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Catalog No.
Product Name
Application
Product Information
Citations
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CaMKII Inhibitor
Autocamtide-2-related inhibitory peptide, myristoylated is a potent and selective inhibitor of CaMKII, exhibiting an IC50 of 40 nM. This peptide is used in research applications to investigate the regulatory mechanisms of calcium-dependent signaling pathways. Its myristoylation enhances its membrane permeability, facilitating in vivo studies of CaMKII activity and function in various cellular contexts. -
Cholinesterase (ChE) Inhibitor
Sophoflavescenol is a prenylated flavonol that acts as a cholinesterase (ChE) inhibitor, demonstrating potent inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50 values of 10.98 μM and 8.21 μM, respectively. Additionally, it shows significant inhibition of other enzymes, including RLAR, HRAR, and BACE1. This compound is primarily utilized in research related to neurodegenerative diseases and cognitive function enhancement, making it a valuable reagent for studying cholinergic pathways. -
COX Inhibitor
Aspirin DL-lysine is a lysine-conjugated derivative of aspirin that functions primarily as a cyclooxygenase (COX) inhibitor. This compound effectively inhibits the synthesis of thromboxane A2 (TXA2) in platelets, leading to a reduction in platelet activation and aggregation. Aspirin DL-lysine is valuable for research applications focused on thrombin generation, particularly in clinical studies involving unstable angina pectoris. -
p38α MAPK/BChE Inhibitor
ARRY-371797 is a potent and orally bioavailable inhibitor of p38α MAPK and butyrylcholinesterase (BChE), demonstrating IC50 values of 12.0 µM for p38α MAPK and 0.13 µM for BChE, with minimal activity against human acetylcholinesterase (hAChE). This compound shows promise for research applications in Alzheimer’s disease, particularly in the context of neuroinflammation and cholinergic system modulation. -
CaMKK2 Inhibitor
CC-3240 is a highly selective inhibitor of CaMKK2, exhibiting a potent inhibitory effect with an IC50 of 9 nM. This molecular glue degrader, developed from CC-8977, effectively disrupts the function of CaMKK2, making it a valuable tool for investigations into calcium and calcium/calmodulin-dependent signaling pathways. CC-3240 is particularly useful in research applications aimed at exploring the role of CaMKK2 in cellular processes and disease states. -
BChE Inhibitor
Pteryxin is a potent butyrylcholinesterase (BChE) inhibitor (IC50 = 12.96 μg/mL) with additional multi-target mechanisms including inhibition of NF-κB, MAPK, NLRP3 inflammasome activation, and modulation of the Nrf2/ARE pathways. This compound demonstrates significant anti-inflammatory, antioxidant, and osteoclastogenesis inhibitory activities. Pteryxin is suitable for research applications related to inflammatory diseases, osteoporosis, diabetes, and neurodegenerative disorders such as Alzheimer's disease. -
COX-2/NLRP3 Inhibitor
COX-2/NLRP3-IN-1 is a selective inhibitor targeting both COX-2 and the NLRP3 inflammasome, with an IC50 of 1.53 μM for COX-2. This compound exhibits notable anti-inflammatory properties by disrupting the NF-κB/NLRP3 signaling pathway, making it a valuable tool for research into inflammatory diseases. It is suitable for studying the roles of COX-2 and NLRP3 in various biological processes and therapeutic interventions. -
P2X7 Receptor Inhibitor
P2X7-IN-2 is a potent inhibitor of the P2X7 receptor, demonstrating an IC50 value of 0.01 nM for the inhibition of IL-1β release. This compound is valuable in research focusing on the mechanisms of autoimmunity, inflammation, and cardiovascular disease. Its selective action on the P2X7 receptor makes it a critical tool for studying inflammatory pathways and potential therapeutic interventions. -
COX Inhibitor
(±)-Aiphanol is a potent inhibitor of cyclooxygenase (COX) enzymes, specifically targeting COX-1 (IC50 = 1.9 μM) and COX-2 (IC50 = 9.9 μM). This compound displays significant anti-inflammatory properties and further inhibits vascular endothelial growth factor receptor 2 (VEGFR2) with an IC50 of 0.92 μM. By impeding both COX-2 and VEGFR2 pathways, (±)-Aiphanol effectively blocks angiogenesis and induces apoptosis, making it a valuable tool in the study of inflammatory diseases and cancer research. The compound demonstrates oral bioactivity, enhancing its potential for in vivo applications. -
AChE/BChE/BACE-1 Inhibitor
AChE/BChE/BACE-1-IN-1 is a potent inhibitor of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and beta-secretase 1 (BACE-1), exhibiting IC50 values of 0.058 μM, 0.082 μM, and 0.115 μM, respectively. This compound demonstrates significant binding affinity for the peripheral anionic site of AChE, facilitates brain penetration, and shows potential in disrupting amyloid-beta (Aβ) aggregates. Additionally, AChE/BChE/BACE-1-IN-1 exhibits neuroprotective properties against Aβ-induced stress and possesses promising antioxidant activity, making it a valuable tool for Alzheimer's disease research and related neurodegenerative studies. -
AChE/BChE Inhibitor
AChE/BChE-IN-9 is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), exhibiting IC50 values of 5.74 μM and 14.05 μM, respectively. In addition to its enzymatic inhibition, AChE/BChE-IN-9 demonstrates antioxidant properties with an IC50 of 57.35 μM and has the ability to chelate iron, potentially mitigating oxidative stress. This compound also influences the aggregation of amyloid β1-42, making it relevant for research in neurodegenerative diseases and gerontology. Its capacity to cross the blood-brain barrier further enhances its suitability for studies focused on central nervous system disorders. -
AChE/GSK-3β Inhibitor
AChE/GSK-3β-IN-1 is a dual inhibitor targeting acetylcholinesterase (AChE) and glycogen synthase kinase 3 beta (GSK-3β), demonstrating potent inhibition with IC50 values of 1.2 nM for hAChE, 149.8 nM for hBChE, and 22.4 nM for hGSK-3β. This compound effectively penetrates the blood-brain barrier and displays high selectivity for the CMGC kinase family, particularly binding to the ATP site of DYRK1A. Additionally, AChE/GSK-3β-IN-1 has been shown to inhibit reactive oxygen species (ROS) expression, thereby reducing oxidative stress. It is a valuable tool for research into Alzheimer's disease and related neurodegenerative conditions. -
AChE/BChE/BACE-1 Inhibitor
AChE/BChE/BACE-1-IN-2 is a potent oral inhibitor of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein cleaving enzyme 1 (BACE-1), exhibiting IC50 values of 0.069 μM, 0.127 μM, and 0.097 μM, respectively. This compound demonstrates significant binding affinity to the peripheral anionic site of AChE, high brain permeability, and the ability to disassemble amyloid-beta (Aβ) aggregates. Additionally, AChE/BChE/BACE-1-IN-2 provides neuroprotective effects against Aβ-induced stress and possesses noteworthy antioxidant properties, making it suitable for research in neurodegenerative disease models. -
AChE/BChE Inhibitor
AChE-IN-14 is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), displaying IC50 values of 0.46 μM for electric eel AChE, 0.48 μM for human recombinant AChE, and 0.44 μM for equine serum BChE. In addition to its cholinesterase inhibition, AChE-IN-14 has a high affinity for the human H3 receptor (H3R) with a Ki value of 159.8 nM. This compound is particularly relevant for research focused on neurodegenerative diseases such as Alzheimer’s disease, where the modulation of cholinergic signaling is critical. -
Gamma-secretase inhibitor
BMS-708163 is an oral gamma secretase inhibitor designed for selective inhibition of amyloid beta synthesis. -
COX-2 inhibitor
Celecoxib is a sulfa non-steroidal anti-inflammatory drug (NSAID) and selective COX-2 inhibitor used in the treatment of osteoarthritis, rheumatoid arthritis, acute pain, painful menstruation and menstrual symptoms, and to reduce numbers of colon and rectum polyps in patients with familial adenomatous polyposis.
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Dihydropyrimidinase Inhibitor
Dihydromyricetin (Ampelopsin (flavanol); Ampeloptin) is a natural antioxidant with good prospects. -
COX inhibitor
Diclofenac Sodium is a non-selective COX inhibitor with IC50 of 0.5 μg/ml and 0.5 μg/ml for COX-1 and -2 in intact cells, respectively, used as a nonsteroidal anti-inflammatory drug (NSAID) to relieve pain and reduce swelling in flammation. -
AChE inhibitor
Donepezil is a centrally acting reversible acetylcholinesterase inhibitor. -
COMT inhibitor
Entacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment. -
AChE inhibitor
Galanthamine is an AChE inhibitor with IC50 of 14 nM. -
COX-1 inhibitor
Ibuprofen Lysine(Motrin) is a non-steroidal anti-inflammatory drug. -
COX-1/COX-2 inhibitor
Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively. -
COX inhibitor
Naproxen sodium is a non-selective cyclooxygenase (COX) inhibitor that displays anti-inflammatory, antipyretic and analgesic effects. Has a neuroprotective role against colchicine-induced cognitive impairment and oxidative stress. -
AChE inhibitor
Neostigmine bromide is a reversible acetylcholine esterase inhibitor that binds to the anionic binding site of AChE. -
α-adrenergic (AR) antagonist/CaM inhibitor
Phenoxybenzamine is a cell-permeable, non-specific, irreversible α-adrenergic (AR) antagonist that also acts as an CaM inhibitor. -
COX inhibitor
Phenylbutazone is a compound of research interest as an anti-inflammatory and anti-proliferative agent. -
COX inhibitor
Piroxicam is an effective and potent inhibitor of prostaglandin synthesis and a Cox-1 and Cox-2 inhibitor. -
platelet inhibitor
Prasugrel is a novel platelet inhibitor used for the reduction of thrombotic cardiovascular events (including stent thrombosis) in patients with acute coronary syndrome who are to be managed with PCI. -
GABA uptake inhibitor
SKF 89976A hydrochloride is a potent inhibitor of GABA uptake with IC50 of 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively. -
COX inhibitor
Sulindac is a non-steroidal COX inhibitor, which potently inhibits prostaglandin synthesis, used in the treatment of acute or chronic inflammatory conditions -
BACE1 inhibitor
Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. -
AChE inhibitor
Distigmine Bromide, also known as Ubretid and BC-51, is an acetylcholinesterase inhibitor used for the treatment of underactive neurogenic bladder and myasthenia gravis. -
OGT inhibitor
OSMI-1 is a potent cell-permeable inhibitor of O-GlcNAc transferase (OGT), with an IC50 value of 2.7 μM. This compound effectively decreases protein O-linked N-acetylglucosamine (O-GlcNAcylation) levels in various mammalian cell lines while maintaining the integrity of cell surface N- and O-linked glycans. OSMI-1 serves as a valuable tool for studying the regulatory roles of O-GlcNAcylation in cellular processes and diseases. -
α-synuclein/Amyloid-β Aggregation Inhibitor
Scyllo-Inositol is an aggregation inhibitor that targets misfolded proteins, specifically α-synuclein and Amyloid-β. It effectively stabilizes non-toxic oligomers, preventing their conversion into toxic fibrils, thus supporting protein homeostasis and providing neuroprotective effects. By binding to the hydrophobic regions of pathogenic proteins, Scyllo-Inositol inhibits protein aggregation and enhances lysosome- and proteasome-mediated degradation pathways, ultimately reducing neurotoxicity. This compound is valuable for researching neurodegenerative diseases, including Parkinson’s disease, Alzheimer’s disease, and Huntington’s disease. -
Amyloid-β Inhibitor
Hoechst 34580 tetrahydrochloride is a nuclear marker dye that selectively targets A/T-rich double-stranded DNA. This compound exhibits enhanced fluorescence intensity when bound to nucleic acids, making it valuable for live cell labeling applications. As the pH of the solution increases, the fluorescence intensity of Hoechst 34580 also increases, providing a reliable tool for studying cellular dynamics, DNA distribution, and nuclear morphology in real-time. This reagent is particularly useful in research focused on amyloid-β and related neurodegenerative processes. -
COX2 Inhibitor
Iminostilbene is a well-characterized inhibitor of COX2 (Cyclooxygenase-2) with additional activity against PKM2 (Pyruvate Kinase M2). This compound effectively reduces the expression of COX2 and iNOS, as well as the release of pro-inflammatory cytokines such as IL-1β, IL-6, TNF-α, and MCP-1 in macrophages. Its ability to mitigate macrophage-mediated inflammatory responses makes iminostilbene a valuable reagent for investigating mechanisms of inflammation regulation, cardiovascular disease, including myocardial ischemia/reperfusion injury, and immune-related disorders. -
CaMK1D Inhibitor
CS640 is a selective inhibitor of calmodulin-dependent kinase 1D (CaMK1D) with additional activity against several other kinases, including CaMK1B, CaMK1A, and MEK5, demonstrating IC50 values of 8 nM, 3 nM, 1 nM, and 25 nM, respectively. This compound effectively inhibits Aβ-induced hyperphosphorylation of tau protein at the Thr181 site, making it valuable for studies on tau pathology. While CS640 does not provide protective effects against Aβ-induced neurotoxicity in primary mouse cortical neurons, it is useful for research focusing on the mechanisms of Alzheimer's disease. -
COX Inhibitor
Aspirin lithium is a potent, orally active, irreversible inhibitor of cyclooxygenase COX-1 and COX-2, exhibiting IC50 values of 5 and 210 μg/mL, respectively. This compound promotes apoptosis and inhibits the activation of NF-κB, making it valuable for studies on inflammation and cell death. Additionally, Aspirin lithium effectively inhibits platelet prostaglandin synthetase, providing potential protective effects against coronary artery and cerebrovascular thrombosis. -
NDs Inhibitor
NDs-IN-1 is a non-covalent multi-target inhibitor designed to inhibit the activities of key enzymes including human beta-secretase 1 (hBACE-1), human acetylcholinesterase (hAChE), and human monoamine oxidase B (hMAO-B). This compound is primarily utilized in research focused on neurodegenerative diseases, offering potential avenues for understanding disease mechanisms and developing therapeutic strategies. -
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. -
AChE Inhibitor
AChE-IN-105 is a potent mixed inhibitor of acetylcholinesterase (AChE) with an IC50 value of 5.02 μM. It exhibits significant antioxidant properties by scavenging reactive oxygen species (ROS) and mitigating hydrogen peroxide-induced activation of Caspase-3, while also downregulating the Nrf2-ARE pathway. In preclinical studies, AChE-IN-105 demonstrated the ability to prevent memory deficits in a zebrafish model of scopolamine-induced cognitive dysfunction. This compound is valuable for research focused on Alzheimer's disease and cognitive impairment mechanisms. -
COX Inhibitor
(E)-Ethyl p-methoxycinnamate is a COX inhibitor that exhibits significant anti-inflammatory properties. Isolated from Kaempferia galangal, this compound demonstrates both anti-neoplastic and anti-microbial activities. In vitro studies reveal that (E)-Ethyl p-methoxycinnamate inhibits COX-1 and COX-2 with IC50 values of 1.12 μM and 0.83 μM, respectively, making it a valuable reagent for research in inflammatory and cancer-related studies. -
GCS Inhibitor
PDMP hydrochloride is a potent inhibitor of glucosylceramide synthase (GCS). This compound has been shown to induce apoptosis in K562/A02 cells, making it a valuable tool for studying cancer biology, particularly in leukemia research. PDMP hydrochloride's ability to disrupt glycosphingolipid metabolism provides insights into therapeutic strategies targeting GCS in cancer treatment. -
COX-2 Specific Inhibitor
SC-236 is a selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 of 10 nM and also acts as a PPARγ agonist. It effectively suppresses activator protein-1 (AP-1) through the inhibition of c-Jun NH2-terminal kinase, demonstrating significant anti-inflammatory effects. SC-236 has been shown to reduce ERK phosphorylation in murine models, highlighting its potential for investigating inflammatory pathways and therapeutic interventions. -
COX-2 Inhibitor
Humulone, a prenylated phloroglucinol derivative, is a selective inhibitor of cyclooxygenase-2 (COX-2). It demonstrates significant anti-inflammatory properties and serves as a positive modulator of GABAA receptors at low micromolar concentrations. Additionally, Humulone is known to inhibit bone resorption and exhibits antioxidant, anti-angiogenic, and pro-apoptotic activities, making it valuable for various research applications in inflammation and cancer studies. -
COX-2 Inhibitor
DuP-697 is a potent, irreversible, and selective inhibitor of cyclooxygenase-2 (COX-2), exhibiting an IC50 of 10 nM for human COX-2 and 800 nM for COX-1. This compound demonstrates significant antiproliferative effects on HT29 colorectal cancer cells with an IC50 of 42.8 nM, as well as antiangiogenic and pro-apoptotic activities. By inhibiting prostaglandin synthesis, DuP-697 offers potential applications in studies related to inflammation, cancer, and fever reduction.
