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TRK, ROS1, ALK inhibitor
Entrectinib, also known as RXDX-101 and NMS-E628, is an oral small molecule inhibitor of TrkA, TrkB and TrkC, as well as ROS1 and ALK, with high potency and selectivity.- Angelina T Regua, .et al. , Cancer Lett, 2024, Jun 7:597:217023 PMID: 38852701
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HPGDS inhibitor
HPGDS inhibitor 1 is a novel and selective Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50 Value of 0.7 nM.- Beixian Zhou, .et al. , Chin Med, 2023, Oct 27;18(1):139 PMID: 37891648
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HO-1 inhibitor
Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is a competitive heme oxygenase-1 (HO-1) inhibitor, markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2.- Beixian Zhou, .et al. , MedComm, 2024, Apr 12;5(4):e531 PMID: 38617435
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NOX1/4 inhibitor
GKT137831 is a first in class inhibitor targeting NOX1 and NOX4 enzymes.- Chia-Hui Huang, .et al. , Toxicol Appl Pharmacol, 2020, Apr 17;397:115013 PMID: 32305283
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NRF2 inhibitor
ML-385 is an inhibitor of nuclear factor erythroid 2-related factor 2 (Nrf2) with IC50 value of 1.9 μM.- Duo Shi, .et al. , Antioxid Redox Signal, 2025, Sep 30 PMID: 41027674
- Liping Luo, .et al. , Heliyon, 2023, Aug 3;9(8):e18929 PMID: 37600361
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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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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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NFAT inhibitor
NFAT Inhibitor, selective inhibitor of calcineurin-mediated dephosphorylation of nuclear factor of activated T cells (NFAT).- Jingwen Liu, .et al. , Cell Mol Gastroenterol Hepatol, 2021, Jul 1;S2352-345X(21)00135-1 PMID: 34217895
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COX-1 inhibitor
Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) targeting COX-1 with an IC50 of 13 μM.- Jingyeong Shin, .et al. , Chemical Engineering Journal, 2023, December
- 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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Gal-3 inhibitor
GB1107 is a potent, selective, orally active inhibitor of Galectin-3 (Gal-3) with a Kd of 37 nM for human Galectin-3. GB1107 reduces human and mouse lung adenocarcinoma growth and blocks metastasis in the syngeneic model.- Jiten R Sharma, .et al. , Life Sci, 2023, Apr 1;318:121480 PMID: 36775116
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RUNX2-DNA binding inhibitor
CADD522 is a potent inhibitor of runt-related transcription factor-2 (RUNX2)-DNA binding with an IC50 of 10 nM. CADD522 exhibits antitumor activity.- Jiten R Sharma, .et al. , Life Sci, 2023, Apr 1;318:121480 PMID: 36775116
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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.- L Wang, .et al. , Physiol Res, 2024, Nov 15;73(5):769-778 PMID: 39545791
- Jingyeong Shin, .et al. , Chemical Engineering Journal, 2023, December
- 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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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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FLAP inhibitor
MK-0591 is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor with an IC50 value of 1.6 nM in a FLAP binding assay.- MA Sartim, .et al. , Biomolecules, 2020, May; 10(5): 794 PMID: 32443924
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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
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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COX inhibitor
Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects.- Rachel Clark, .et al. , Mol Carcinog, 2026, Apr;65(4):508-522 PMID: 41664946
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NOS inhibitor
Asymmetric dimethylarginine is an endogenous inhibitor of nitric oxide synthase (NOS), and functions as a marker of endothelial dysfunction in a number of pathological states.- Raul Salinas, .et al. , PLoS One, 2023, Mar 2;18(3):e0282155 PMID: 36862634
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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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HDAC inhibitor
Sulforaphane activates Nrf2 and inhibits high glucose-induced progression of pancreatic cancer via AMPK dependent signaling. Sulforaphane has shown anti-cancer and anti-inflammatory activities.- Satoshi Endo, .et al. , J Biochem, 2021, Mar 17 PMID: 33729485
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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).- Saudatu Faruk, .et al. , J Nutr Biochem, 2025, 148: 110157
- Saudatu Faruk, .et al. , J Trace Elem Med Biol, 2025, Sep 6:92:127740 PMID: 40945136
- Saudatu Faruk, .et al. , Biol Trace Elem Res, 2025, May 8 PMID: 40338453
- Saudat Faruk, .et al. , Iron, 2025, March
- Yudong Li, .et al. , J Polym Sci, 2024, 62:2215-2230
- Ross van de Weterin, .et al. , Glia, 2024, Jun 20 PMID: 38899723
- Yuanqin Zhang, .et al. , Cancers (Basel), 2023, Dec 2;15(23):5691 PMID: 38067394
- Amnon Wittenstein, .et al. , PLoS Biol, 2023, Nov 9;21(11):e3002355 PMID: 37943958
- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- 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
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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TLR Inhibitor
TLR2-IN-C29 is an inhibitor of TLR2/1 and TLR2/6 signaling.- Sholihah, I.A., .et al. , BioNanoSci, 2026, 16, 396
- Qian-Lu Wang, .et al. , Mol Immunol, 2021, Oct;138:99-109 PMID: 34365196
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NOD-like receptors inhibitor
NOD-IN-1 is a potent mixed inhibitor of nucleotide-binding oligomerization domain (NOD)-like receptors, NOD1 and NOD2, with IC50 of 5.74 μM and 6.45 μM, respectively.- Shuqin Lai, .et al. , Int Immunopharmacol, 2025, Feb 6:147:114036 PMID: 39778279
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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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NLRP3 inhibitor
MCC950 sodium is a potent NLRP3 inflammasome inhibitor that inhibits IL-1beta production with IC50 value of 7.5 nm.- Takemasa Takii, .et al. , mSphere, 2025, 10:e00110-25 PMID: 40387341
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COX-1 Inhibitor
Paradol is the active flavor constituent of the seeds of Guinea pepper (Aframomum melegueta); Paradol has been found to have antioxidative and antitumor promoting effects- Taurin Hughes, .et al. , Int J Biol Macromol, 2021, Jul 1;182:2130-2143 PMID: 34087308
- Lihan Zhao, .et al. , Sci Rep, 2020, Nov 5;10(1):19182 PMID: 33154433
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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.- Tomoya Terashima, .et al. , Regenerative Cellular Therapies for Neurological Diseases, 2025, August: 95-107
- 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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Topoisomerase IV inhibitor
Ciprofloxacin Hydrochloride is a broad-spectrum antimicrobial carboxyfluoroquinoline, interfering with the bacterial DNA gyrase, inhibiting the DNA synthesis, and preventing bacterial cell growth.- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
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Factor B inhibitor
LNP023 is a highly potent factor B (FB) inhibitor with an IC50 value of 10 nM. LNP023 shows direct, reversible, and high-affinity binding to human FB (KD=7.9 nM).- Wenbin Yang, .et al. , J Clin Invest, 2022, Oct 17;132(20):e157975 PMID: 36250462
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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
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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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. -
xanthine oxidase inhibitor
Febuxostat is a non-purine inhibitor of xanthine oxidase (Ki = 1.2 nM). -
COX-1 inhibitor
Ibuprofen Lysine(Motrin) is a non-steroidal anti-inflammatory drug. -
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
Sulindac is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions -
Primates' C3 Inhibitor
Compstatin, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin inhibits only the activation of primates' complement system. Compstatin exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively.
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Complement factor C3 inhibitor
POT-4 (AL-78898A), a Compstatin derivative, is a potent inhibitor of complement factor C3 activation. POT-4 can be used for age-related macular degeneration research -
CKLF1/CCL17 inhibitor
CKLF1-C19 is the C-terminal peptide of human chemokine-like factor 1 (CKLF1). CKLF1-C19 interacts with CCR4, and inhibits chemotaxis induced by both CKLF1 and CCL17. CKLF1-C19 can suppress allergic lung inflammation via inhibiting chemotaxis mediated by CCR3 and CCR4.

