidal anti-inflammatory drug. |
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S1576 |
Sulfasalazine (NSC 667219)
|
Sulfasalazine (NSC 667219, Azulfidine, Salazopyrin, Sulphasalazine) is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy. |
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Cell Mol Life Sci, 2022, 79(5):228
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Front Bioeng Biotechnol, 2022, 10:855755
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Cell Metab, 2021, S1550-4131(21)00233-3
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S1626 |
Naproxen Sodium
|
Naproxen Sodium (RS-3650) is a COX inhibitor for COX-1 and COX-2 with IC50 of 8.7 μM and 5.2 μM, respectively. |
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Drug Metab Dispos, 2020, 48(8):613-621
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Adv Ther (Weinh), 2020, 2000034
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S1638 |
Ibuprofen (NSC 256857)
|
Ibuprofen (NSC 256857, Dolgesic) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively. |
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Immunity, 2020, 52(2):328-341
-
Anticancer Drugs, 2020, 31(1):27-34
-
Virol Sin, 2019, 34(6):648-661
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|
S1645 |
Ketoprofen
|
Ketoprofen (RP-19583) is a dual COX1/2 inhibitor, used as a nonsteroidal anti-inflammatory drug to treat arthritis-related inflammatory pains. |
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Signal Transduct Target Ther, 2022, 7(1):46
-
J Nucl Med, 2020, jnumed.120.249367
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S1646 |
Ketorolac
|
Ketorolac is a non-selective COX inhibitor of COX-1 and COX-2 with IC50 of 1.23 μM and 3.50 μM, respectively. |
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J Virol, 2020, 6;94(2):e01679-19
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Life Sci, 2020, 15;251:117604
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S1713 |
Piroxicam
|
Piroxicam (CP 16171) is a non-selective COX inhibitor, used in the treatment of rheumatoid and osteoarthritis. |
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S1723 |
Indomethacin (NSC-77541)
|
Indomethacin (NSC-77541, Indometacin) 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. |
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J Exp Clin Cancer Res, 2021, 40(1):344
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Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00738-w
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Front Endocrinol (Lausanne), 2021, 12:665145
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S1734 |
Meloxicam
|
Meloxicam is a selective COX inhibitor, used to relieve pain and fever effects. |
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J Oncol, 2022, 2022:4598573
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PLoS One, 2020, 13;15(3):e0230272
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Oncol Lett, 2017, 14(2):2198-2206
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S1761 |
Suprofen
|
Suprofen is a dual COX-1/COX-2 inhibitor, used as a non-steroidal anti-inflammatory analgesic and antipyretic. |
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S1903 |
Diclofenac Sodium
|
Diclofenac Sodium (GP 45840) 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. |
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Oxid Med Cell Longev, 2018, 2018:3692752
-
Arch Toxicol, 2018, 92(6):1953-1967
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Cell, 2016, 167(7):1803-1813
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S1959 |
Tolfenamic Acid
|
Tolfenamic Acid is a COX-2 inhibitor with IC50 of 0.2 μM. |
-
Hum Mol Genet, 2020, ddaa244
-
Front Microbiol, 2020, 10:2936
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Oncotarget, 2017, 8(57):96865-96884
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|
S1960 |
Pranoprofen
|
Pranoprofen (Pyranoprofen) is a non-steroidal COX inhibitor, used as an anti-inflammatory drug in ophthalmology. |
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Front Immunol, 2020, 11:534099
-
Mol Med Rep, 2017, 15(6):4305-4311
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S2007 |
Sulindac
|
Sulindac is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions. |
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Hum Cell, 2022, 10.1007/s13577-022-00671-y
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Hum Cell, 2021, 34(6):1911-1918
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Hum Cell, 2021, 10.1007/s13577-021-00639-4
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S2040 |
Nimesulide
|
Nimesulide is a relatively COX-2 selective inhibitor with IC50 of 26 μM. |
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Front Microbiol, 2020, 10:2936
-
Elife, 2016, 5e14653
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Viruses, 2015, 7(5):2268-87
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S2047 |
Lornoxicam
|
Lornoxicam (Chlortenoxicam) is a non-steroidal COX-1/COX-2 inhibitor, used as an anti-inflammatory drug to treat pain, osteoarthritis, and rheumatoid arthritis. |
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S2108 |
Flunixin Meglumin
|
Flunixin Meglumin is a potent inhibitor of the enzyme cyclooxygenase (COX) used as analgesic agent with anti-inflammatory and antipyretic activity. |
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S2121 |
Licofelone (ML3000)
|
Licofelone (ML3000, Compound 3e) is a dual inhibitor of COX and 5-lipoxygenase (5-LOX) with IC50 of 0.21 μM and 0.18 μM, respectively. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins. Licofelone is considered as a treatment for osteoarthritis. |
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Hum Mol Genet, 2020, ddaa244
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S2272 |
Indoprofen
|
Indoprofen is a nonsteroidal anti-inflammatory drug (NSAID) and cyclooxygenase (COX) inhibitor. Indoprofen prevents muscle wasting in aged mice through activation of PDK1/AKT pathway.Indoprofen selectively increases SMN2-luciferase reporter protein and endogenous SMN protein. |
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S2349 |
Rutaecarpine
|
Rutaecarpine (Rutecarpine) is an indolopyridoquinazolinone alkaloid isolated from Evodia rutaecarpa and related herbs; a new class of COX-2 inhibitor. |
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Theranostics, 2020, 10(8):3366-3381
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|
S2351 |
Salicin
|
Salicin (Salicoside, Salicine) is a phenol β-glycosid produced from willow bark that shows anti-inflammatory effects. It is a natural, non-selective COX-1 and COX-2 inhibitor. |
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Biochem Biophys Res Commun, 2019, 508(3):682-689
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S2410 |
Paeoniflorin (NSC 178886)
|
Paeoniflorin (NSC 178886) is a herbal constituent extracted from the root of Paeonia albiflora Pall. Paeoniflorin reduces COX-2 expression. Paeoniflorin alleviates liver fibrosis by inhibiting HIF-1α through mTOR-dependent pathway. |
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Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Hum Cell, 2021, 34(6):1911-1918
-
Hum Cell, 2021, 10.1007/s13577-021-00639-4
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S2531 |
Asaraldehyde
|
Asaraldehyde (Asaronaldehyde) is a natural COX-2 inhibitor, exhibiting 17-fold selectivity over COX-1. |
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S2577 |
Phenacetin
|
Phenacetin (Acetophenetidin) is a non-opioid analgesic without anti-inflammatory properties. |
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S2595 |
FK-3311
|
FK-3311 (COX-2 Inhibitor V) is a selective, cell-permeable and orally available inhibitor of cyclooxygenase-2 (COX-2) with antiinflammatory. FK-3311 has protective effects against hepatic warm ischemia-reperfusion injury by marked inhibition of TxA2. |
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S2602 |
Acemetacin
|
Acemetacin (K-708) is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor. |
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S2903 |
Lumiracoxib
|
Lumiracoxib (COX-189) is a novel, selective COX-2 inhibitor with Ki of 0.06 μM. It also inhibits COX1 with Ki of 3 μM. |
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Int J Biol Macromol, 2021, 187:603-613
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Cells, 2020, 9(9)E2005
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J Am Heart Assoc, 2020, 9(1):e013470
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S2995 |
4-Hydroxyphenylpyruvic acid
|
4-Hydroxyphenylpyruvic acid (4-HPPA), an abundant colon metabolite of polyphenols, is a potent scavenger that suppresses levels of free radicals and cyclooxygenase-2 (COX-2) and contributes to reduced risk of colon cancer development. |
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S3008 |
Zaltoprofen
|
Zaltoprofen is an inhibitor of COX-1 and COX-2 for treatment of arthritis. |
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S3017 |
Aspirin (NSC 27223)
|
Aspirin (NSC 27223, Acetylsalicylic acid, ASA) 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. Aspirin induces autophagy and stimulates mitophagy. |
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Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Dev Cell, 2021, S1534-5807(21)00485-8
-
Pigment Cell Melanoma Res, 2021, 10.1111/pcmr.13021
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|
S3018 |
Niflumic acid
|
Niflumic acid is an inhibitor of cyclooxygenase-2 used for joint and muscular pain. |
-
Oncol Lett, 2020, 20(4):39
|
|
S3023 |
Bufexamac
|
Bufexamac is a COX inhibitor for IFN-α release with EC50 of 8.9 μM. |
-
Int J Mol Sci, 2021, 22(9)4559
-
Reprod Sci, 2021, 10.1007/s43032-021-00533-2
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Autophagy, 2016, 12(10):1738-1758
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|
S3043 |
Rofecoxib
|
Rofecoxib (MK-0966) is a COX-2 inhibitor with IC50 of 18 nM. |
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Toxicol Appl Pharmacol, 2015, 285(1):51-60
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|
S3063 |
Diclofenac Diethylamine
|
Diclofenac diethylamine is a nonsteroidal anti-inflammatory drug taken to reduce inflammation and as an analgesic reducing pain in certain conditions. Diclofenac exerts its action via inhibition of prostaglandin synthesis by inhibiting cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) with relative equipotency. |
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S3168 |
cis-Resveratrol
|
cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively. |
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S3173 |
Antipyrine
|
Antipyrine (Phenazone) is an analgesic and antipyretic agent; selective COX-3 inhibitor. |
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|
S3200 |
Triflusal
|
Triflusal (UR1501) irreversibly inhibits the production of thromboxane-B2 in platelets by acetylating cycloxygenase-1. |
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J Am Heart Assoc, 2020, 9(1):e013470
|
|
S3255 |
Pectolinarigenin
|
Pectolinarigenin, an active anti-inflammatory ingredient in Cirsium chanroenicum, is a dual inhibitor of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX). |
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S3261 |
Myrislignan
|
Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan inhibits interleukin-6 (IL-6) and tumour necrosis factor-α (TNF-α). Myrislignan significantly inhibits the expressions of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2) dose-dependently in LPS-stimulated macrophage cells. Myrislignan inhibits the NF-κB signalling pathway activation. |
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|
S3283 |
Marmesin
|
Marmesin (S-(+)-Marmesin, (+)-Marmesin, (S)-Marmesin) is a natural coumarin with COX-2 and 5-LOX dual inhibitory activity. |
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S3304 |
Stylopine
|
Stylopine ((R,S)-Stylopine, Tetrahydrocoptisine) reduces nitric oxide (NO), prostaglandin E2 (PGE2), tumor necrosis factor-alpha (TNF-alpha) and interleukin-1beta (IL-1beta), and the IL-6 production and cyclooxygenase-2 (COX-2) activity caused by the LPS stimulation. Stylopine is a major component of the leaf of Chelidonium majus L. |
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S3816 |
Dehydroevodiamine
|
Dehydroevodiamine (DHED), a constituent of Evodia rutaecarpa, has various biological effects such as hypotensive, negative chronotropic, ion channel depressant, inhibition of nitric oxide production and cerebral blood flow enhancing activities. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells. |
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S3872 |
Guaiacol
|
Guaiacol (O-methoxyphenol, 2-hydroxyanisole, O-methylcatechol) is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. It is a precursor to various flavorants, such as eugenoland vanillin. Guaiacol, a phenolic compound isolated from Guaiac resin, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity. |
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S3899 |
Hederagenin
|
Hederagenin (Caulosapogenin, Hederagenol, Hederagenic acid, Astrantiagenin E) is a highly water insoluble triterpenoid compound that can be found in various plants including Hedera helix and Chenopodium quinoa. It exhibits a variety of biological activities, including potent antitumor properties both in vitro and in vivo. Hederagenin inhibits LPS-stimulated expression of iNOS, COX-2, and NF-κB. |
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S3925 |
(-)-Epicatechin gallate
|
(-)-Epicatechin gallate (ECG) is an inhibitor of cyclooxygenase-1 (COX-1) with IC50 of 7.5 μM. |
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Cell Death Dis, 2018, 9(2):205
-
PLoS One, 2018, 13(10):e0205123
-
J Fish Dis, 2018, 10.1111/jfd.12819
|
|
S3931 |
Ginsenoside Rd
|
Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively. |
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J Ethnopharmacol, 2021, S0378-8741(21)00169-0
|
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S3969 |
Veratric acid
|
Veratric acid (3,4-Dimethoxybenzoic acid), a simple benzoic acid derived from plants and fruits, has anti-oxidant, anti-inflammation, and blood pressure-lowering effects. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation. |
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S3974 |
(+)-Catechin hydrate
|
Catechins are a plant derived polyphenolic anti-oxidants with phytotoxic properties. (+)-Catechin hydrate is a frequent component of traditional herbal remedies, such as Uncaria rhynchophylla. (+)-Catechin hydrate inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM. |
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J Steroid Biochem Mol Biol, 2021, 211:105906
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S4011 |
Ampiroxicam
|
Ampiroxicam (CP 65703) is a nonselective cyclooxygenase inhibitor uesd as anti-inflammatory drug. |
|
|
S4028 |
Dexamethasone Sodium Phosphate
|
Dexamethasone (Dexamethasone 21-phosphate disodium salt) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. |
-
Pharmaceutics, 2022, 14(2)400
-
Dis Model Mech, 2022, dmm.049109
-
Hematology, 2022, 27(1):32-42
|
|
S4032 |
Bismuth Subsalicylate
|
Bismuth Subsalicylate is the active ingredient in Pepto-Bismol and inhibits prostaglandin G/H Synthase 1/2. |
|
|
S4049 |
Valdecoxib
|
Valdecoxib is a potent and selective inhibitor of COX-2 with IC50 of 5 nM. |
-
Cancer Cell, 2022, S1535-6108(21)00662-0
-
Cell Rep, 2022, 38(10):110490
-
Biochem Bioph Res Co, 2015, 460(2):198-204
|
|
S4051 |
Nabumetone
|
Nabumetone (BRL-14777) is a non-steroidal anti-inflammatory drug and its active metabolite inhibits the COX. |
|
|
S4078 |
Mefenamic Acid
|
Mefenamic Acid (CI 473, CN-35355) is a competitive inhibitor of COX-1 and COX-2. |
-
Am J Physiol Renal Physiol, 2022, 10.1152/ajprenal.00568.2020
-
Brain Res, 2020, 20;1740:146846
|
|
S4136 |
Carprofen
|
Carprofen inhibits canine COX2 with IC50 of 30 nM. |
|
|
S4149 |
Amfenac Sodium Monohydrate
|
Amfenac Sodium monohydrate is a non-steroidal analgesic anti-inflammatory drug with acetic acid moiety. The IC50 values for COX1 and COX2 is 250 nM and 150 nM, respectively. |
|
|
S4176 |
Trometamol
|
Trometamol is a proton acceptor used to treat acidemia. It inhibits both isoforms of cyclooxygenases (COX1 and COX2), thereby blocking the conversion of arachidonic acid to pro-inflammatory pro-prostaglandins. |
|
|
S4230 |
Oxaprozin
|
Oxaprozin (WY-21743) 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. |
|
|
S4248 |
Bromfenac Sodium
|
Bromfenac Sodium (AHR 10282R) is a nonsteroidal anti-inflammatory drug (NSAID), which has anti-inflammatory activity and may block prostaglandin synthesis by inhibiting cyclooxygenase 1 and 2. |
|
|
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. Meclofenamate Sodium is a non-selective gap-junction blocker and a highly selective inhibitor of fat mass and obesity-associated (FTO) enzyme inhibitor. |
-
Front Oncol, 2022, 12:817584
-
Nature, 2019, 573(7775):539-545
|
|
S4360 |
Tolmetin Sodium
|
Tolmetin is a non-steroidal anti-inflammatory drug of the arylalkanoic acids. Tolmetin sodium dihydrate is a non-steroidal antiinflammatory agent, and acts as a non-selective COX inhibitor. |
|
|
S4435 |
Metamizole sodium hydrate
|
Metamizole (Dipyrone) sodium hydrate is a potent inhitior of cyclooxygenase (COX) with strong analgesic as well as antipyretic and spasmolytic properties. |
|
|
S4509 |
4-Aminoantipyrine
|
4-Aminoantipyrine(Ampyrone) is a metabolite of aminopyrine with analgesic, anti-inflammatory, and antipyretic properties. It is used as a reagent for biochemical reactions producing peroxides or phenols. |
|
|
S4526 |
Fenbufen
|
Fenbufen (Lederfen, CL-82204) is an orally active phenylalkanoic derivative with anti-inflammatory, analgesic and antipyretic activity. It is a non-steroidal anti-inflammatory drug. |
-
Gastroenterology, 2019, 10.1053/j
|
|
S4539 |
Salicylic acid
|
Salicylic acid (2-Hydroxybenzoic acid) is a beta hydroxy acid that occurs as a natural compound in plants which is an inhibitor of ethylene biosynthesis and cyclooxygenase activity. |
|
|
S4609 |
Diflunisal
|
Diflunisal (Dolobid, Dolobis, Flovacil, Fluniget) 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. |
|
|
S4628 |
(+/-)-Sulfinpyrazone
|
Sulfinpyrazone (G-28315, NSC 75925) is one of the most studied platelet COX inhibitors, also a uricosuric agent that competitively inhibits uric acid reabsorption in kidney proximal tubules. |
-
Cell Chem Biol, 2021, S2451-9456(21)00442-6
|
|
S4651 |
Etoricoxib
|
Etoricoxib (Arcoxia, MK-663, MK-0663, Tauxib, Algix, Nucoxia) is a new COX-2 selective inhibitor with anti-inflammatory, antipyretic, analgesic, and potential antineoplastic properties. |
-
Virol Sin, 2019, 34(6):648-661
|
|
S4656 |
Parecoxib
|
Parecoxib (SC-69124, Valus-P, Vorth-P) is a selective COX2 inhibitor. |
-
Theranostics, 2020, 10(8):3366-3381
|
|
S4686 |
Vitamin E
|
Vitamin E (D-alpha-Tocopherol) 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. |
-
Bone Res, 2022, 10(1):26
-
EMBO Mol Med, 2022, 14(2):e14903
-
Biosci Biotechnol Biochem, 2020, 18;1-8
|
|
S4765 |
Syringaldehyde
|
Syringaldehyde (Syringic aldehyde) is an organic compound that occurs naturally in trace amounts. It possesses worthy bioactive properties and is, therefore, used in pharmaceuticals, food, cosmetics, textiles, pulp and paper industries, and even in biological control applications. Syringaldehyde is a polyphenolic compound belonging to the group of flavonoids and is found in different plant species like Manihot esculenta and Magnolia officinalis. Syringaldehyde moderately inhibits COX-2 activity with an IC50 of 3.5 μg/mL[2]. Anti-hyperglycemic and anti-inflammatory activities. |
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S5010 |
Indometacin Sodium
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Indometacin Sodium (Indomethacin Sodium) is the sodium salt of indomethacin, which is a non-selective, reversible, and competitive inhibitor of cyclooxygenases 1 and 2 with anti-inflammatory, analgesic-antipyretic and tocolytic effects. |
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J Exp Clin Cancer Res, 2021, 40(1):344
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Mol Cell, 2020, 80(3):525-540.e9
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Mol Cancer Ther, 2020, 19;molcanther00152020
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S5019 |
Indobufen
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Indobufen (Ibustrin, K 3920) is a reversible platelet aggregation inhibitor. Indobufen is a reversible inhibitor of platelet cyclooxygenase (Cox) activity and suppresses thromboxane synthesis. |
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S5177 |
Naproxen
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Naproxen is an anti-inflammatory agent with analgesic and antipyretic properties. It is a nonselective inhibitor of COX-1 and COX-2. |
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Drug Metab Dispos, 2020, 48(8):613-621
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Biogerontology, 2016, 17(5-6):907-920
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S5192 |
S-(+)-Ketoprofen
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S-(+)-Ketoprofen (Compound 1, Actron, (S)-Ketoprofen, Dexketoprofen) is a potent inhibitor of cyclooxygenase (COX) with IC50 of 1.9 nM and 27 nM for COX-1 and COX-2, respectively. |
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S5309 |
Propyphenazone (4-Isopropylantipyrine)
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Propyphenazone(4-Isopropylantipyrine, Isopropyrine), an analgesic and antipyretic agent, is a selective cyclooxygenase-2 inhibitor with anti-inflammatory activity. |
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S5418 |
Parecoxib Sodium
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Parecoxib Sodium (SC-69124) is a water-soluble, injectable sodium salt form of parecoxib, which is a potent and selective inhibitor of cyclo-oxygenase-2 (COX2). |
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S5520 |
Phenidone
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Phenidone (1-phenyl-3-pyrazolidinone), a dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), is an organic compound that is primarily used as a photographic developer. |
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S5551 |
6-Paradol
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6-Paradol is a minor constituent of ginger, mainly formed from 6-gingerol via 6-shogaol, and exhibits a variety of biological activities including anti-cancer, anti-inflammatory, and anti-oxidative activities. Paradol is an inhibitor of cyclooxygenase (COX)-2. |
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S5595 |
3-Carene
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3-Carene (Carene, Delta-3-Carene) is a bicyclic monoterpene in essential oils extracted from pine trees. 3-Carene have potent pharmacological effects on COX-2 overexpression and LPS-induced migration of Raw264.7 macrophages. 3‐carene is shown to significantly stimulate the activity and expression of alkaline phosphatase, an early phase marker of osteoblastic differentiation. |
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Phytomedicine, 2021, 91:153707
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S5640 |
Ethyl caffeate
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Ethyl caffeate, a naturally occurring compound found in Bidens pilosa, suppresses NF-kappaB activation and its downstream inflammatory mediators, iNOS, COX-2 and PGE2 in vitro. |
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S5698 |
Ketorolac tromethamine salt
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Ketorolac tromethamine is a synthetic pyrrolizine carboxylic acid derivative with anti-inflammatory, analgesic and antipyretic properties. It is a non-selective COX inhibitor with IC50s of 20 nM for both COX-1 and COX-2. |
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Front Immunol, 2021, 12:616402
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S5711 |
Deracoxib
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Deracoxib (SC-046) is a COX-2 inhibitor with >48-fold selectivity over COX-1. It also exhibits inhibitory activity against phosphodiesterase (Ki = 3.6 μM against human PDE4D3). |
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S5786 |
Bromfenac sodium hydrate
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Bromfenac sodium hydrate (Bromsite, Bromday, Prolensa, Xibrom), a brominated nonsteroidal anti-inflammatory drugs (NSAID) with strong in vitro anti-inflammatory potency, is a potent and orally active inhibitor of COX with IC50 of 5.56 nM and 7.45 nM for COX-1 and COX-2, respectively. |
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S6073 |
Diclofenac acid
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Diclofenac acid is a nonsteroidal anti-inflammatory drug that has analgesic, anti-inflammatory, and antipyretic properties, and has been shown to be effective in treating a variety of acute and chronic pain and inflammatory conditions. It inhibits cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) with relative equipotency. |
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S6457 |
Flurbiprofen Axetil
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Flurbiprofen Axetil is one of the commonly used nonsteroidal anti-inflammatory drugs (NSAIDs) that nonselectively inhibits cyclooxygenase. |
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S6615 |
ATB 346
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ATB 346, a novel hydrogen sulphide-releasing derivative of naproxen with remarkably reduced toxicity, inhibits COX activity. ATB 346 is an anti-inflammatory agent that induces apoptosis of human melanoma cells. |
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S6685 |
Mavacoxib
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Mavacoxib (Trocoxil) is a selective, long-acting cyclooxygenase-2 (COX-2) inhibitor. Mavacoxib is a novel nonsteroidal anti-inflammatory drug (NSAID). |
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S6686 |
SC-560
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SC-560 is a highly selective COX-1 inhibitor with IC50 of 9 nM, compared with the IC50 of 6.3 μM for COX-2, nearly 1,000-fold higher than with COX-1. |
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S6780 |
TFAP
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TFAP (N-(5-Aminopyridin-2-yl)-4-(trifluoromethyl)benzamide) is a selective and cell-permeable cyclooxygenase-1 (COX-1) inhibitor with IC50 of 0.8 μM. |
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S6850 |
NE 52-QQ57
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NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with NE 52-QQ57 significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2). |
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S7889 |
Xanthohumol
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Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Xanthohumol inhibits diacylglycerol acyltransferase 1 (DGAT1) and DGAT2 with both IC50 of 40 μM. Xanthohumol is also a potent antiviral agent against a series of DNA and RNA viruses. Xanthohumol induces growth inhibition and apoptosis in cancer cells. Phase 1. |
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Oxid Med Cell Longev, 2022, 2022:9523491
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Int J Mol Sci, 2021, 22(22)12134
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J-Cancer, 2020, 6;11-14-:4047-4058
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S8433 |
NS-398 (NS398)
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NS-398 (N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide) 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. |
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PLoS Negl Trop Dis, 2022, 16(4):e0010402
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Mol Oncol, 2021, 10.1002/1878-0261.13077
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Oxid Med Cell Longev, 2021, 2021:7394344
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S9029 |
Prim-o-glucosylcimifugin
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Prim-O-glucosylcimifugin (Cimifugin beta-D-glucopyranoside, Cimifugin 7-glucoside) is a major constituent in Radix Saposhnikovia that has been long used for the treatment of pyrexia, rheumatism, and cancer in traditional Chinese medicine. It shows potential anticancer activity. Prim-O-glucosylcimifugin downregulates the mRNA and protein expression inducible NO synthase (iNOS) and cyclooxygenase 2 (COX-2) in LPS-activated RAW 264.7 macrophages in a concentration-dependent manner. |
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S9149 |
Benzoylpaeoniflorin
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Benzoylpaeoniflorin, a natural product isolated from Chinese paeony root, could inhibit COX-1 and COX-2 in vitro. |
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S9190 |
Oroxin B
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Oroxin B (Hypocretin-2), one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer.COX-2, VEGF, PI3K, and p-AKT expression levels are downregulated, while PTEN is upregulated after Oroxin B treatment. |
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Theranostics, 2022, 12(2):910-928
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J Cancer, 2021, 12(7):2140-2150
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S9208 |
Ginsenoside Rb3
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Ginsenoside Rb3, extracted from the plant Panax ginseng, plays important roles in cardiovascular diseases, including myocardial ischemia-reperfusion (I/R) injury. Ginsenoside Rb3 (0.1-10 μM) is tested for inhibition of tumor necrosis factor-α (TNF)-induced nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) luciferase reporter activity using a human kidney 293T cell-based assay. Ginsenoside Rb3 shows the significant activity with an IC50 of 8.2 μM. Ginsenoside Rb3 also inhibits the induction of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) messenger Ribonucleic acid (mRNA) in a dose-dependent manner after HepG2 cells have been treated with TNF-α (10 ng/mL). |
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S9236 |
α-Cyperone
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α-Cyperone (alpha-cyperone), a major active compound of Cyperus rotundus, exhibits biological activities, such as antivirulence, antigenotoxic, and antibacterial activities. α-Cyperone (alpha-cyperone) is associated with the down-regulation of COX-2, IL-6, Nck-2, Cdc42 and Rac1. |
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S9386 |
Polygalacic acid
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Polygalacic acid is the triterpenoid tetrahydroxyacid isolated from Polygala paenea L.. Polygalacic acid (0-100 μM; 24 hours) significantly decreases the mRNAexpressions of MMP-3, MMP-9, MMP-13 and COX-2, which are significantly increased by IL-1β, in a dose-dependent manner. |
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S9502 |
Madecassic acid
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Madecassic acid (Brahmic acid), a natural triterpene first isolated from C. asiatica, has diverse anti-inflammatory and anti-diabetic effects, blocking NF-κB activation in macrophages and causing by iNOS, COX-2, TNF-alpha, IL-1beta and IL-6 inhibition. |
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E0226New |
Chebulagic acid
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Chebulagic acid, isolated form Terminalia chebula Retz, is a reversible and non-competitive inhibitor of maltase with a Ki value of 6.6 μM. Chebulagic acid shows potent anti-inflammatory effects in LPS-stimulated RAW 264.7 cells. Chebulagic acid also shows potent COX–LOX dual inhibition activity with IC50 values of 15 μM, 0.92 μM and 2.1 μM for COX-1, COX-2 and 5-LOX respectively.
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E0500New |
Firocoxib (ML 1785713)
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Firocoxib (ML 1785713) is a cyclooxygenase (COX)-2 inhibitor and a nonsteroidal anti-inflammatory drug. In vitro firocoxib inhibits COX-1 and COX-2 with an IC50 of 7.5 mM and 0.13 mM respectively in feline blood. |
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S0759 |
FPL 62064
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FPL 62064 is a potent dual inhibitor of 5-lipoxygenase (5-LOX) and prostaglandin synthetase (cyclooxygenase, COX) with IC50 of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and seminal vesicle prostaglandin synthetase, respectively. FPL 62064 has potent anti-inflammatory activity. |
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S0761 |
Desmethyl Celecoxib
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Desmethyl Celecoxib (compound 3b), an analog of Celecoxib with the optimal yield of 75%, is a selective inhibitor of cyclooxygenase-2 (COX-2) with anti-inflammatory activities. |
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S0766 |
RHC 80267
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RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL, DAG lipase) with IC50 of 4 μM for cholinesterase activity. RHC 80267 inhibits cyclooxygenase (COX) activity, phospholipase C (PLC) activity and the hydrolysis of phosphatidylcholine (PC). |
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S0821 |
Pamicogrel
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Pamicogrel (KBT3022) is an inhibitor of cyclooxygenase (COX) with platelet anti-aggregatory properties. |
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S0931 |
Jaceosidin
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Jaceosidin, a flavonoid isolated from Artemisia vestita, possesses anti-tumor and anti-proliferative activities in many cancer cells. Jaceosidin induces apoptosis, activates Bax and down-regulates Mcl-1 and c-FLIP expression. Jaceosidin inhibits COX-2 expression and NF-κB activation. |
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S1204 |
Melatonin (NSC 113928)
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Melatonin (NSC 113928, NSC 56423, N-Acetyl-5-methoxytryptamine) is a MT receptor agonist, used as a dietary supplement. Melatonin is a selective ATF-6 inhibitor and downregulates COX-2. Melatonin enhances mitophagy and regulates the homeostasis of apoptosis and autophagy. |
- Cell Chem Biol, 2021, S2451-9456(21)00442-6
- Int J Mol Sci, 2021, 22(11)5649
- Int Immunopharmacol, 2021, 96:107787
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S1255 |
Nepafenac
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Nepafenac (AHR 9434, AL 6515) 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. |
- Adv Sci (Weinh), 2020, 7(21):2001018
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S1261 |
Celecoxib (SC 58635)
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Celecoxib (SC 58635) is a selective COX-2 inhibitor with IC50 of 40 nM in Sf9 cells. |
- Nat Commun, 2022, 13(1):1487
- Hypertens Res, 2022, 10.1038/s41440-022-00889-1
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
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S1328 |
Etodolac
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Etodolac is a nonsteroidal anti-inflammatory drug (NSAID) and a COX inhibitor, used for the treatment of inflammation and pain. |
- Genome Med, 2021, 13(1):168
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S1396 |
Resveratrol (SRT501)
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Resveratrol (SRT501, trans-Resveratrol) has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis. |
- Placenta, 2022, 122:56-65
- Int Immunopharmacol, 2022, 103:108489
- Eur J Neurosci, 2022, 10.1111/ejn.15596
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S1518 |
Ibuprofen Lysine
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Ibuprofen Lysine is a non-steroidal anti-inflammatory drug. |
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S1576 |
Sulfasalazine (NSC 667219)
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Sulfasalazine (NSC 667219, Azulfidine, Salazopyrin, Sulphasalazine) is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy. |
- Cell Mol Life Sci, 2022, 79(5):228
- Front Bioeng Biotechnol, 2022, 10:855755
- Cell Metab, 2021, S1550-4131(21)00233-3
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S1626 |
Naproxen Sodium
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Naproxen Sodium (RS-3650) is a COX inhibitor for COX-1 and COX-2 with IC50 of 8.7 μM and 5.2 μM, respectively. |
- Drug Metab Dispos, 2020, 48(8):613-621
- Adv Ther (Weinh), 2020, 2000034
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S1638 |
Ibuprofen (NSC 256857)
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Ibuprofen (NSC 256857, Dolgesic) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively. |
- Immunity, 2020, 52(2):328-341
- Anticancer Drugs, 2020, 31(1):27-34
- Virol Sin, 2019, 34(6):648-661
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S1645 |
Ketoprofen
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Ketoprofen (RP-19583) is a dual COX1/2 inhibitor, used as a nonsteroidal anti-inflammatory drug to treat arthritis-related inflammatory pains. |
- Signal Transduct Target Ther, 2022, 7(1):46
- J Nucl Med, 2020, jnumed.120.249367
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S1646 |
Ketorolac
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Ketorolac is a non-selective COX inhibitor of COX-1 and COX-2 with IC50 of 1.23 μM and 3.50 μM, respectively. |
- J Virol, 2020, 6;94(2):e01679-19
- Life Sci, 2020, 15;251:117604
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S1713 |
Piroxicam
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Piroxicam (CP 16171) is a non-selective COX inhibitor, used in the treatment of rheumatoid and osteoarthritis. |
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S1723 |
Indomethacin (NSC-77541)
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Indomethacin (NSC-77541, Indometacin) 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. |
- J Exp Clin Cancer Res, 2021, 40(1):344
- Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00738-w
- Front Endocrinol (Lausanne), 2021, 12:665145
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S1734 |
Meloxicam
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Meloxicam is a selective COX inhibitor, used to relieve pain and fever effects. |
- J Oncol, 2022, 2022:4598573
- PLoS One, 2020, 13;15(3):e0230272
- Oncol Lett, 2017, 14(2):2198-2206
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S1761 |
Suprofen
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Suprofen is a dual COX-1/COX-2 inhibitor, used as a non-steroidal anti-inflammatory analgesic and antipyretic. |
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S1903 |
Diclofenac Sodium
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Diclofenac Sodium (GP 45840) 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. |
- Oxid Med Cell Longev, 2018, 2018:3692752
- Arch Toxicol, 2018, 92(6):1953-1967
- Cell, 2016, 167(7):1803-1813
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S1959 |
Tolfenamic Acid
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Tolfenamic Acid is a COX-2 inhibitor with IC50 of 0.2 μM. |
- Hum Mol Genet, 2020, ddaa244
- Front Microbiol, 2020, 10:2936
- Oncotarget, 2017, 8(57):96865-96884
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S1960 |
Pranoprofen
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Pranoprofen (Pyranoprofen) is a non-steroidal COX inhibitor, used as an anti-inflammatory drug in ophthalmology. |
- Front Immunol, 2020, 11:534099
- Mol Med Rep, 2017, 15(6):4305-4311
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S2007 |
Sulindac
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Sulindac is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions. |
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Hum Cell, 2021, 34(6):1911-1918
- Hum Cell, 2021, 10.1007/s13577-021-00639-4
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S2040 |
Nimesulide
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Nimesulide is a relatively COX-2 selective inhibitor with IC50 of 26 μM. |
- Front Microbiol, 2020, 10:2936
- Elife, 2016, 5e14653
- Viruses, 2015, 7(5):2268-87
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S2047 |
Lornoxicam
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Lornoxicam (Chlortenoxicam) is a non-steroidal COX-1/COX-2 inhibitor, used as an anti-inflammatory drug to treat pain, osteoarthritis, and rheumatoid arthritis. |
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S2108 |
Flunixin Meglumin
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Flunixin Meglumin is a potent inhibitor of the enzyme cyclooxygenase (COX) used as analgesic agent with anti-inflammatory and antipyretic activity. |
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S2121 |
Licofelone (ML3000)
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Licofelone (ML3000, Compound 3e) is a dual inhibitor of COX and 5-lipoxygenase (5-LOX) with IC50 of 0.21 μM and 0.18 μM, respectively. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins. Licofelone is considered as a treatment for osteoarthritis. |
- Hum Mol Genet, 2020, ddaa244
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S2272 |
Indoprofen
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Indoprofen is a nonsteroidal anti-inflammatory drug (NSAID) and cyclooxygenase (COX) inhibitor. Indoprofen prevents muscle wasting in aged mice through activation of PDK1/AKT pathway.Indoprofen selectively increases SMN2-luciferase reporter protein and endogenous SMN protein. |
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S2349 |
Rutaecarpine
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Rutaecarpine (Rutecarpine) is an indolopyridoquinazolinone alkaloid isolated from Evodia rutaecarpa and related herbs; a new class of COX-2 inhibitor. |
- Theranostics, 2020, 10(8):3366-3381
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S2351 |
Salicin
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Salicin (Salicoside, Salicine) is a phenol β-glycosid produced from willow bark that shows anti-inflammatory effects. It is a natural, non-selective COX-1 and COX-2 inhibitor. |
- Biochem Biophys Res Commun, 2019, 508(3):682-689
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S2410 |
Paeoniflorin (NSC 178886)
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Paeoniflorin (NSC 178886) is a herbal constituent extracted from the root of Paeonia albiflora Pall. Paeoniflorin reduces COX-2 expression. Paeoniflorin alleviates liver fibrosis by inhibiting HIF-1α through mTOR-dependent pathway. |
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Hum Cell, 2021, 34(6):1911-1918
- Hum Cell, 2021, 10.1007/s13577-021-00639-4
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S2531 |
Asaraldehyde
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Asaraldehyde (Asaronaldehyde) is a natural COX-2 inhibitor, exhibiting 17-fold selectivity over COX-1. |
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S2577 |
Phenacetin
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Phenacetin (Acetophenetidin) is a non-opioid analgesic without anti-inflammatory properties. |
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S2595 |
FK-3311
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FK-3311 (COX-2 Inhibitor V) is a selective, cell-permeable and orally available inhibitor of cyclooxygenase-2 (COX-2) with antiinflammatory. FK-3311 has protective effects against hepatic warm ischemia-reperfusion injury by marked inhibition of TxA2. |
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S2602 |
Acemetacin
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Acemetacin (K-708) is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor. |
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S2903 |
Lumiracoxib
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Lumiracoxib (COX-189) is a novel, selective COX-2 inhibitor with Ki of 0.06 μM. It also inhibits COX1 with Ki of 3 μM. |
- Int J Biol Macromol, 2021, 187:603-613
- Cells, 2020, 9(9)E2005
- J Am Heart Assoc, 2020, 9(1):e013470
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S2995 |
4-Hydroxyphenylpyruvic acid
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4-Hydroxyphenylpyruvic acid (4-HPPA), an abundant colon metabolite of polyphenols, is a potent scavenger that suppresses levels of free radicals and cyclooxygenase-2 (COX-2) and contributes to reduced risk of colon cancer development. |
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S3008 |
Zaltoprofen
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Zaltoprofen is an inhibitor of COX-1 and COX-2 for treatment of arthritis. |
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S3017 |
Aspirin (NSC 27223)
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Aspirin (NSC 27223, Acetylsalicylic acid, ASA) 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. Aspirin induces autophagy and stimulates mitophagy. |
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Dev Cell, 2021, S1534-5807(21)00485-8
- Pigment Cell Melanoma Res, 2021, 10.1111/pcmr.13021
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S3018 |
Niflumic acid
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Niflumic acid is an inhibitor of cyclooxygenase-2 used for joint and muscular pain. |
- Oncol Lett, 2020, 20(4):39
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S3023 |
Bufexamac
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Bufexamac is a COX inhibitor for IFN-α release with EC50 of 8.9 μM. |
- Int J Mol Sci, 2021, 22(9)4559
- Reprod Sci, 2021, 10.1007/s43032-021-00533-2
- Autophagy, 2016, 12(10):1738-1758
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S3043 |
Rofecoxib
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Rofecoxib (MK-0966) is a COX-2 inhibitor with IC50 of 18 nM. |
- Toxicol Appl Pharmacol, 2015, 285(1):51-60
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S3063 |
Diclofenac Diethylamine
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Diclofenac diethylamine is a nonsteroidal anti-inflammatory drug taken to reduce inflammation and as an analgesic reducing pain in certain conditions. Diclofenac exerts its action via inhibition of prostaglandin synthesis by inhibiting cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) with relative equipotency. |
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S3168 |
cis-Resveratrol
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cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively. |
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S3173 |
Antipyrine
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Antipyrine (Phenazone) is an analgesic and antipyretic agent; selective COX-3 inhibitor. |
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S3200 |
Triflusal
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Triflusal (UR1501) irreversibly inhibits the production of thromboxane-B2 in platelets by acetylating cycloxygenase-1. |
- J Am Heart Assoc, 2020, 9(1):e013470
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S3255 |
Pectolinarigenin
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Pectolinarigenin, an active anti-inflammatory ingredient in Cirsium chanroenicum, is a dual inhibitor of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX). |
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S3261 |
Myrislignan
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Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan inhibits interleukin-6 (IL-6) and tumour necrosis factor-α (TNF-α). Myrislignan significantly inhibits the expressions of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2) dose-dependently in LPS-stimulated macrophage cells. Myrislignan inhibits the NF-κB signalling pathway activation. |
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S3283 |
Marmesin
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Marmesin (S-(+)-Marmesin, (+)-Marmesin, (S)-Marmesin) is a natural coumarin with COX-2 and 5-LOX dual inhibitory activity. |
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S3304 |
Stylopine
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Stylopine ((R,S)-Stylopine, Tetrahydrocoptisine) reduces nitric oxide (NO), prostaglandin E2 (PGE2), tumor necrosis factor-alpha (TNF-alpha) and interleukin-1beta (IL-1beta), and the IL-6 production and cyclooxygenase-2 (COX-2) activity caused by the LPS stimulation. Stylopine is a major component of the leaf of Chelidonium majus L. |
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S3816 |
Dehydroevodiamine
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Dehydroevodiamine (DHED), a constituent of Evodia rutaecarpa, has various biological effects such as hypotensive, negative chronotropic, ion channel depressant, inhibition of nitric oxide production and cerebral blood flow enhancing activities. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells. |
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S3872 |
Guaiacol
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Guaiacol (O-methoxyphenol, 2-hydroxyanisole, O-methylcatechol) is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. It is a precursor to various flavorants, such as eugenoland vanillin. Guaiacol, a phenolic compound isolated from Guaiac resin, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity. |
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S3899 |
Hederagenin
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Hederagenin (Caulosapogenin, Hederagenol, Hederagenic acid, Astrantiagenin E) is a highly water insoluble triterpenoid compound that can be found in various plants including Hedera helix and Chenopodium quinoa. It exhibits a variety of biological activities, including potent antitumor properties both in vitro and in vivo. Hederagenin inhibits LPS-stimulated expression of iNOS, COX-2, and NF-κB. |
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S3925 |
(-)-Epicatechin gallate
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(-)-Epicatechin gallate (ECG) is an inhibitor of cyclooxygenase-1 (COX-1) with IC50 of 7.5 μM. |
- Cell Death Dis, 2018, 9(2):205
- PLoS One, 2018, 13(10):e0205123
- J Fish Dis, 2018, 10.1111/jfd.12819
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S3931 |
Ginsenoside Rd
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Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively. |
- J Ethnopharmacol, 2021, S0378-8741(21)00169-0
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S3969 |
Veratric acid
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Veratric acid (3,4-Dimethoxybenzoic acid), a simple benzoic acid derived from plants and fruits, has anti-oxidant, anti-inflammation, and blood pressure-lowering effects. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation. |
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S3974 |
(+)-Catechin hydrate
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Catechins are a plant derived polyphenolic anti-oxidants with phytotoxic properties. (+)-Catechin hydrate is a frequent component of traditional herbal remedies, such as Uncaria rhynchophylla. (+)-Catechin hydrate inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM. |
- J Steroid Biochem Mol Biol, 2021, 211:105906
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S4011 |
Ampiroxicam
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Ampiroxicam (CP 65703) is a nonselective cyclooxygenase inhibitor uesd as anti-inflammatory drug. |
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S4028 |
Dexamethasone Sodium Phosphate
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Dexamethasone (Dexamethasone 21-phosphate disodium salt) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. |
- Pharmaceutics, 2022, 14(2)400
- Dis Model Mech, 2022, dmm.049109
- Hematology, 2022, 27(1):32-42
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S4032 |
Bismuth Subsalicylate
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Bismuth Subsalicylate is the active ingredient in Pepto-Bismol and inhibits prostaglandin G/H Synthase 1/2. |
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S4049 |
Valdecoxib
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Valdecoxib is a potent and selective inhibitor of COX-2 with IC50 of 5 nM. |
- Cancer Cell, 2022, S1535-6108(21)00662-0
- Cell Rep, 2022, 38(10):110490
- Biochem Bioph Res Co, 2015, 460(2):198-204
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S4051 |
Nabumetone
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Nabumetone (BRL-14777) is a non-steroidal anti-inflammatory drug and its active metabolite inhibits the COX. |
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S4078 |
Mefenamic Acid
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Mefenamic Acid (CI 473, CN-35355) is a competitive inhibitor of COX-1 and COX-2. |
- Am J Physiol Renal Physiol, 2022, 10.1152/ajprenal.00568.2020
- Brain Res, 2020, 20;1740:146846
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S4136 |
Carprofen
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Carprofen inhibits canine COX2 with IC50 of 30 nM. |
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S4149 |
Amfenac Sodium Monohydrate
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Amfenac Sodium monohydrate is a non-steroidal analgesic anti-inflammatory drug with acetic acid moiety. The IC50 values for COX1 and COX2 is 250 nM and 150 nM, respectively. |
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S4176 |
Trometamol
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Trometamol is a proton acceptor used to treat acidemia. It inhibits both isoforms of cyclooxygenases (COX1 and COX2), thereby blocking the conversion of arachidonic acid to pro-inflammatory pro-prostaglandins. |
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S4230 |
Oxaprozin
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Oxaprozin (WY-21743) 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. |
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S4248 |
Bromfenac Sodium
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Bromfenac Sodium (AHR 10282R) is a nonsteroidal anti-inflammatory drug (NSAID), which has anti-inflammatory activity and may block prostaglandin synthesis by inhibiting cyclooxygenase 1 and 2. |
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S4295 |
Meclofenamate Sodium
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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. Meclofenamate Sodium is a non-selective gap-junction blocker and a highly selective inhibitor of fat mass and obesity-associated (FTO) enzyme inhibitor. |
- Front Oncol, 2022, 12:817584
- Nature, 2019, 573(7775):539-545
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S4360 |
Tolmetin Sodium
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Tolmetin is a non-steroidal anti-inflammatory drug of the arylalkanoic acids. Tolmetin sodium dihydrate is a non-steroidal antiinflammatory agent, and acts as a non-selective COX inhibitor. |
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S4435 |
Metamizole sodium hydrate
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Metamizole (Dipyrone) sodium hydrate is a potent inhitior of cyclooxygenase (COX) with strong analgesic as well as antipyretic and spasmolytic properties. |
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S4509 |
4-Aminoantipyrine
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4-Aminoantipyrine(Ampyrone) is a metabolite of aminopyrine with analgesic, anti-inflammatory, and antipyretic properties. It is used as a reagent for biochemical reactions producing peroxides or phenols. |
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S4526 |
Fenbufen
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Fenbufen (Lederfen, CL-82204) is an orally active phenylalkanoic derivative with anti-inflammatory, analgesic and antipyretic activity. It is a non-steroidal anti-inflammatory drug. |
- Gastroenterology, 2019, 10.1053/j
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S4539 |
Salicylic acid
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Salicylic acid (2-Hydroxybenzoic acid) is a beta hydroxy acid that occurs as a natural compound in plants which is an inhibitor of ethylene biosynthesis and cyclooxygenase activity. |
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S4609 |
Diflunisal
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Diflunisal (Dolobid, Dolobis, Flovacil, Fluniget) 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. |
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S4628 |
(+/-)-Sulfinpyrazone
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Sulfinpyrazone (G-28315, NSC 75925) is one of the most studied platelet COX inhibitors, also a uricosuric agent that competitively inhibits uric acid reabsorption in kidney proximal tubules. |
- Cell Chem Biol, 2021, S2451-9456(21)00442-6
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S4651 |
Etoricoxib
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Etoricoxib (Arcoxia, MK-663, MK-0663, Tauxib, Algix, Nucoxia) is a new COX-2 selective inhibitor with anti-inflammatory, antipyretic, analgesic, and potential antineoplastic properties. |
- Virol Sin, 2019, 34(6):648-661
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S4656 |
Parecoxib
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Parecoxib (SC-69124, Valus-P, Vorth-P) is a selective COX2 inhibitor. |
- Theranostics, 2020, 10(8):3366-3381
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S4686 |
Vitamin E
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Vitamin E (D-alpha-Tocopherol) 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. |
- Bone Res, 2022, 10(1):26
- EMBO Mol Med, 2022, 14(2):e14903
- Biosci Biotechnol Biochem, 2020, 18;1-8
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S4765 |
Syringaldehyde
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Syringaldehyde (Syringic aldehyde) is an organic compound that occurs naturally in trace amounts. It possesses worthy bioactive properties and is, therefore, used in pharmaceuticals, food, cosmetics, textiles, pulp and paper industries, and even in biological control applications. Syringaldehyde is a polyphenolic compound belonging to the group of flavonoids and is found in different plant species like Manihot esculenta and Magnolia officinalis. Syringaldehyde moderately inhibits COX-2 activity with an IC50 of 3.5 μg/mL[2]. Anti-hyperglycemic and anti-inflammatory activities. |
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S5010 |
Indometacin Sodium
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Indometacin Sodium (Indomethacin Sodium) is the sodium salt of indomethacin, which is a non-selective, reversible, and competitive inhibitor of cyclooxygenases 1 and 2 with anti-inflammatory, analgesic-antipyretic and tocolytic effects. |
- J Exp Clin Cancer Res, 2021, 40(1):344
- Mol Cell, 2020, 80(3):525-540.e9
- Mol Cancer Ther, 2020, 19;molcanther00152020
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S5019 |
Indobufen
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Indobufen (Ibustrin, K 3920) is a reversible platelet aggregation inhibitor. Indobufen is a reversible inhibitor of platelet cyclooxygenase (Cox) activity and suppresses thromboxane synthesis. |
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S5177 |
Naproxen
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Naproxen is an anti-inflammatory agent with analgesic and antipyretic properties. It is a nonselective inhibitor of COX-1 and COX-2. |
- Drug Metab Dispos, 2020, 48(8):613-621
- Biogerontology, 2016, 17(5-6):907-920
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S5192 |
S-(+)-Ketoprofen
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S-(+)-Ketoprofen (Compound 1, Actron, (S)-Ketoprofen, Dexketoprofen) is a potent inhibitor of cyclooxygenase (COX) with IC50 of 1.9 nM and 27 nM for COX-1 and COX-2, respectively. |
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S5309 |
Propyphenazone (4-Isopropylantipyrine)
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Propyphenazone(4-Isopropylantipyrine, Isopropyrine), an analgesic and antipyretic agent, is a selective cyclooxygenase-2 inhibitor with anti-inflammatory activity. |
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S5418 |
Parecoxib Sodium
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Parecoxib Sodium (SC-69124) is a water-soluble, injectable sodium salt form of parecoxib, which is a potent and selective inhibitor of cyclo-oxygenase-2 (COX2). |
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S5520 |
Phenidone
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Phenidone (1-phenyl-3-pyrazolidinone), a dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), is an organic compound that is primarily used as a photographic developer. |
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S5551 |
6-Paradol
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6-Paradol is a minor constituent of ginger, mainly formed from 6-gingerol via 6-shogaol, and exhibits a variety of biological activities including anti-cancer, anti-inflammatory, and anti-oxidative activities. Paradol is an inhibitor of cyclooxygenase (COX)-2. |
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S5595 |
3-Carene
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3-Carene (Carene, Delta-3-Carene) is a bicyclic monoterpene in essential oils extracted from pine trees. 3-Carene have potent pharmacological effects on COX-2 overexpression and LPS-induced migration of Raw264.7 macrophages. 3‐carene is shown to significantly stimulate the activity and expression of alkaline phosphatase, an early phase marker of osteoblastic differentiation. |
- Phytomedicine, 2021, 91:153707
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S5640 |
Ethyl caffeate
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Ethyl caffeate, a naturally occurring compound found in Bidens pilosa, suppresses NF-kappaB activation and its downstream inflammatory mediators, iNOS, COX-2 and PGE2 in vitro. |
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S5698 |
Ketorolac tromethamine salt
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Ketorolac tromethamine is a synthetic pyrrolizine carboxylic acid derivative with anti-inflammatory, analgesic and antipyretic properties. It is a non-selective COX inhibitor with IC50s of 20 nM for both COX-1 and COX-2. |
- Front Immunol, 2021, 12:616402
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S5711 |
Deracoxib
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Deracoxib (SC-046) is a COX-2 inhibitor with >48-fold selectivity over COX-1. It also exhibits inhibitory activity against phosphodiesterase (Ki = 3.6 μM against human PDE4D3). |
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S5786 |
Bromfenac sodium hydrate
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Bromfenac sodium hydrate (Bromsite, Bromday, Prolensa, Xibrom), a brominated nonsteroidal anti-inflammatory drugs (NSAID) with strong in vitro anti-inflammatory potency, is a potent and orally active inhibitor of COX with IC50 of 5.56 nM and 7.45 nM for COX-1 and COX-2, respectively. |
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S6073 |
Diclofenac acid
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Diclofenac acid is a nonsteroidal anti-inflammatory drug that has analgesic, anti-inflammatory, and antipyretic properties, and has been shown to be effective in treating a variety of acute and chronic pain and inflammatory conditions. It inhibits cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) with relative equipotency. |
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S6457 |
Flurbiprofen Axetil
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Flurbiprofen Axetil is one of the commonly used nonsteroidal anti-inflammatory drugs (NSAIDs) that nonselectively inhibits cyclooxygenase. |
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S6615 |
ATB 346
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ATB 346, a novel hydrogen sulphide-releasing derivative of naproxen with remarkably reduced toxicity, inhibits COX activity. ATB 346 is an anti-inflammatory agent that induces apoptosis of human melanoma cells. |
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S6685 |
Mavacoxib
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Mavacoxib (Trocoxil) is a selective, long-acting cyclooxygenase-2 (COX-2) inhibitor. Mavacoxib is a novel nonsteroidal anti-inflammatory drug (NSAID). |
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S6686 |
SC-560
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SC-560 is a highly selective COX-1 inhibitor with IC50 of 9 nM, compared with the IC50 of 6.3 μM for COX-2, nearly 1,000-fold higher than with COX-1. |
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S6780 |
TFAP
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TFAP (N-(5-Aminopyridin-2-yl)-4-(trifluoromethyl)benzamide) is a selective and cell-permeable cyclooxygenase-1 (COX-1) inhibitor with IC50 of 0.8 μM. |
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S6850 |
NE 52-QQ57
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NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with NE 52-QQ57 significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2). |
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S7889 |
Xanthohumol
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Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Xanthohumol inhibits diacylglycerol acyltransferase 1 (DGAT1) and DGAT2 with both IC50 of 40 μM. Xanthohumol is also a potent antiviral agent against a series of DNA and RNA viruses. Xanthohumol induces growth inhibition and apoptosis in cancer cells. Phase 1. |
- Oxid Med Cell Longev, 2022, 2022:9523491
- Int J Mol Sci, 2021, 22(22)12134
- J-Cancer, 2020, 6;11-14-:4047-4058
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S8433 |
NS-398 (NS398)
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NS-398 (N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide) 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. |
- PLoS Negl Trop Dis, 2022, 16(4):e0010402
- Mol Oncol, 2021, 10.1002/1878-0261.13077
- Oxid Med Cell Longev, 2021, 2021:7394344
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S9029 |
Prim-o-glucosylcimifugin
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Prim-O-glucosylcimifugin (Cimifugin beta-D-glucopyranoside, Cimifugin 7-glucoside) is a major constituent in Radix Saposhnikovia that has been long used for the treatment of pyrexia, rheumatism, and cancer in traditional Chinese medicine. It shows potential anticancer activity. Prim-O-glucosylcimifugin downregulates the mRNA and protein expression inducible NO synthase (iNOS) and cyclooxygenase 2 (COX-2) in LPS-activated RAW 264.7 macrophages in a concentration-dependent manner. |
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S9149 |
Benzoylpaeoniflorin
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Benzoylpaeoniflorin, a natural product isolated from Chinese paeony root, could inhibit COX-1 and COX-2 in vitro. |
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S9190 |
Oroxin B
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Oroxin B (Hypocretin-2), one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer.COX-2, VEGF, PI3K, and p-AKT expression levels are downregulated, while PTEN is upregulated after Oroxin B treatment. |
- Theranostics, 2022, 12(2):910-928
- J Cancer, 2021, 12(7):2140-2150
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S9208 |
Ginsenoside Rb3
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Ginsenoside Rb3, extracted from the plant Panax ginseng, plays important roles in cardiovascular diseases, including myocardial ischemia-reperfusion (I/R) injury. Ginsenoside Rb3 (0.1-10 μM) is tested for inhibition of tumor necrosis factor-α (TNF)-induced nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) luciferase reporter activity using a human kidney 293T cell-based assay. Ginsenoside Rb3 shows the significant activity with an IC50 of 8.2 μM. Ginsenoside Rb3 also inhibits the induction of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) messenger Ribonucleic acid (mRNA) in a dose-dependent manner after HepG2 cells have been treated with TNF-α (10 ng/mL). |
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S9236 |
α-Cyperone
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α-Cyperone (alpha-cyperone), a major active compound of Cyperus rotundus, exhibits biological activities, such as antivirulence, antigenotoxic, and antibacterial activities. α-Cyperone (alpha-cyperone) is associated with the down-regulation of COX-2, IL-6, Nck-2, Cdc42 and Rac1. |
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S9386 |
Polygalacic acid
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Polygalacic acid is the triterpenoid tetrahydroxyacid isolated from Polygala paenea L.. Polygalacic acid (0-100 μM; 24 hours) significantly decreases the mRNAexpressions of MMP-3, MMP-9, MMP-13 and COX-2, which are significantly increased by IL-1β, in a dose-dependent manner. |
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S9502 |
Madecassic acid
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Madecassic acid (Brahmic acid), a natural triterpene first isolated from C. asiatica, has diverse anti-inflammatory and anti-diabetic effects, blocking NF-κB activation in macrophages and causing by iNOS, COX-2, TNF-alpha, IL-1beta and IL-6 inhibition. |
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