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Catalog No.
Product Name
Application
Product Information
Citations
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Gamma-secretase inhibitor
BMS-708163 is an oral gamma secretase inhibitor designed for selective inhibition of amyloid beta synthesis. -
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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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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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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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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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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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 . -
γ-Secretase Inhibitor
BMS 433796 is a γ-secretase inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer's disease. -
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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gamma-secretase inhibitor
Flurbiprofen Axetil is potentnon-steroidal anti-inflammatory drug(NSAID). -
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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γ-secretase inhibitor
MRK 560 is an orally bioavailable gamma-secretase inhibitor with the ability to markedly reduce Abeta peptide in the brain and CSF of the rat and confirm the utility of the rat for assessing the effects of gamma-secretase inhibitors on central nervous system Abeta(40) levels in vivo. -
β-secretase/BACE1 inhibitor
Verubecesta is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor. -
γ-Secretase inhibitor
Z-Ile-Leu-aldehyde is a potent gamma-Secretase inhibitor; Notch signaling inhibitor. -
gamma secretase inhibitor
BMS-906024 is an oral and selective gamma secretase inhibitor (GSI) that is a small molecule Notch inhibitor. -
δ-Secretase Inhibitor
δ-Secretase inhibitor 11 is a potent and selective inhibitor targeting δ-secretase, displaying an IC50 of 0.7 μM. This compound effectively interacts with both the active and allosteric sites of δ-secretase, resulting in the attenuation of tau and amyloid precursor protein cleavage. Its oral bioavailability and blood-brain barrier penetration make it suitable for in vivo studies, particularly in transgenic mouse models. δ-Secretase inhibitor 11 is a valuable tool for Alzheimer's disease research, facilitating investigations into the mechanisms underlying synaptic dysfunction and cognitive impairments. -
γ-Secretase Inhibitor I
Z-LLNle-CHO is a γ-secretase inhibitor that effectively disrupts the Akt-mediated pro-survival signaling pathway, leading to caspase activation and ROS-dependent apoptosis. This compound is instrumental in cancer research, particularly in the studies of breast cancer and leukemia, where inhibiting γ-secretase activity may provide insights into therapeutic strategies. -
γ-secretase Inhibitor
Nirogacestat dihydrobromide is a selective, noncompetitive inhibitor of γ-secretase, with a reported IC50 of 6.2 nM. This compound effectively inhibits Notch signaling, making it a valuable tool for studying Notch receptor-dependent cancers while minimizing gastrointestinal toxicity. It is particularly useful in research focused on the role of γ-secretase in cancer biology and therapeutic development. -
γ-secretase Inhibitor
MRK 003 is a selective and orally bioavailable inhibitor of γ-secretase. It demonstrates significant reduction of Aβ peptide production in the brain in vivo, making it a valuable tool for Alzheimer's disease research. Additionally, MRK 003 induces caspase-dependent apoptosis and inhibits tumor cell proliferation both in vitro and in vivo, supporting its potential applications in cancer research. -
γ-Secretase Inhibitor
EVP-0015962 is a potent γ-secretase inhibitor that effectively penetrates the blood-brain barrier, exhibiting an IC50 value of 3.9 μM. By modulating the γ-secretase-mediated cleavage of amyloid precursor protein, EVP-0015962 decreases the production of Aβ42 while increasing Aβ38 levels. This compound has demonstrated efficacy in reducing amyloid aggregates, mitigating amyloid plaque formation, and lowering inflammatory markers in mouse models, thereby enhancing cognitive function. EVP-0015962 serves as a valuable tool in Alzheimer's disease research. -
γ-secretase Inhibitor
JNJ-40418677 is a potent orally active inhibitor of γ-secretase, capable of crossing the blood-brain barrier. It effectively inhibits the production of Aβ42 and the activity of NS2B-NS3 protease, with IC50 values of 200 nM and 3.9 μM, respectively. This compound exhibits favorable biological tolerance and is suitable for research applications related to Alzheimer's disease. -
γ-secretase Inhibitor
Sulindac sulfide is a noncompetitive inhibitor of γ-secretase, exhibiting an IC50 of 20.2 μM for γ42-secretase activity. This compound plays a crucial role in research involving Alzheimer's disease and other neurodegenerative conditions by modulating the processing of amyloid precursor protein. Its ability to inhibit γ-secretase makes it a valuable tool for studies focused on reducing amyloid-beta peptide formation and investigating related signaling pathways. -
γ-secretase Inhibitor
ELND 006 is a selective γ-secretase inhibitor that effectively reduces amyloid beta (Aβ) generation while preserving Notch signaling pathways. Developed with a focus on metabolic stability, this compound has shown significant efficacy in lowering Aβ levels both in vitro and in vivo during preclinical studies. ELND 006, alongside its structural analog ELND 007, has advanced into human clinical trials, indicating its potential therapeutic applications in Alzheimer's disease research and treatment. -
gamma-Secretase Inhibitor
Gamma-secretase modulator 6 is a gamma-secretase inhibitor that effectively reduces the secretion of Aβ42 in HEK cells stably expressing amyloid precursor protein (APP), with a pIC50 value of 8.1. This compound plays a crucial role in the study of Alzheimer's disease by modulating gamma-secretase activity, thereby influencing amyloid plaque formation. It is a valuable tool for researchers exploring therapeutic strategies targeting amyloid pathology in neurodegenerative disorders. -
γ-secretase/Aβ42 Inhibitor
Amyloid-β-IN-2 is a selective γ-secretase inhibitor that effectively reduces the secretion of Aβ42 in H4 cells, exhibiting an EC50 value of 226 nM. This compound demonstrates potential for research applications in Alzheimer's disease and other conditions associated with Aβ deposition. Its ability to modulate γ-secretase activity makes it a valuable tool for studying the mechanisms underlying amyloid-related pathologies. -
γ-secretase/Aβ42 Inhibitor
Amyloid-β-IN-3 is a selective inhibitor of γ-secretase that effectively reduces the secretion of Aβ42 in H4 cells, exhibiting an EC50 value of 148 nM. By modulating γ-secretase catalytic activity, it decreases Aβ42 production and helps mitigate the neurotoxicity associated with amyloid deposition. This compound shows potential for research applications in Alzheimer's disease (AD) studies. -
γ-secretase Inhibitor
ELN318463 is a selective inhibitor of γ-secretase, targeting the amyloid precursor protein (APP). It demonstrates differential inhibition of presenilin 1 (PS1) and presenilin 2 (PS2) γ-secretase complexes, with EC50 values of 12 nM and 656 nM, respectively, showcasing a 51-fold greater selectivity for PS1. This compound is primarily utilized in research focused on Alzheimer's disease and related neurodegenerative disorders, making it a valuable tool for studies investigating APP processing and amyloid plaque formation. -
γ-secretase Inhibitor
(9R)-RO7185876 is a selective inhibitor of γ-secretase, targeting the cleavage of amyloid precursor protein. This compound significantly reduces the secretion of Aβ42 peptides, making it a valuable tool for research on Alzheimer's disease and related disorders, such as cerebral amyloid angiopathy and multi-infarct dementia. Additionally, (9R)-RO7185876 may be utilized to investigate conditions associated with amyloid deposition, including dementia pugilistica and Down syndrome. -
γ-secretase Inhibitor
MK-0752 sodium is a potent, orally bioavailable inhibitor of γ-secretase, exhibiting a dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. This compound effectively crosses the blood-brain barrier and demonstrates the ability to decrease newly generated central nervous system Aβ levels in vivo. MK-0752 sodium is primarily utilized in research on Alzheimer’s disease and other neurodegenerative disorders linked to amyloid-beta pathology. -
γ-secretase Inhibitor
γ-Secretase modulator 11 functions as a potent γ-secretase inhibitor, effectively reducing levels of amyloid beta 42 in vitro and demonstrating significant brain penetration. This compound exhibits minimal inhibition of cytochrome P450 enzymes, highlighting its selective profile. Additionally, γ-secretase modulator 11 has shown considerable efficacy in alleviating cognitive deficits in Alzheimer's disease model mice, making it a valuable tool for research in neurodegenerative disorders. -
γ-Secretase Inhibitor
GSI-18 is a potent γ-secretase inhibitor that disrupts Notch signaling, contributing to its anticancer properties. This compound effectively inhibits the attachment-free growth of pancreatic cancer cells, making it valuable for research into cancer biology and therapeutic interventions. Its mechanism of action offers insights into the regulation of cell proliferation and differentiation in oncogenic contexts. -
γ-secretase Inhibitor
ELND 007 is a selective γ-secretase inhibitor that primarily targets the reduction of amyloid beta (Aβ) generation while minimizing inhibition of Notch signaling. It demonstrates significant biological activity in both in vitro and in vivo settings, effectively decreasing Aβ levels. This compound has shown potential therapeutic benefits for Alzheimer’s disease, particularly as evidenced by reductions in Aβ levels observed in cerebrospinal fluid during human clinical trials, following a strategic emphasis on metabolic stability and chirality in its development. -
γ-secretase Inhibitor
γ-Secretase-IN-2 is a potent inhibitor of γ-secretase, demonstrating an IC50 of 0.06 nM. This compound is instrumental in researching Alzheimer's disease, providing insights into the enzymatic processes involved in neurodegeneration. Its high efficacy makes it a valuable tool for studying the pathophysiology of Alzheimer's and exploring potential therapeutic strategies. -
γ-secretase Inhibitor
LY3056480 is a potent γ-secretase inhibitor that targets Notch signaling pathways. This compound has demonstrated efficacy in enhancing recovery from mild to moderate sensorineural hearing loss, while exhibiting a favorable safety profile. Additionally, intratympanic administration of LY3056480 has been shown to promote hair cell regeneration and contribute to partial auditory recovery in mammalian models, making it a valuable tool for research in hearing restoration and neurodegenerative studies. -
γ-secretase Inhibitor
III-31-C is a hydroxyethyl urea-based inhibitor of γ-secretase. It demonstrates potent inhibition of amyloid-beta (Aβ) production, with an IC50 value of 10 nM in a cell-free γ-secretase assay and 200 nM in APP-transfected cells. This compound is relevant for research focused on Alzheimer's disease and offers valuable insights into the modulation of Aβ metabolism. -
γ-secretase Inhibitor
LY-411575 (isomer 2) is a potent inhibitor of γ-secretase, an enzyme involved in the cleavage of amyloid precursor protein and a key player in the pathogenesis of Alzheimer's disease. This compound has been shown to effectively reduce the production of amyloid-beta peptides, making it valuable for research into therapeutic strategies for neurodegenerative disorders. Its selective inhibition of γ-secretase also facilitates the study of its role in cellular signaling and development. -
γ-secretase Inhibitor
GSI-136 is a potent inhibitor of γ-secretase, exhibiting an IC50 of 3 nM. This compound effectively reduces Aβ40 levels in diethylamine-extracted brain homogenates from C57BL/6 mice in a dose-dependent manner. GSI-136 serves as a valuable tool in medicinal chemistry and Alzheimer’s disease research, aiding in the exploration of therapeutic strategies targeting amyloid-beta production. -
γ-secretase Inhibitor
LY-411575 (isomer 3) is a potent inhibitor of γ-secretase, an enzyme complex involved in the proteolytic processing of various transmembrane proteins, including amyloid precursor protein (APP). This compound is utilized in research studying Alzheimer's disease and other conditions associated with aberrant Notch signaling. Its ability to modulate γ-secretase activity makes it a valuable tool for investigating the therapeutic potential of targeting this pathway. -
γ-secretase Inhibitor
ELN318463 racemate is a selective γ-secretase inhibitor targeting the amyloid precursor protein (APP). It demonstrates differential inhibition of presenilin (PS1) and PS2-comprised γ-secretase, with EC50 values of 12 nM for PS1 and 656 nM for PS2, indicating a 51-fold selectivity for PS1. This compound is useful in research applications focused on Alzheimer's disease and the modulation of amyloid beta peptide production.
