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COX inhibitor
Acetaminophen (paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic drug. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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xanthine oxidase inhibitor
Allopurinol is a structural isomer of hypoxanthine (a naturally occurring purine in the body) and is an inhibitor of the enzyme xanthine oxidase. -
COX-2 inhibitor
Celecoxib is a sulfa non-steroidal anti-inflammatory drug (NSAID) and selective COX-2 inhibitor used in the treatment of osteoarthritis, rheumatoid arthritis, acute pain, painful menstruation and menstrual symptoms, and to reduce numbers of colon and rectum polyps in patients with familial adenomatous polyposis.
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Dihydropyrimidinase Inhibitor
Dihydromyricetin (Ampelopsin (flavanol); Ampeloptin) is a natural antioxidant with good prospects. -
COX inhibitor
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. -
COX inhibitor
Etodolac (AY-24236) is a non-steroidal anti-inflammatory compound that is a non-selective inhibitor of COX (IC50=53.5 nM).- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
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xanthine oxidase inhibitor
Febuxostat is a non-purine inhibitor of xanthine oxidase (Ki = 1.2 nM). -
mTOR inhibitor
FK-506 is an immunosuppressive drug that is mainly used after allogeneic organ transplant to reduce the activity of the patient's immune system and so lower the risk of organ rejection. It reduces interleukin-2 (IL-2) production by T-cells.- Ogawa Y, .et al. , Neurobiol Dis, 2018, Oct;118:142-154 PMID: 30026035
- Yuko Okamoto, .et al. , J Drug Deliv Sci Technol, 2018, 47: 62-66
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COX-1 inhibitor
Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) targeting COX-1 with an IC50 of 13 μM.- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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COX-1 inhibitor
Ibuprofen Lysine(Motrin) is a non-steroidal anti-inflammatory drug. -
COX inhibitor
Indomethacin is a nonselective COX1 and COX2 inhibitor with IC50 of 0.1 μg/mL and 5 μg/mL, respectively. Indomethacin(Indocid, Indocin) is a non-steroidal anti-inflammatory compound commonly used to reduce fever, pain, stiffness, and swelling.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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NLRP3 inflammasome inhibitor
Isoliquiritigenin is a licorice chalconoid, a type of natural phenols that is currently under experimentation phase testing for use as a cancer treatment as well as an aide for cocaine addiction. -
COX-1/COX-2 inhibitor
Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively. -
IMPDH inhibitor
Mycophenolate mofetil is a reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH) in purine biosynthesis (specifically guanine synthesis) which is necessary for the growth of T cells and B cells. -
COX inhibitor
Naproxen sodium is a non-selective cyclooxygenase (COX) inhibitor that displays anti-inflammatory, antipyretic and analgesic effects. Has a neuroprotective role against colchicine-induced cognitive impairment and oxidative stress. -
COX inhibitor
Phenylbutazone is a compound of research interest as an anti-inflammatory and anti-proliferative agent. -
COX inhibitor
Piroxicam is an effective and potent inhibitor of prostaglandin synthesis and a Cox-1 and Cox-2 inhibitor. -
COX inhibitor
Pravadoline (WIN 48,098) is antiinflammatory and prostaglandin synthesis inhibitor, acting through inhibition of the enzyme cyclooxygenase (COX).- Sharma P, .et al. , Org Lett, 2016, Feb 5;18(3):412-5 PMID: 26745849
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mTOR Inhibitors
Rapamycin (Sirolimus) prevents activation of T cells and B-cells by inhibiting their response to interleukin-2 (IL-2).- Hideki Kawasaki, .et al. , J Insect Physiol, 2023, Mar;145:104476 PMID: 36623750
- R Mahalakshmi, .et al. , Mol Biol Rep, 2022, Jan;49(1):463-476 PMID: 34739690
- Yusuke Murase, .et al. , Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
- Zhichao Wu, .et al. , Cells, 2021, Oct 27;10(11):2912 PMID: 34831135
- Matthew A Schaller, .et al. , JCI Insight, 2021, Sep 22;6(18):e148003 PMID: 34357881
- Matthew A. Schaller, .et al. , bioRxiv, 2021, January 21
- Ashley VanCleave, .et al. , Oncotarget, 2020, Jul 7; 11(27): 2597-2610 PMID: 32676162
- Y Huang, .et al. , Experimental and Therapeutic Medicine, 2020, 20(2), 736-747 PMID: 32742319
- Takuya Hirao, .et al. , Cancer Sci, 2018, Jan; 109(1): 121-131 PMID: 29121435
- Ya-Hui Chen, .et al. , J Diabetes Res, 2016, 2016: 1828071 PMID: 28004006
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COX inhibitor
Sulindac is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions -
HIV Entry Inhibitor
BMS-806, also known as BMS-378806 , is a type of medicine called an entry inhibitor. Entry inhibitors work by blocking HIV from entering human cells. BMS-378806 (BMS-806) is a small molecule that blocks the binding of host-cell CD4 with viral gp120 protein and therefore inhibits the first steps of HIV-1 infection. -
COX-2 inhibitor
Iguratimod(T 614) is one of a series of 4H-1-benzopyran-4-ones which has potent anti-inflammatory, analgesic and antipyretic activity. Iguratimod(T 614) is a selective inhibitor of cyclo-oxygenase-2 (COX-2), and inhibits the production of interleukin-1 (IL-1), IL-6, IL-8 and tumour necrosis factor. -
TLR4 inhibitor
Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor and plays pivotal role in various inflammatory diseases. -
COX inhibitor
Pranoprofen is a non-steroidal anti-inflammatory drug used in ophthalmology -
COX inhibitor
Flunixin Meglumin is a potent inhibitor of the enzyme cyclooxygenase (COX) used as analgesic agent with anti-inflammatory and antipyretic activity.- Yukari Nakajima, .et al. , Sci Rep, 2018, 8: 7078 PMID: 29728629
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COX inhibitor
Acemetacin is a glycolic acid ester of indometacin. It is metabolized to indometacin, which then acts as an inhibitor of cyclooxygenase, producing the anti-inflammatory effects. -
COX-2 inhibitor
Tolfenamic Acid is a COX-2 inhibitor with IC50 of 0.2 μM. It is one of the class of non-steroidal anti-inflammatory drugs (NSAIDs). It is used to treat the symptoms of migraine. -
COX-2 inhibitor
Nimesulide is a relatively COX-2 selective, non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. -
COX inhibitor
Lornoxicam is a non-steroidal COX-1/COX-2 inhibitor. It is a non-steroidal anti-inflammatory drug (NSAID) of the oxicam class with analgesic (pain relieving), anti-inflammatory and antipyretic (fever reducing) properties. -
COX/LOX inhibitor
Licofelone is a dual COX/LOX inhibitor, being considered as a treatment for osteoarthritis. It may reduce the gastrointestinal toxicity associated with other non-steroidal anti-inflammatory drugs, which only inhibit COX (cyclooxygenase). Licofelone is the first drug to inhibit both.- Silke Neumann, .et al. , Front Immunol, 2016, 7: 537 PMID: 27994586
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Hsp90/SRC/COX-2 Inhibitor
Radicicol is a potent inhibitor of Hsp90, SRC, and Cox-2- Guangsen Li, .et al. , Pharm Biol, 2023, 61(1): 271-280 PMID: 36655371
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COX inhibitor/histamine H1 receptor agonist
Fexofenadine HCl is an antihistamine that inhibits Cox-1, Cox-2, and is a histamine H1 receptor agonist -
mTOR inhibitor
Zotarolimus is an immunosuppressant. It is a semi-synthetic derivative of rapamycin. It was designed for use in stents with phosphorylcholine as a carrier. -
NADPH-oxidase inhibitor
Apocynin is a NADPH oxidase inhibitor- Liling Su, .et al. , Ecotoxicol Environ Saf, 2022, Jun 1;237:113519 PMID: 35453021
- Shimizu S, .et al. , Br J Pharmacol, 2018, Sep;175(18):3727-3737 PMID: 29981238
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COX-1 inhibitor
(-)-Epicatechin is a natural product from green tea. (-)Epicatechin is an inhibitor of Cox-1- Grace Northrop, .et al. , Food Funct, 2022, Apr 4;13(7):3894-3904 PMID: 35285840
- A S D'Costa, .et al. , Food Chem, 2020, Oct 1;341(Pt 2):128256 PMID: 33035827
- Mihaela Tudorache, .et al. , Food Hydrocoll, 2019, 97, Dec, 105193
- Md Shajedul Islam, .et al. , Innovative food science & emerging technologies, 2016, v.34 pp. 344-351
- Islam MS, .et al. , J Agric Food Chem, 2016, Oct 10 PMID: 27632812
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COX-2 inhibitor
Gallic acid is a trihydroxybenzoic acid found in many plants as either the free acid or in the esterified form of gallotannins and ellagitannins. Gallic acid is an antioxidant which can inhibit both COX-2. -
PD1 signaling pathway inhibitor
PD-1-IN-18 is a PD1 signaling pathway inhibitor, which acts as an immunomodulator. -
programmed cell death-1 (PD-1) inhibitor
PD-1-IN-17 is a programmed cell death-1 (PD-1) inhibitor extracted from patent WO2015033301A1, Compound 12, inhibits 92% splenocyte proliferation at 100 nM. -
COX-1 inhibitor
Catechin is a polyphenolic flavonoid which has been isolated from a variety of natural sources including tea leaves, grape seeds, and the wood and bark of trees such as acacia and mahogany. -
HPGDS inhibitor
HPGDS inhibitor 1 is a novel and selective Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50 Value of 0.7 nM. -
CXCL8/CXCR1/2 Inhibitor
Reparixin is a potent inhibitor of both CXCL8 receptors CXCR1/2, it inhibits weakly CXCR2-mediated cell migration (IC50=100 nM), whereas it strongly blocks CXCR1-mediated chemotaxis (IC50=1 nM).- Naour AL, .et al. , J Mol Cell Biol, 2019, Sep 3 PMID: 31504643
- Wigenstam E, .et al. , Toxicology, 2015, Feb 3;328:40-7 PMID: 25497111
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COX inhibitor
(S)-(+)-Flurbiprofen is a non-selective Cox-1 and Cox-2 inhibitor.- Xing Jin, .et al. , Microchemical Journal, 2018, 143: 280-285
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COX inhibitor
Meclofenamate Sodium is a dual COX-1/COX-2 inhibitor with IC50 of 40 nM and 50 nM.