Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Multitarget Inhibitor
SSZ is a multitarget inhibitor that engages multiple pathological mechanisms associated with Alzheimer's disease (AD). It inhibits key enzymes including acetylcholinesterase, butyrylcholinesterase, β-site amyloid precursor protein cleavage enzyme 1 (BACE1), and γ-secretase. Research demonstrates that SSZ enhances cognitive function and provides neuroprotective effects in murine models of Alzheimer's disease, making it a valuable tool for studying therapeutic strategies in neurodegenerative disorders. -
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. -
AChE/IL-6 Inhibitor
Y13g is a potent dual inhibitor of acetylcholinesterase (AChE) and interleukin-6 (IL-6). By targeting these pathways, Y13g demonstrates significant potential in addressing memory deficits associated with Alzheimer’s Disease. In preclinical studies, Y13g effectively reverses memory impairment induced by STZ and exhibits histopathological profiles akin to those of healthy specimens, making it a valuable tool for research in neurodegeneration and inflammatory responses.
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BChE/p38-α MAPK Inhibitor
BChE/p38-α MAPK-IN-1 is a selective dual inhibitor targeting human butyrylcholinesterase (BChE) with an IC50 of 772 nM and p38 α MAPK with an IC50 of 191 nM. This compound significantly reduces the production of pro-inflammatory cytokines such as IL-1β, IL-6, IL-8, and TNF-α in cellular models. BChE/p38-α MAPK-IN-1 demonstrates the potential to ameliorate cognitive impairments induced by scopolamine and alleviate spatial learning deficits in LPS-treated mice, making it a valuable tool for studying Alzheimer's disease by addressing cholinergic deficits and neuroinflammation. -
α7nAChR Activator
Lemairamin, an α7nAChR activator, is a hydroxylamine compound derived from the pericarps of Zanthoxylum species. This compound is known to stimulate the expression of anti-inflammatory cytokine IL-10 and proopiomelanocortin (POMC), while concurrently reducing Akt activity. Lemairamin has demonstrated efficacy in attenuating dextran sulfate sodium (DSS)-induced intestinal inflammation and alleviating pain hypersensitivity, making it a valuable reagent for research in inflammation and pain modulation. -
P2Y14R Antagonist
P2Y14R Antagonist 4 is a potent oral antagonist of the P2Y14 receptor, exhibiting an IC50 value of 5.6 nM, indicating high binding affinity. This compound demonstrates anti-inflammatory activity by effectively reducing the release of proinflammatory cytokines, such as IL-1β, IL-6, and TNF-α, in response to LPS stimulation. P2Y14R Antagonist 4 is valuable for research applications in inflammation and immune response modulation. -
P2 receptor/NAADP receptor Antagonist
PPADS is a reversible competitive antagonist of P2X receptors, specifically targeting P2X1 and P2X3, with IC50 values of 68 nM and 214 nM, respectively. It demonstrates significant anti-nociceptive effects in mouse models of neuropathic pain and inhibits pro-inflammatory cytokines such as IL-1β and IL-6, as well as nitric oxide synthases. Additionally, PPADS effectively blocks ATP-mediated inward currents in recombinant rat P2X receptors and reduces contractions in rabbit bladder detrusor muscle induced by purinergic nerve stimulation. This compound is valuable for research on neuropathic pain mechanisms and related therapeutic interventions. -
P2X7R Selective Allosteric Antagonist
SMW139 is a selective allosteric antagonist of the P2X7 receptor, demonstrating a Ki value of 32 nM for human P2X7R. This compound exhibits potential in modulating inflammatory responses and has applications in research related to Alzheimer's disease and multiple sclerosis. With a half-life of 47 minutes in rat liver microsomes, SMW139 serves as a valuable tool for investigating the therapeutic effects on P2X7R-mediated pathways. -
AChE/ACP/ALP Inhibitor
Trimyristin is a potent inhibitor of acetylcholinesterase (AChE) as well as acid and alkaline phosphatase (ACP/ALP). It has demonstrated significant inhibitory effects on AChE, ACP, and ALP activities in the nervous tissue of Lymnaea acuminata, with IC50 values of 0.11 mM, 0.16 mM, and 0.18 mM, respectively. This compound is valuable for research applications focused on neurological pathways and enzyme activity modulation. -
CaMKP/CaMKP-N Inhibitor
CaMKP Inhibitor Sodium targets Ca2+/neutral protein-dependent protein kinase (CaMKP) and its nuclear variant (CaMKP-N), exhibiting IC50 values of 6.4 μM and 6.6 μM, respectively. This compound suppresses CaMKP-mediated phospho-CaMKI hydrolysis while leaving protein phosphatases PP2C and calcineurin unaffected. CaMKP plays a critical role in various cellular processes involving serine/threonine phosphorylation, making this inhibitor valuable for research into calcium-dependent signaling pathways and protein regulation. -
Stable Isotope
Trimyristin-d15 is a deuterium-labeled derivative of Trimyristin, a naturally occurring compound extracted from Myristica fragrans. This reagent effectively inhibits acetylcholinesterase (AChE), as well as acid and alkaline phosphatase (ACP/ALP) activities in the nervous tissue of Lymnaea acuminata, with IC50 values of 0.11 mM, 0.16 mM, and 0.18 mM, respectively. Trimyristin-d15 serves as a valuable tool for biochemical research and enzyme activity studies, particularly in exploring the mechanisms of neurotoxicity and molluscicidal action. -
α4β2 nAChR Agonist
TC-2559 free base is an agonist of the α4β2 nicotinic acetylcholine receptor (nAChR), demonstrating an EC50 value of 0.18 μM. It exhibits reduced potency on β4-containing nAChR subtypes, such as α2β4, α4β4, and α3β4, with EC50 values between 10-30 µM. Research indicates that TC-2559 enhances dopamine neuron activity in the ventral tegmental area, which may influence excitability and aggression. Additionally, it possesses anti-inflammatory effects via STAT3 inhibition, proving beneficial in models of mechanical allodynia and cognitive deficits. This compound is useful for investigations into nerve pain and related neurological conditions. -
AChE Inhibitor
Propoxur is a reversible competitive inhibitor of acetylcholinesterase (AChE) that effectively penetrates the blood-brain barrier. This compound induces neurotoxicity by inhibiting AChE activity, resulting in the accumulation of acetylcholine, thereby causing neurological dysfunction. In addition, Propoxur promotes MMP-2 expression and enhances tumor cell migration and invasion through the generation of reactive oxygen species (ROS) and the activation of the ERK/Nrf2 signaling pathway. It is also utilized as a carbamate insecticide for managing pests in turf, forestry, and household environments. -
Peptide
PHF6 (VQIVYK) is a peptide that facilitates the self-assembly and aggregation of the full-length tau protein, specifically targeting the third microtubule-binding repeat region of tau. This peptide is instrumental in studies of tau pathology associated with neurodegenerative diseases, particularly in understanding the mechanisms underlying tau aggregation and its implications in tau-related disorders. Its unique structure makes it a valuable tool for investigating tau fibrillogenesis and potential therapeutic interventions. -
CaMK Substrate
Syntide 2 is a substrate peptide for calcium/calmodulin-dependent protein kinase II (CaMKII) that demonstrates selective inhibition of the gibberellin (GA) signaling pathway. By targeting this pathway, Syntide 2 facilitates the investigation of mechanisms underlying plant hormone responses while preserving the activity of other regulatory events, such as those mediated by abscisic acid. This reagent is valuable for studies related to cellular signaling and hormone regulation in plant biology. -
CaMKII Inhibitor
Autocamtide-2-related inhibitory peptide is a selective inhibitor of Calcium/Calmodulin-dependent protein kinase II (CaMKII), exhibiting an IC50 value of 40 nM. This peptide effectively modulates CaMKII activity, making it a valuable tool for studying calcium signaling pathways and their implications in various physiological and pathological processes. Its high specificity and potency simplify the investigation of CaMKII-related mechanisms in cellular signaling research. -
COX Inhibitor
Indomethacin farnesil is a prodrug of indomethacin, primarily targeting cyclooxygenase (COX) enzymes. This potent, blood-brain barrier-permeable inhibitor exhibits nonselective activity against COX-1 and COX-2, with IC50 values of 18 nM and 26 nM, respectively. Indomethacin farnesil has been shown to disrupt autophagic flux by impairing lysosomal function, making it useful for investigating inflammatory pathways and autophagy-related processes in research applications. -
Tau ATTEC
MRL828 is a Tau pathology-binding compound that employs the ATTEC technology to selectively target aggregated tau proteins for degradation via the autophagic lysosomal pathway. This reagent effectively decreases intracellular tau aggregates while promoting the secretion of tau from cells. Its unique mechanism makes MRL828 a valuable tool for research on tau-related pathologies and neurodegenerative diseases. -
Sesquiterpene Lactone
Lactupicrin, a sesquiterpene lactone, primarily targets acetylcholinesterase (AChE), exhibiting an inhibitory activity with an IC50 of 150.3 μM. This compound demonstrates notable analgesic, sedative, and antimalarial effects, alongside its atheroprotective properties. Lactupicrin is an orally active bitter compound, making it valuable for research applications focused on neuropharmacology and cardiovascular health. -
GABA(A) Receptor Antagonist/σ1 Receptor Agonist
Dehydroepiandrosterone sulfate (DHEA sulfate) functions as a GABA(A) receptor antagonist and a σ1 receptor agonist. This neurosteroid, primarily secreted by the adrenal gland, is capable of partially penetrating the blood-brain barrier. It inhibits GABA(A) receptor-mediated chloride influx while enhancing NMDA receptor activity via σ1 receptor interaction, displaying anti-inflammatory and antidepressant properties. DHEA sulfate is relevant for research in neuroprotection, depression, post-traumatic stress disorder (PTSD), and Alzheimer’s disease, and may serve as a biomarker for cardiovascular disease mortality due to its correlation with mortality rates. -
GABA(A) Receptor Antagonist/σ1 Receptor Agonist
Dehydroepiandrosterone sulfate sodium (DHEA sulfate) primarily acts as a non-competitive GABA(A) receptor antagonist and σ1 receptor agonist. This neurosteroid, predominantly secreted by the adrenal gland, has demonstrated significant biological activities, including enhancing NMDA receptor function and exerting anti-inflammatory and antidepressant effects. DHEA sulfate sodium can penetrate the blood-brain barrier, making it valuable in research applications related to neuroprotection, neurite growth regulation, and neuropsychiatric disorders such as depression, post-traumatic stress disorder (PTSD), and Alzheimer's disease. Additionally, it may serve as a biomarker for cardiovascular disease mortality, with its levels inversely correlated with mortality rates. -
COX-2 Inhibitor/PPAR-γ Activator
Zaltoprofen sulfoxide is a selective COX-2 inhibitor with an IC50 of 45.38 nM, as well as a PPAR-γ activator. This compound effectively inhibits NF-κB and MAPK inflammatory signaling pathways, making it a valuable tool in the study of inflammation and acute lung injury models. It is particularly relevant for research focused on LPS-induced acute lung injury. -
AChE/BChE Inhibitor
Epiberberine chloride is an alkaloid derived from Coptis chinensis, functioning primarily as a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with IC50 values of 1.07 μM and 6.03 μM, respectively. This compound also serves as a non-competitive inhibitor of BACE1, with an IC50 of 8.55 μM. In addition to its cholinesterase inhibition, Epiberberine chloride exhibits antioxidant properties, demonstrated by its ability to scavenge peroxynitrite (IC50 of 16.83 μM), suggesting a potential protective role in Alzheimer’s disease research. Furthermore, it inhibits the early differentiation of 3T3-L1 preadipocytes and downregulates key signaling pathways, indicating its relevance in studies on diabetes. -
COX-2 Inhibitor
Hexahydrocurcumin is a selective, orally active inhibitor of cyclooxygenase-2 (COX-2), demonstrating significant potential in anti-inflammatory applications. As one of the primary metabolites of curcumin, it exhibits antioxidant and anticancer properties, making it relevant for research in various therapeutic areas. Its selectivity towards COX-2 over COX-1 highlights its potential for minimizing gastrointestinal side effects often associated with non-steroidal anti-inflammatory drugs (NSAIDs). -
Aβ/tau Aggregation Inhibitor
Aβ/tau aggregation-IN-4 is a potent inhibitor of amyloid-beta (Aβ) and tau aggregation. It effectively promotes the degradation of Aβ40 and Aβ42 with IC50 values of 2.151 μM and 3.622 μM, respectively. Additionally, Aβ/tau aggregation-IN-4 exhibits selective inhibition of acetylcholinesterase (AChE) with an IC50 of 5.56 μM, and inhibits monoamine oxidase A (MAO-A) and B (MAO-B) with IC50 values of 0.59 μM and 0.09 μM, respectively. This compound also reduces intracellular reactive oxygen species (ROS) levels, making it a valuable tool in Alzheimer's disease research. -
COX-2 Inhibitor
COX-2-IN-65 is a selective inhibitor of cyclooxygenase-2 (COX-2) with a reported IC50 of 10.24 μM. This compound exhibits antibacterial activity against Staphylococcus aureus and Escherichia coli, while also scavenging reactive oxygen species (ROS). COX-2-IN-65 is valuable for research applications focused on bacterial infections and inflammation pathways. -
MAO-B Inhibitor
MAO-B-IN-7 is a selective inhibitor of monoamine oxidase B (MAO-B) and acetylcholinesterase (AChE), demonstrating IC50 values of 41 nM for human AChE, 87 nM for electric eel AChE, and 0.3 μM for MAO-B. This compound is notable for its ability to penetrate the blood-brain barrier, making it suitable for central nervous system research. MAO-B-IN-7 has been shown to mitigate oxidative stress and neuroinflammation, supporting its potential applications in neurodegenerative disease studies. -
Insecticide
Methiocarb is an orally active carbamate insecticide primarily targeting acetylcholinesterase to induce cholinergic excitation. It exhibits dose-dependent toxic effects on various organisms, including notable oxidative stress through lipid peroxidation in liver, kidney, brain, and testicular tissues, while also altering reduced glutathione levels via reactive oxygen species generation. This compound is utilized for agricultural pest control and serves as a valuable research tool for studying oxidative stress-related cellular damage in mammalian models. -
NMDA Receptor Inhibitor
MN-05 is a dual neuroprotective and vasodilatory inhibitor of the NMDA receptor. By blocking calcium influx, it reduces free radical production and preserves mitochondrial membrane potential in cortical neurons exposed to glutamate. Additionally, MN-05 exhibits vasodilatory effects by dilating aortic rings in response to phenylephrine-induced contraction. This compound demonstrates protective properties against glutamate-induced neuronal injury in vitro, making it valuable for research in neurodegenerative diseases. -
Diallyl Tetrasulfide
Diallyl tetrasulfide functions as an antioxidant, primarily by mitigating cadmium-induced neurotoxicity and oxidative liver injury. This compound has demonstrated the ability to regulate acetylcholinesterase and adenosine triphosphatase activities, as well as protect against oxidative stress in the brain and liver tissues of animal models. Diallyl tetrasulfide also inhibits lipid peroxidation and reduces reactive oxygen species (ROS) production, thereby enhancing cell viability and decreasing apoptosis. It is a valuable reagent for studies focused on cadmium-induced cellular damage and neuroprotection. -
mAChR Ligand
Azacyclonol hydrochloride is a selective ligand for the M3 muscarinic acetylcholine receptor, demonstrating significant inhibition of proliferation in androgen-refractory cancer cell lines, including DU145 and PC-3. This compound exhibits notable anticancer activity, particularly in A549 human lung cancer cells, by inhibiting NOX-derived reactive oxygen species. Additionally, Azacyclonol hydrochloride has shown antitumor effects in xenografted chorioallantoic membrane models. Beyond its anticancer applications, it is also explored for its potential in the treatment of chronic schizophrenia. -
Pancreatic Lipase/Acetylcholinesterase/Glutamic-oxaloacetic Transaminase 1/Alpha-glucosidase Inhibitor
Aspulvinone H is a potent inhibitor targeting pancreatic lipase, acetylcholinesterase, glutamic-oxaloacetic transaminase 1 (GOT1), and α-glucosidase, with IC50 values of 25.95 μM, 47.06 μM, 5.91/6.91 μM, and 4.6 μM, respectively. It demonstrates key biological activities including inhibition of cancer cell proliferation, disruption of glutamine metabolism, and induction of apoptosis in cancer cells. Additionally, Aspulvinone H lowers postprandial blood glucose levels in mice and exhibits antibacterial properties against Staphylococcus aureus. This compound is suitable for research into pancreatic ductal adenocarcinoma, diabetes management, and infectious diseases caused by Staphylococcus aureus. -
Cysteine Analog
D-Ribose-L-cysteine is an orally active cysteine analog that enhances intracellular glutathione (GSH) biosynthesis, thereby improving cellular antioxidant capacity. This compound exhibits memory-enhancing effects and can reverse Scopolamine-induced memory impairment through the inhibition of oxidative stress and acetylcholinesterase (AChE) activity. D-Ribose-L-cysteine is valuable for research on neurodegenerative and cardiovascular diseases, providing insights into therapeutic strategies for these conditions. -
CaMK II Inhibitor
KN-93 hydrochloride is a potent and selective inhibitor of calmodulin-dependent kinase type II (CaMKII), functioning through a reversible and competitive mechanism with an inhibition constant (Ki) of 370 nM. This compound is widely utilized in research involving calcium signaling pathways and neuronal activity modulation. Its ability to inhibit CaMKII makes it valuable for studies investigating cardiac function, neurodegenerative diseases, and synaptic plasticity. -
TFEB Activator
TFEB Activator 2 is a potent oral compound that effectively crosses the blood-brain barrier, targeting the dopamine transporter (DAT). It promotes TFEB nuclear translocation and enhances lysosome biogenesis through modulation of the DAT-CDK9-TFEB signaling pathway. With demonstrated neuroprotective properties, this reagent is valuable for research applications related to Alzheimer's disease and other neurodegenerative conditions. -
CaMKII Substrate
Autocamtide 2 is a selective peptide substrate for calcium/calmodulin-dependent protein kinase II (CaMKII). This reagent is primarily utilized in assays to measure CaMKII activity, providing valuable insights into cellular signaling pathways influenced by calcium. Its specificity ensures reliable results in research applications involving calcium-dependent processes.
