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γ-secretase inhibitor
BMS 299897 is an orally active, potent γ-secretase inhibitor (IC50 = 12 nM). Inhibits Aβ40 and Aβ42 formation in vitro (IC50 values are 7.4 and 7.9 nM respectively) and reduces Aβ in the brain, plasma and cerebrospinal fluid in vivo.- Chao Liu, .et al. , Cell Death Differ, 2018, Apr; 25(4): 661-676 PMID: 29238071
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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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Gamma secretase inhibitor
LY-411575 is a selective, cell permeable, small molecule gamma secretase inhibitor.
- Haiwen Yu, .et al. , Immunol Invest, 2023, Feb;52(2):241-255 PMID: 36562737
- Wojciech J Szlachcic, .et al. , iScience, 2022, Jul 15;25(7) PMID: 35756892
- Zhang ZH, .et al. , APMIS, 2019, Jul 5 PMID: 31274210
- Bo Pang, .et al. , Biosci Rep, 2018, Dec 21; 38(6): BSR20181922 PMID: 30473538
- Shuo Li, .et al. , Int Immunopharmacol, 2018, Oct;63:129-136 PMID: 30086535
- Jiang BC, .et al. , Viral Immunol, 2017, Sep;30(7):522-532 PMID: 28410452
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OGT inhibitor
OSMI-4 is a low nanomolar O-GlcNAc transferase (OGT) inhibitor, with an EC50 of 3 μM in cells.- Haoxue Wang, .et al. , FASEB J, 2026, Feb 28;40(4):e71592 PMID: 41729008
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Gamma-secretase inhibitor
RO4929097 is an orally bioavailable, small-molecule gamma secretase (GS) inhibitor with an IC50 of 4 nM.- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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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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CaMKII inhibitor
KN-93 Phosphate is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.37 μM, no remarkable inhibitory effects on APK, PKC, MLCK or Ca2+-PDE activities.- Kazuki Yuasa, .et al. , Sci Rep, 2018, 8: 9037 PMID: 29899565
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CaMK-II inhibitor
KN-93 phosphate is a novel membrane-permeant synthetic inhibitor of purified neuronal CaMK-II, with Ki of 370 nM.- Kazuki Yuasa, .et al. , Sci Rep, 2018, 8: 9037 PMID: 29899565
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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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CaM kinase II inhibitor
KN-93 is an inhibitor of multifunctional Ca++/calmodulin-dependent protein kinase.- Margherita Zaupa, .et al. , Neuron, 2024, Apr 3;112(7):1150-1164 PMID: 38295792
- Christian E Coleman, .et al. , Arch Microbiol, 2022, Jul 24;204(8):519 PMID: 35871646
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BACE1 inhibitor
LY2886721 is a novel potent agent that is used to treat Alzheimer's Disease in preclinical experiments.- Naomi Ito, .et al. , Br J Pharmacol, 2017, Mar; 174(5): 386-395 PMID: 28012171
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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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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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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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HIV-1 production Inhibitor
Baicalin is a known prolyl endopeptidase inhibitor and affects the GABA receptors.- Shoichi Ozawa, .et al. , Sci Rep, 2019, 9: 15464 PMID: 31664047
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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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Gamma-secretase inhibitor
FLI-06 is a Notch inhibitor and the early secretory pathway inhibitor. FLI-06 disrupts the Golgi apparatus in a manner distinct from that of brefeldin A and golgicide A.- Tan YJ, .et al. , Future Med Chem, 2018, Sep 1;10(17):2039-2057 PMID: 30066578
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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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Gamma secretase inhibitor
DAPT (GSI-IX) is an inhibitor of γ-secretase that causes a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures with IC50 values of 115 and 200 nM for total Aβ and Aβ42 respectively.- Tzu-Pei Lee, .et al. , Journal of Dental Sciences, 2025, Jul;20(3):1629-1638 PMID: 40654420
- Kubra Telli, .et al. , Turkish Journal of Biochemistry, 2023, February 6
- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
- Tatsuya Usui, .et al. , Int J Mol Sci, 2018, Apr; 19(4): 1098 PMID: 29642386
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γ-secretase inhibitor
YO-01027 is a dipeptidic γ-secretase inhibitor, an antiAlzheimer agent.- Weijun Zhang, .et al. , Stem Cell Rev Rep, 2023, Jan 7 PMID: 36609902
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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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Gamma-secretase inhibitor
Semagacestat (LY450139) is a γ-secretase blocker for Aβ42, Aβ40 and Aβ38 with IC50 of 10.9 nM, 12.1 nM and 12.0 nM, respectively. Semagacestat also inhibits Notch signaling with IC50 of 14.1 nM.- Yesuvadian R, .et al. , Biochem Biophys Res Commun., 2014, May 16;447(4):590-5 PMID: 24747079
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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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Glucocerebroside synthase inhibitor
Commonly used as the tartrate salt, Eliglustat is believed to work by inhibition of glucosylceramide synthase.- Zunke F, .et al. , Neuron, 2018, Jan 3;97(1):92-107.e10 PMID: 29290548
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muscarinic receptor inhibitor
Darenzepine is a muscarinic receptor inhibitor extracted from patent US 20170095465 A1. -
Glucosylceramide synthase inhibitor
Eliglustat is a specific and potent inhibitor of glucosylceramide synthase. -
PKD inhibitor
CID 2011756 is a protein kinase D (PKD) inhibitor (IC50 values are 0.6, 0.7 and 3.2 μM for PKD2, PKD3 and PKD1 respectively). -
PKD inhibitor
kb NB 142-70 is a selective protein kinase D (PKD) inhibitor (IC50 values are 28.3, 58.7 and 53.2 nM for PKD1, 2 and 3 respectively). -
AChE inhibitor
Galanthamine is a potent acetylcholinesterase (AChE) inhibitor with an IC50 of 500 nM. -
COX inhibitor
Meclofenamate Sodium is a dual COX-1/COX-2 inhibitor with IC50 of 40 nM and 50 nM. -
amyloid β42 inhibitor
Ro 90-7501 is an inhibitor of amyloid β42 (Aβ42) fibril assembly; reduces Aβ42-induced toxicity (EC50 = 2 μM). -
GABA transport inhibitor
(S)-SNAP5114 is a selective GABA transport inhibitor, with IC50 values of 5 μM and 21 μM for hGAT-3 and rGAT-2, respectively. (S)-SNAP5114 is an anticonvulsant drug. -
COX-1 and COX-2 inhibitor
Naproxen etemesil is a lipophilic, non-acidic, inactive prodrug of naproxen that is hydrolysed to pharmacologically active Naproxen once absorbed. Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay. -
COMT inhibitor
opicapone is a novel catechol-O-methyltransferase inhibitor -
COX-2 inhibitor
Bromfenac sodium is a topically selective cyclooxygenase (COX)-2 inhibitor -
COX inhibitor
Flufenamic acid is a nonsteroidal anti-inflammatory drug (NSAID). Inhibits calcium-activated chloride channels (CaCCs). Also increases currents through TRPC6 channels and inhibits currents through TRPC3 and TRPC7 channels. -
COX-2 inhibitor
Valdecoxib, also known as SC-65872, is a non-steroidal anti-inflammatory drug (NSAID) used in the treatment of osteoarthritis, rheumatoid arthritis, and painful menstruation and menstrual symptoms. It is a selective cyclooxygenase-2 inhibitor. -
γ-secretase inhibitor
Begacestat is a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease. -
γ-secretase inhibitor
PF-03084014 is a reversible and selective inhibitor of γ-secretase with IC50 value of 6.2 nM .

