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RAGE Antagonist
FPS-ZM1 inhibits A??40- and A??42-induced cellular stress in RAGE-expressing cells.- Ahana Banerjee, .et al. , Biomater Adv, 2024, Oct:163:213937 PMID: 38968788
- Ahana Banerjee, .et al. , Int J Biol Macromol, 2024, Jun;270(Pt 2):132384 PMID: 38754682
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Amyloid beta (Aβ or Abeta) is a peptide of 36-C43 amino acids that is processed from the Amyloid precursor protein. Amyloid β-Peptide (1-42) human is a 42-amino acid peptide which plays a key role in the pathogenesis of Alzheimer disease. Downregulates bcl-2 and increases the levels of bax. Neurotoxic.
- Aysu Şen, .et al. , Iranian Journal of Basic Medical Sciences, 2026, 29: 1241-1248
- Naveen Kumar, .et al. , ACS Chem Neurosci, 2025, Dec 17;16(24):4751-4768 PMID: 41331838
- Bahar Sarikamis Johnson, .et al. , Metab Brain Dis, 2025, Oct 29;40(8):300 PMID: 41160319
- Kailash Jangid, .et al. , RSC Medicinal Chemistry, 2025, Sep 17 PMID: 41122453
- Kailash Jangid, .et al. , Comput Biol Med, 2025, Sep;196(Pt A):110762 PMID: 40664126
- Nilufer Ercin, .et al. , Mol Neurobiol, 2025, Sep;62(9):11030-11046 PMID: 40257688
- Naveen Kumar, .et al. , RSC Med Chem, 2024, Sep 24 PMID: 39399311
- Naveen Kumar, .et al. , ACS Chem Neurosci, 2024, May 25 PMID: 38795037
- Yinhua Ni, .et al. , J Agric Food Chem, 2024, Jul 31;72(30):16708-16725 PMID: 39016108
- Seda Onder, .et al. , Chem Biol Interact, 2022, Aug 25;363:110029 PMID: 35779611
- Seham S El-Hawary, .et al. , Food Funct, 2022, Sep 7;12(17):8078-8089 PMID: 34286787
- Zsolt Datki, .et al. , Int J Biol Macromol, 2022, Jan 7;201:262-269 PMID: 34999044
- Suresh K.Bowroju, .et al. , Bioorg Med Chem, 2021, 45:116311 PMID: 34304133
- Zsolt Datki, .et al. , Ecotoxicol Environ Saf, 2021, Jan 15;208:111666 PMID: 33396176
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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
- Methoctramine hydrate is a selective M2 muscarinic receptor antagonist at nM concentrations
- Dan Li, .et al. , Cell Biosci, 2023, Oct 3;13(1) PMID: 37789469
- Lingyu Wang, .et al. , Gut Microbes, 2020, 12(1): 1-20 PMID: 33006494
- Propofol is a hypnotic alkylphenol derivative. Propofol is a General Anesthetic. Propofol is a short-acting medication that results in a decreased level of consciousness and lack of memory for events. Formulated for intravenous induction of sedation and hypnosis during anesthesia, propofol facilitates inhibitory neurotransmission mediated by gamma-aminobutyric acid (GABA).
- Daphne Chun-Che Chien, .et al. , Sci Transl Med, 2024, May 8;16(746):eadk8198 PMID: 38718132
- Chenghao Jin, .et al. , Immun Inflamm Dis, 2023, Aug;11(8):e952 PMID: 37647434
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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
- (-)-Nicotine ditartrate is a potent agonist of AChR (nicotinic acetylcholine recepto).
- Guochao Ni, .et al. , Reprod Biol Endocrinol, 2020, 18: 65 PMID: 32552695
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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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Nicotinic (α7) Receptor Modulator
PNU-120596 is a positive allosteric modulator of α7 neuronal nicotinic acetylcholine receptors.- Hugo R Arias, .et al. , Br J Pharmacol, 2022, Sep 9 PMID: 36082615
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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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GABAA antagonist
(+)-Bicuculline is a classical GABAA antagonist.- Maryam Adenike Salaudeen, .et al. , J Pharmacy and Drug Innovations, 2022, 3(4)
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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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nAChR agonist
GTS-21 dihydrochloride is a selective α7 nicotinic acetylcholine receptor agonist, has recently been established as a promising treatment for inflammation.- P Yamini, .et al. , Pharmacol Biochem Behav, 2022, Jun;217:173402 PMID: 35533773
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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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NMDA receptor ion channel antagonist
ARL-15896 is a novel N-methyl-D-aspartate receptor ion channel antagonist.- Robert A. Volkmann, .et al. , PLoS One, 2016, 11(2): e0148129 PMID: 26829109
- Miglustat hydrochloride is an orally active α-glucosidase I and II and ceramide-specific glycosyltransferase inhibitor.
- Sayaka Tsuda, .et al. , J.Hard Tissue Biology, 2025, Vol. 34(1): 1-8
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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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GABA(A) receptor agonist
Muscimol hydrobromide is a potent but toxic structural analog of g-aminobutyric acid (GABA), with a zwitterionic structure.- Shi, Mengting, .et al. , Acupuncture and Herbal Medicine, 2025, 5(2):p 217-228
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M2/M4 AChR agonist
LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.- Shimrit Hazan, .et al. , Biochem Pharmacol, 2024, Sep:227:116421 PMID: 38996933
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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
- alpha-Amyloid Precursor Protein Modulator is a cell-permeable benzolactam derived PKC activator (Ki = 11.9 nM for PKCα) that efficiently enhances non-amyloidogenic α-processing of amyloid precursor protein (APP) even at 100 nM in human fibroblas.
- Shusen Wang, .et al. , Cell, 2024, Oct 31;187(22):6152-6164 PMID: 39326417
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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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α7 Positive Modulator
NS 1738 is a α7 positive allosteric modulator.- Spencer R. Pierce, .et al. , Biomolecules, 2023, 13(4), 698 PMID: 37189445
- Hugo R Arias, .et al. , Br J Pharmacol, 2022, Sep 9 PMID: 36082615
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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
- Cangrelor is a potent intravenous adenosine diphosphate-receptor antagonist
- Tasuku SAKAYORI, .et al. , Sysmex Journal International, 2024, Vol.34 No.1
- Satoru Koyanagi, .et al. , Nat Commun, 2016, 7: 13102 PMID: 27739425
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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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α7 nAChR agonist
PNU 282987 (PNU-282,987)is a drug that acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors.- Thorsang Weerakul, .et al. , ACS Pharmacol Transl Sci, 2026, 9 (1): 45-58 PMID: 41536290
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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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NMDA receptor antagonist
Memantine hydrochloride is an antagonist at the NMDA receptor, binding to the ion channel site. it was used in the treatment of Parkinsonism.- Xuefeng Hu, .et al. , Research Square, 2024, Apr 12
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gamma-secretase modulator
E 2012 is γ-secretase inhibitor.- Yesuvadian R, .et al. , Biochem Biophys Res Commun., 2014, May 16;447(4):590-5 PMID: 24747079
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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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P2X7 receptor antagonist
A 438079 Hcl is a competitive P2X7 receptor antagonist (pIC50 = 6.9 for the inhibition of Ca2+ influx in the human recombinant P2X7 cell line).- Zhihua Yi, .et al. , Front Pharmacol, 2018, 9: 593 PMID: 29950989
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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. -
acetylcholine receptor antagonist
Beperidium iodide shows a competitive antagonistic effect against acetylcholine receptor with a pA2 of 7.93. -
Glucosylceramide synthase inhibitor
Eliglustat is a specific and potent inhibitor of glucosylceramide synthase. -
P2X3 and P2X2/3 receptor antagonist
A-317491 sodium salt hydrate is a non-nucleotide P2X3 and P2X2/3 receptor antagonist, which inhibits calcium flux mediated by the receptors.

