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Catalog No.
Product Name
Application
Product Information
Citations
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CaMKII inhibitor
CaMKII-IN-1 is a potent and highly selective CaMKII inhibitor with IC50 of 63 nM. -
P2Y Receptor Inhibitor
N6-(4-Hydroxybenzyl)adenosine is a inhibitor of platelet aggregation induced in vitro by collagen and their activity range was demonstrated (IC50: 6.77-141 μM). -
GCS inhibitor
Ibiglustat (Venglustat), a potential therapy for PD Parkinson??s disease, SRT in Fabry??s and Gaucher??s, is a selective, allosteric inhibitor of glucosylceramide synthase (GCS) with ability to cross the blood-brain barrier. -
gamma secretase inhibitor
BMS-906024 is an oral and selective gamma secretase inhibitor (GSI) that is a small molecule Notch inhibitor. -
P2Y12 receptor inhibitor
Clopidogrel is a well-known and orally active platelet inhibitor that targets P2Y12 receptor. Clopidogrel is used to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease. -
Aβ-ABAD inhibitor
Frentizole, an FDA-approved immunosuppressive drug, is a novel inhibitor of the Aβ-ABAD interaction.
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BACE-1 inhibitor
β-Secretase Inhibitor IV is a potent, cell-active BACE-1 inhibitor with IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively. -
cholinesterase inhibitor
(R)-Rivastigmine D6 (tartrate) is the deuterium labeled (R)-Rivastigmine, which is an cholinesterase inhibitor. -
glucosylceramide synthase inhibitor
Genz-123346 is a potent, orally available glucosylceramide synthase inhibitor. -
BACE1 inhibitor
AZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor. -
GlyT1 inhibitor
LY2365109 hydrochloride is a potent and selective GlyT1 inhibitor, with an IC50 of 15.8 nM for glycine uptake in cells over-expressing hGlyT1a. -
calmodulin inhibitor
Zaldaride maleate (CGS-9343B) is a potent and selective inhibitor of calmodulin. -
[3H](+)pentazocine binding inhibitor
Levetimide is a potent and stereoselective inhibitor of [3H](+)pentazocine binding, with a Ki of 2.2 nM. -
COX-2 inhibitor
Etoricoxib D4 (MK-0663 D4) is a deuterium labeled Etoricoxib. Etoricoxib is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood. -
COMT inhibitor
Entacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment. -
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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Inhibitor of U46619-induced Rat Platelet Aggregation
Timosaponin AIII is a potent Inhibitor of U46619-induced Rat Platelet Aggregation, Selectively Inhibiting TxA2-induced Platelet Activation, Preferably Suppressing TP-mediated Activation of Gq, not G12/13, Signaling Pathways. -
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. -
COX-2/MMP-7/TLR4 Inhibitor
Isofraxidin is a coumarin compound derived from *Acanthopanax senticosus* that exhibits anti-invasive and anti-inflammatory properties. It inhibits MMP-7 expression and suppresses cell invasion in human hepatoma cells by reducing ERK1/2 phosphorylation. Isofraxidin also downregulates the expression of iNOS and COX-2 and inhibits the formation of the TLR4/myeloid differentiation protein-2 (MD-2) complex. -
COX/LOX inhibitor
Phenidone is an orally active dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX) pathways, exhibiting anti-inflammatory and immunomodulatory effects. It has been shown to ameliorate paralysis in rat models of experimental autoimmune encephalomyelitis (EAE), a model for multiple sclerosis. Phenidone also acts as a potent hypotensive agent in spontaneously hypertensive rats. Additionally, it has a long-standing application as a photographic developer due to its redox properties. -
COX-1/COX-2 inhibitor
Glafenine is a non-selective, non-steroidal anti-inflammatory drug (NSAID) that inhibits both COX-1 and COX-2 enzymes. It exerts anti-inflammatory, anti-proliferative, and anti-migratory effects by suppressing the arachidonic acid metabolic pathway, thereby reducing prostaglandin production. Additionally, glafenine induces cell cycle arrest in vascular smooth muscle cells and endothelial cells and decreases the synthesis of the extracellular matrix protein tenascin. It is utilized in research related to inflammatory disorders, vascular restenosis, and cystic fibrosis. -
AChE inhibitor
Picfeltarraenin IA is a triterpenoid compound isolated from *Picria fel-terrae* (*P. fel-terrae*) that functions as an acetylcholinesterase (AChE) inhibitor. It exhibits therapeutic potential for the treatment of herpes infections, cancer, and inflammatory conditions, making it a promising candidate for further pharmacological research. -
COX inhibitor
Dexketoprofen trometamol (Dexketoprofen tromethamine salt) is an orally active, non-selective cyclooxygenase (COX) inhibitor. It exhibits analgesic, anti-inflammatory, and anti-cancer effects. As the active enantiomer of ketoprofen, Dexketoprofen trometamol is commonly used for the management of pain and inflammation, and it is also under investigation for its potential anticancer properties. -
COX-2 inhibitor
SC-58125 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 0.04 μM. It demonstrates antitumor activity both in vitro and in vivo and is effective in reducing inflammation-related edema. Additionally, SC-58125 possesses analgesic properties, making it a valuable compound for research in cancer, inflammation, and pain management. -
NSAID/COX inhibitor
Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory drug (NSAID) that functions primarily by inhibiting cyclooxygenase (COX) enzymes, thereby reducing the synthesis of pro-inflammatory prostaglandins. In addition to its classical NSAID activity, Fenoprofen has been identified as a positive allosteric modulator (PAM) of melanocortin receptors (MCRs), enhancing MCR-mediated signaling. Fenoprofen also promotes ERK1/2 activation in HEK293T cells, suggesting additional modulation of intracellular signaling pathways involved in inflammation and cellular proliferation. -
MAPK inhibitor
MAPK-IN-1 (Compound 2) is an inhibitor of the MAPK signaling pathway with demonstrated neuroprotective and anti-neuroinflammatory properties. It also exhibits acetylcholinesterase (AChE) inhibitory activity, with an IC₅₀ of 23.84 μM, contributing to enhanced cholinergic signaling. These combined actions make MAPK-IN-1 a promising candidate for research in Alzheimer's disease and other neurodegenerative disorders, where modulation of MAPK signaling and cholinergic function are of therapeutic interest. -
COX-1/HDAC/Tyrosinase Inhibitor
Gnetol is a bioactive phenolic compound isolated from the root of *Gnetum montanum* with diverse pharmacological properties. It potently inhibits cyclooxygenase-1 (COX-1) with an IC₅₀ of 0.78 μM and exhibits histone deacetylase (HDAC) inhibitory activity. Gnetol is also a strong tyrosinase inhibitor, with an IC₅₀ of 4.5 μM against murine tyrosinase, leading to suppression of melanin biosynthesis. In addition to its antioxidant, antiproliferative, anticancer, and hepatoprotective effects, Gnetol modulates metabolic enzymes in a concentration-dependent manner, including α-amylase, α-glucosidase, and adipogenesis pathways, making it a promising candidate for research in oncology, dermatology, and metabolic disorders. -
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. -
COX-1/2 Inhibitor
Cudraflavone B is a prenylated flavonoid that functions as a dual inhibitor of COX-1 and COX-2, demonstrating significant anti-inflammatory and anti-tumor activity. This compound inhibits the translocation of nuclear factor κB (NF-κB) in macrophages, leading to decreased tumor necrosis factor α (TNFα) gene expression and secretion. Additionally, Cudraflavone B induces the mitochondrial apoptotic pathway while activating MAPK signaling pathways, including p38 and ERK, and upregulating SIRT1 expression. These mechanisms contribute to its efficacy in attenuating the growth of human oral squamous cell carcinoma cells, making it a valuable tool for cancer research. -
COX Inhibitor
Oxaprozin is a potent, orally active cyclooxygenase (COX) inhibitor, demonstrating IC50 values of 2.2 μM for human platelet COX-1 and 36 μM for IL-1-stimulated human synovial cell COX-2. This compound exhibits significant anti-inflammatory activity and is known to inhibit the activation of NF-κB, promoting cell apoptosis. The inhibition of the Akt/IKK/NF-κB signaling pathway is a key mechanism underlying its anti-inflammatory properties, making Oxaprozin valuable for research in inflammation and related disorders. -
AChE Inhibitor
SCR1693 is a selective, reversible, orally active noncompetitive inhibitor of acetylcholinesterase (AChE), with an IC50 value of 0.68 μM, and exhibits calcium channel blocking properties. This compound effectively reduces tau phosphorylation levels and inhibits the generation and release of amyloid-beta (Aβ). Additionally, SCR1693 has been shown to restore insulin signaling and improve cognitive deficits, making it a valuable tool for studying Alzheimer's disease, particularly in cases complicated by type 2 diabetes mellitus. -
Dual COX-2/EGFR Inhibitor
Melafolone is a potent dual inhibitor of COX-2 and EGFR, displaying IC50 values of 13.2 μM for COX-2 and 17.4 μM for EGFR. This compound enhances the efficacy of anti-PD-1 therapy by promoting vascular normalization and downregulating PD-L1 through the PI3K/Akt signaling pathway in Lewis lung carcinoma (LLC) and CMT167 models. Melafolone is suitable for applications in lung cancer research.
