Catalog No.
Product Name
Application
Product Information
Citations
-
γ-Secretase Modulator
PF-06648671 is an orally active γ-secretase modulator that effectively penetrates the blood-brain barrier. This compound demonstrates the ability to reduce levels of amyloid-beta peptides Aβ42 and Aβ40, while concurrently increasing Aβ37 and Aβ38 in vitro. PF-06648671 is valuable for research applications focused on Alzheimer’s disease and the modulation of amyloid processing pathways. -
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. -
γ-secretase Modulator
RO7185876 is a selective gamma-secretase modulator that plays a crucial role in the regulation of amyloid precursor protein processing. This compound is primarily investigated for its potential in Alzheimer's disease research, where it may help reduce the production of amyloid-beta peptides. Its unique mechanism of action positions RO7185876 as a valuable tool for studying the pathophysiology of Alzheimer's and exploring therapeutic options. -
γ-secretase Modulator
GSM-1 is a potent γ-secretase modulator that directly targets the transmembrane domain (TMD) 1 of presenilin 1 (PS1). By modulating γ-secretase activity, GSM-1 influences the processing of amyloid precursor protein (APP), making it valuable in Alzheimer's disease research. This compound can be utilized to investigate mechanisms of amyloid-beta peptide generation and potential therapeutic strategies for neurodegenerative disorders. -
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 Modulator
FRM-024 is a potent γ-secretase modulator designed for central nervous system applications. It selectively alters the activity of γ-secretase, a critical enzyme involved in the pathogenesis of familial Alzheimer’s disease. This compound has demonstrated the ability to influence amyloid precursor protein processing, making it a valuable tool for research focused on Alzheimer’s therapeutics and disease mechanisms. -
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 Modulator
(-)-FRM-024 is a potent γ-secretase modulator that effectively penetrates the central nervous system. This compound is instrumental in Alzheimer’s disease research, facilitating the study of amyloid precursor protein processing and its implications in neurodegeneration. Its ability to modulate γ-secretase activity makes it a valuable tool for exploring therapeutic interventions in Alzheimer's pathology. -
γ-Secretase Modulator
γ-Secretase modulator 4 is a potent modulator of the γ-secretase enzyme, characterized by its ability to effectively reduce Aβ42 peptide levels with IC50 values of 0.014 μM in human samples and 0.017 μM in mouse samples. This compound has significant implications in Alzheimer's research, particularly in the study of amyloid-beta production and the related pathophysiology. Its mechanism of action makes it a valuable tool for investigations into therapeutic strategies targeting Alzheimer's disease. -
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. -
Gamma-Secretase Modulator
Gamma-Secretase Modulator 1 Hydrochloride acts as a modulator of gamma-secretase, a crucial enzyme implicated in the pathogenesis of Alzheimer's disease. This compound is designed to influence the processing of amyloid precursor protein (APP), ultimately affecting the production of amyloid-beta peptide. Its potential applications include studying the modulation of amyloid-beta levels and investigating therapeutic strategies for Alzheimer's disease and related neurodegenerative disorders. -
γ-secretase Modulator
Nivegacetor is a potent γ-secretase modulator that plays a critical role in the modulation of amyloid precursor protein processing. By influencing the activity of γ-secretase, Nivegacetor is valuable for research into Alzheimer's disease and other neurodegenerative conditions. Its ability to alter the production of amyloid-beta peptides makes it a useful tool for exploring therapeutic pathways and understanding the molecular mechanisms underlying these diseases. -
γ-Secretase Modulator
Aβ42-IN-1 is a potent γ-secretase modulator (GSM) designed to target the enzymatic cleavage of amyloid precursor protein, effectively lowering amyloid-beta 42 (Aβ42) levels. With an IC50 value of 0.091 μM, Aβ42-IN-1 demonstrates significant inhibition of Aβ42 production while avoiding CYP3A4 inhibition, indicating a favorable safety profile. Its sustained pharmacokinetic properties make it a valuable tool for research into Alzheimer's disease and related neuropathologies. This compound holds promise for exploring therapeutic strategies aimed at modulating γ-secretase activity in neurodegenerative disorders. -
γ-Secretase Modulator
Aβ42-IN-1 free base is a potent γ-secretase modulator that exhibits high oral bioavailability and significant brain penetration. This compound effectively lowers Aβ42 levels with an IC50 of 0.091 μM, demonstrating substantial reduction of brain Aβ42 levels in murine models. Aβ42-IN-1 free base holds considerable potential for therapeutic applications in Alzheimer's disease research. -
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 Modulator
γ-Secretase modulator 10 is a selective modulator of the γ-secretase enzyme complex. It influences the cleavage of amyloid precursor protein (APP), thereby altering the production of amyloid β peptides associated with Alzheimer's disease pathogenesis. This compound is valuable for research applications focused on neurodegenerative diseases and therapeutic strategies aimed at modulating γ-secretase activity. -
γ-Secretase Modulator
γ-Secretase modulator 14 is a selective modulator of the γ-secretase complex, influencing the cleavage of amyloid precursor protein (APP). This compound exhibits potential in Alzheimer's disease research by altering the production of amyloid-beta peptides. Its utility extends to investigating the mechanisms underlying neurodegenerative disorders and developing novel therapeutic strategies aimed at modulating γ-secretase activity. -
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 Modulator
BPN-15606 besylate is a potent orally active γ-secretase modulator (GSM) that effectively reduces the production of Aβ42 and Aβ40 peptides in SHSY5Y neuroblastoma cells, exhibiting IC50 values of 7 nM and 17 nM, respectively. This compound has demonstrated the ability to lower Aβ42 and Aβ40 levels in the central nervous system of rodent models. Additionally, BPN-15606 besylate features favorable pharmacokinetic and pharmacodynamic properties, including good bioavailability, optimal half-life, and manageable clearance rates, making it valuable for Alzheimer's disease research and neurodegenerative studies. -
γ-secretase Modulator
BMS-932481 is a potent γ-secretase modulator that demonstrates selective reduction of β-amyloid peptides Aβ1-42 and Aβ1-40, exhibiting IC50 values of 6.6 nM and 25.3 nM, respectively. This compound is valuable for research into Alzheimer's disease and mechanisms of amyloid plaque formation, offering insights into potential therapeutic strategies targeting γ-secretase activity. -
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 Modulator
γ-Secretase modulator 12 is a selective modulator of γ-secretase, specifically designed to reduce levels of amyloid-β42 (Aβ42) with an IC50 of 0.39 µM. This compound is valuable for investigating Alzheimer's disease mechanisms and potential therapeutic interventions. Additionally, γ-secretase modulator 12 demonstrates favorable pharmacokinetics with a good brain-to-plasma ratio (Kp, brain = 0.72) in murine models, making it suitable for in vivo studies. -
γ-Secretase Modulator
γ-Secretase modulator 11 hydrochloride is a potent modulator of γ-secretase with an IC50 of 0.029 µM, demonstrating oral bioavailability. It effectively reduces brain Aβ42 levels, a critical factor in Alzheimer's disease pathology. Furthermore, this compound has shown the capability to improve cognitive deficits in Alzheimer's disease model mice, making it valuable for research into therapeutic strategies targeting Alzheimer's disease. -
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 Modulator
BMS-869780 is an orally active γ-secretase modulator that selectively regulates γ-secretase activity to modify the production profile of β-amyloid proteins. It alters the relative levels of specific β-amyloid subtypes while not inhibiting the overall production of β-amyloid proteins. Additionally, BMS-869780 demonstrates a synergistic effect when used in combination with acidic γ-secretase modulators, resulting in a reduction of total β-amyloid production in cell cultures. This compound is valuable for research into Alzheimer’s disease and related neurodegenerative disorders. -
γ secretase Modulator
PF-06442609 is an orally active γ secretase modulator that effectively inhibits amyloid-beta (Aβ42) production with an IC50 of 6 nM. This compound demonstrates excellent brain penetration, making it suitable for research in neurodegenerative disease models, particularly Alzheimer's disease. Its modulatory effects on γ secretase activity provide valuable insights into the mechanistic understanding of amyloid plaque formation and associated pathologies. -
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
LY-411575 (isomer 1) is a potent γ-secretase inhibitor that selectively modulates the enzyme's activity. This compound is primarily utilized in the investigation of Alzheimer’s disease pathogenesis by reducing the production of harmful amyloid-beta peptides. Its mechanism of action allows for a deeper understanding of γ-secretase's role in cellular signaling and pathology, making it a valuable tool in neurological research. -
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. -
CK1δ/1ε Inhibitor
SR-2890 is a highly selective ATP-competitive inhibitor of casein kinase 1 delta (CK1δ) and 1 epsilon (CK1ε), exhibiting IC50 values of 4 nM and 44 nM, respectively. This compound effectively inhibits the serine/threonine kinase activity of CK1δ and has demonstrated antiproliferative effects against human A375 melanoma cells. Additionally, SR-2890 has shown potential utility in research related to melanoma and in studying diseases associated with CK1δ/ε, such as Alzheimer's disease, due to its favorable in vivo pharmacokinetic properties and metabolic stability. -
Hedgehog Inhibitor
TPB15 is a potent inhibitor of Hedgehog (Hh) signaling, specifically targeting Smoothened (Smo). This compound effectively induces cell cycle arrest and apoptosis in MDA-MB-468 breast cancer cells by blocking Smo translocation into cilia and reducing the expression of Smo protein and mRNA. Additionally, TPB15 downregulates glioma-associated oncogene 1 (Gli1), a key downstream regulator. TPB15 demonstrates significant anti-tumor activity with a favorable toxicity profile, making it a valuable tool for cancer research focused on Hedgehog pathway modulation. -
Pro-Apoptotic Peptide
CIGB-300 is a pro-apoptotic peptide that targets casein kinase 2 (CK2). It exhibits potent anticancer activity by disrupting CK2 phosphorylation, leading to apoptosis in various tumor cell lines. This compound is valuable for cancer research, particularly in studies focused on apoptosis and CK2 modulation. -
p38/CK1 Inhibitor
Casein kinase 1δ-IN-29 is a potent inhibitor of p38α and casein kinase 1, demonstrating IC50 values of 0.041 µM for p38α, 0.005 µM for CK1δ, and 0.447 µM for CK1ε. This compound effectively interrupts the cell cycle at the subG1 phase and induces apoptosis in AC1-M88 cells. It serves as a valuable tool in research applications focused on cell cycle regulation and apoptosis pathways. -
β-catenin Inhibitor
β-catenin-IN-9 is a potent inhibitor of β-catenin, a key regulator in various signaling pathways. It has been shown to induce apoptosis and cell cycle arrest, while effectively inhibiting migration, invasion, and epithelial-mesenchymal transition (EMT) in colorectal cancer cells. Additionally, β-catenin-IN-9 suppresses the transcription of β-catenin and vimentin, leading to significant reductions in β-catenin protein levels. This reagent is valuable for research focused on colorectal cancer and related signaling pathways. -
Hsp90-Cdc37 PPI Inhibitor
Hsp90-Cdc37-IN-4 is a selective inhibitor of the Hsp90-Cdc37 protein-protein interaction (PPI). This compound disrupts the interaction by inhibiting casein kinase 2 (CK2), leading to reduced phosphorylation of Cdc37 at Serine 13. In cellular assays, Hsp90-Cdc37-IN-4 has been shown to induce G0/G1 cell cycle arrest and activate apoptotic pathways via the mitochondria. Additionally, it exhibits significant anti-breast cancer properties, making it a valuable tool in cancer research. -
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. -
CK1ε Inhibitor
Orobol is a selective inhibitor of Casein Kinase 1 epsilon (CK1ε) with demonstrated anti-skin-aging and anti-obesity effects. It targets multiple kinases, including VEGFR2, MAP4K5, MNK1, MUSK, TOPK, and TNIK, exhibiting inhibitory activity with IC50 values ranging from 1.24 to 4.45 μM. Additionally, Orobol inhibits various phosphoinositide 3-kinase (PI3K) isoforms, specifically showing activity with IC50 values between 3.46 and 5.27 μM for PI3K α/β/γ/K/δ. These properties make Orobol valuable for investigating signaling pathways related to cellular growth, metabolism, and aging. -
Fyn/GSK-3β Inhibitor
Fyn-IN-1 is a selective inhibitor of Fyn and GSK-3β, demonstrating IC50 values of 0.044 μM and 0.61 μM, respectively. This compound effectively downregulates the expression of the pro-inflammatory enzyme iNOS, making it a valuable tool in studying neuroinflammatory processes. Fyn-IN-1 is particularly relevant for research focused on neurodegenerative diseases, providing insights into potential therapeutic interventions. -
DYRK1A/GSK3β Inhibitor
GNF4877 is a potent dual inhibitor of DYRK1A and GSK3β, demonstrating IC50 values of 6 nM and 16 nM, respectively. This inhibition results in the blockade of nuclear export of nuclear factor of activated T-cells (NFATc) and promotes β-cell proliferation, with an EC50 of 0.66 μM in mouse β (R7T1) cells. GNF4877 serves as a valuable tool in research related to diabetes and T-cell signaling pathways. -
GSK-3β/FYN Inhibitor
ARN25068 is a sub-micromolar inhibitor targeting the protein kinases GSK-3β, FYN, and DYRK1A. It plays a significant role in modulating tau hyperphosphorylation, which is implicated in neurodegenerative diseases. This compound is valuable for research applications focused on neurobiology and pathology related to tau protein and related neurodegenerative processes. -
Casein Kinase/DYRK/TNIK Inhibitor
ON 108600 is a potent inhibitor of casein kinase 2 (CK2), TYRK1 (DYRK), and TNIK, demonstrating IC50 values of 0.016 μM against DYRK1A, 0.007 μM against DYRK2, 0.05 μM against CK2α1, 0.005 μM against CK2α2, and 0.005 μM against TNIK. This compound exhibits promising antitumor activity, making it a valuable tool for research applications focused on cancer biology, signaling pathways, and kinase inhibition studies. Its specificity for these kinases positions ON 108600 as a critical reagent for investigating therapeutic strategies targeting kinase-related diseases. -
GSK3 Inhibitor
GSK3-IN-10 is a potent inhibitor of glycogen synthase kinase 3 (GSK3) isoforms α and β, demonstrating IC50 values of 1.0 nM and 2.0 nM, respectively. This compound effectively inhibits the activation of β-catenin, thereby promoting neuronal survival and providing a protective effect against endoplasmic reticulum stress. GSK3-IN-10 is valuable for research applications focused on neuroprotection and cellular stress response mechanisms.
