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mAChR Agonist
CDD0102 Hydrochloride is a potent agonist of the M1 muscarinic acetylcholine receptor (mAChR). This compound exhibits significant biological activity in modulating cholinergic signaling, making it valuable for research into neurological disorders and cognitive function. Its application extends to studying M1 receptor-related pathways and developing potential treatments for conditions such as Alzheimer's disease and schizophrenia. -
mAChR Antagonist
4,4-Difluorobenzhydrol serves as a precursor for a muscarinic acetylcholine receptor (mAChR) antagonist, with potential applications in neuroscience research. Its derivative, 4,4-Difluorobenzhydrol Carbamate, can selectively target the M1 receptor subtype. This specificity makes 4,4-Difluorobenzhydrol an important compound for studying the physiological roles of mAChRs and developing therapeutics for related disorders. -
Stable Isotope
Itopride-d6 hydrochloride is a deuterium-labeled derivative of Itopride hydrochloride that serves as a stable isotope. Itopride functions as a gastroprokinetic agent by inhibiting acetylcholinesterase (AChE) and antagonizing dopamine D2 receptors. This compound is valuable for studies investigating gastrointestinal motility and neurotransmitter interactions, as well as for tracing and quantifying its metabolic pathways in biological research. -
Acetylcholinesterase Inhibitor
Trimethylammonium chloride is a non-competitive inhibitor of acetylcholinesterase, targeting the enzymatic activity responsible for the hydrolysis of the neurotransmitter acetylcholine. By reversibly blocking the deacetylation process of acetylcholinesterase, this reagent plays a critical role in studies related to neurobiology and the modulation of synaptic transmission. Its application extends to research investigating cholinergic signaling pathways and potential therapeutic strategies for neurological disorders. -
Racemate of Anabasine
(±) Anabasine is the racemic mixture of Anabasine, acting as an agonist of the alpha-7 nicotinic acetylcholine receptor (α7nAChR). This compound has demonstrated anti-inflammatory properties and insecticidal activity, making it relevant for research in neuropharmacology and pest control studies. Its biological activities encourage further investigations into its therapeutic potential and applications. -
Stable Isotope
(Z)-Tetrachlorvinphos-d6 is a deuterated form of Tetrachlorvinphos, an organophosphorus pesticide that primarily acts as a cholinesterase inhibitor. This stable isotope is utilized in research to trace metabolic pathways and analyze pesticide residues in various biological matrices. With low toxicity to mammals, it provides a safe and useful tool for studying the environmental impact and biochemical interactions of pesticide application. -
Endogenous Metabolite
Bendiocarb is a carbamate compound that primarily acts as an inhibitor of the enzyme acetylcholinesterase. This inhibition results in increased levels of acetylcholine, which plays a crucial role in neurotransmission and muscle contraction. Bendiocarb is utilized in research applications focusing on neurobiology and the study of cholinergic systems, as well as in the examination of potential neurotoxic effects. -
Endogenous Metabolite
Neostigmine iodide is a reversible inhibitor of acetylcholinesterase, enhancing muscle tone and function. This compound is primarily utilized in the management of myasthenia gravis, aiming to improve muscle strength in affected patients. Additionally, Neostigmine iodide is employed in anesthetic procedures to counteract the effects of nondepolarizing muscle relaxants, such as rocuronium, thereby facilitating recovery from anesthesia. -
Endogenous Metabolite
BuChE-IN-14 is a selective inhibitor of acetylcholinesterase (AChE), primarily targeting endogenous metabolite pathways. In vitro studies demonstrated a concentration-dependent inhibition of AChE activity in rat brain tissue, leading to increased extracellular acetylcholine (ACh) levels in the hippocampus and striatum. This compound shows potential for addressing memory impairments linked to cholinergic dysfunction, making it valuable for research into neurodegenerative diseases and cognitive enhancement. -
Methyltransferase
Catechol O-methyltransferase (COMT), derived from porcine liver, is a methyltransferase that facilitates the magnesium-dependent transfer of methyl groups from S-adenosyl methionine to the hydroxyl group of dopamine, resulting in the formation of 3-methoxytyramine. This enzyme exists in two forms: a soluble form (S-COMT) and a membrane-bound form (MB-COMT). COMT plays a critical role in regulating the levels of key neurotransmitters, including epinephrine, norepinephrine, and dopamine, making it essential for research related to neuropharmacology and psychiatric disorders. -
Isotope-Labeled Compounds
(±) Anabasine-d4 is a deuterated analog of (±) Anabasine, serving as a useful isotope-labeled compound. This racemic mixture acts as an agonist of the α7 nicotinic acetylcholine receptor (α7nAChR), demonstrating notable anti-inflammatory properties and insecticidal activity. It is suitable for applications in pharmacological research, particularly studies involving receptor activation and inflammatory responses. -
Cholinesterase (ChE) Inhibitor
Vomifoliol is a cholinesterase (ChE) inhibitor that exhibits significant antiacetylcholinesterase activity, comparable to that of abscisic acid (ABA). Additionally, this compound shows moderate antileishmanial activity, making it a valuable tool for research into neurodegenerative disorders and parasitic infections. Its unique structure, featuring a modified 2,4-pentadiene side chain, further contributes to its biological activity, offering potential applications in pharmacological studies. -
Prolyl Endopeptidase (PREP) Inhibitor
ONO 1603 is a selective inhibitor of prolyl endopeptidase (PREP), investigated for its potential in antidementia therapy. This compound has demonstrated neuroprotective properties and neurotrophic effects in cerebellar granule cells, enhancing neuronal survival and promoting neurite outgrowth at a concentration of 0.03 µM. Additionally, ONO 1603 increases m3-muscarinic acetylcholine receptor (mAChR) mRNA levels and stimulates mAChR-mediated signaling pathways. These pharmacological properties suggest that ONO 1603 could be a promising therapeutic agent for Alzheimer's disease by enhancing cholinergic neurotransmission and supporting neuronal function. -
Ligand for Target Protein for PROTAC
Aberrant tau ligand 1 is a specific ligand targeting abnormal tau proteins. This compound facilitates the development of proteolysis-targeting chimeras (PROTACs) designed for the degradation of aberrant tau, enabling research into tau-related pathologies. It is a valuable tool for studying tau protein dynamics and their implications in neurodegenerative diseases. -
AAK1 Inhibitor
BMS-986176 is a potent and selective inhibitor of adaptor associated kinase 1 (AAK1) with an IC50 value of 2 nM. This compound is designed for effective brain penetration, making it a valuable tool in the investigation of neurodegenerative diseases. It is applicable in research focused on the modulation of AAK1 pathways and their implications in various neurological disorders. -
AAK1 Inhibitor
AAK1-IN-12 is a selective inhibitor of the AP2-associated kinase 1 (AAK1) that demonstrates oral bioavailability and the ability to cross the blood-brain barrier. This compound has important implications for research into neurodegenerative disorders, including schizophrenia, Parkinson's disease, neuropathic pain, and Alzheimer's disease. AAK1-IN-12 serves as a valuable tool for investigating the therapeutic potential of AAK1 modulation in various neurological contexts. -
AAK1 Inhibitor
LP-922761 is a selective inhibitor of adapter protein-2 associated kinase 1 (AAK1), demonstrating potent activity with IC50 values of 4.8 nM in enzyme assays and 7.6 nM in cellular assays. Additionally, LP-922761 inhibits BMP-2-inducible protein kinase (BIKE) at an IC50 of 24 nM. Importantly, it shows no significant activity against cyclin G-associated kinase (GAK), opioid receptors, adrenergic α2 receptors, or GABAa receptors, making it a valuable tool for studying AAK1-related signaling pathways and its role in cellular processes. -
AAK1
BMS-911172 is an inhibitor of adaptor-associated kinase 1 (AAK1), exhibiting an IC50 value of 35 nM. This compound is primarily used in research focused on modulating clathrin-mediated endocytosis and exploring the role of AAK1 in cellular processes. Its ability to selectively inhibit AAK1 makes it a valuable tool for investigating signaling pathways related to receptor internalization and trafficking. -
AAK1 Inhibitor
BMT-124110 is a highly selective inhibitor of AAK1 (AP2-associated protein kinase 1) with an IC50 value of 0.9 nM. This compound exhibits notable antinociceptive activity, making it relevant in pain management research. Additionally, BMT-124110 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50 values of 17 nM and 99 nM, respectively, further supporting its utility in kinase-related studies. -
AAK1 Inhibitor
SGC-AAK1-1N is a selective inhibitor of AAK1 (AP2 associated kinase 1) with an IC50 value of 1.8 μM. This compound is utilized in research to elucidate the role of AAK1 in cellular processes, particularly in clathrin-mediated endocytosis and signaling pathways. Its potency makes it a valuable tool in studies focused on understanding the therapeutic potential of AAK1 modulation in various diseases. -
AAK1 Inhibitor
BMS-901715 is a highly selective inhibitor of adaptor protein-2 associated kinase 1 (AAK1) with an IC50 of 3.3 nM. This compound disrupts clathrin-mediated endocytosis, making it valuable for studying cellular processes related to membrane trafficking. BMS-901715 is particularly useful in research applications focused on viral infections and the modulation of synaptic transmission. -
AAK1 Inhibitor
AAK1-IN-2 TFA is a selective and potent inhibitor of Adaptor Protein 2-Associated Kinase 1 (AAK1), demonstrating an IC50 value of 5.8 nM. This compound effectively penetrates the blood-brain barrier, making it a valuable tool for research in neuropathic pain mechanisms. AAK1-IN-2 TFA enables the investigation of AAK1's role in various neurological conditions, providing insights into potential therapeutic targets for pain management. -
AAK1 Inhibitor
AAK1-IN-3 is a potent inhibitor of adaptor protein 2-associated kinase 1 (AAK1), exhibiting an IC50 of 11 nM. This quinoline analogue effectively penetrates the blood-brain barrier, making it suitable for investigating the role of AAK1 in neuropathic pain mechanisms. AAK1-IN-3 is a valuable tool for research focused on neuropharmacology and the modulation of pain pathways. -
AAK1 Inhibitor
AAK1-IN-4 is a selective inhibitor of adaptor protein-2-associated kinase 1 (AAK1), demonstrating an IC50 of 4.6 nM. This orally active compound effectively penetrates the central nervous system, with a filtration Ki of 0.9 nM and a cell IC50 of 8.6 nM. AAK1-IN-4 is primarily utilized in research studies focused on neuropathic pain, offering insights into its underlying mechanisms and potential therapeutic applications. -
AAK1 Inhibitor
AAK1-IN-3 TFA is a quinoline derivative that selectively inhibits adaptor protein 2-associated kinase 1 (AAK1) with an IC50 of 11 nM. This compound demonstrates significant brain penetration and is suitable for investigating neuropathic pain mechanisms. Its ability to modulate AAK1 activity makes it a valuable tool for research applications focused on pain pathways and related neurobiological processes. -
AAK1 Inhibitor
HW161023 is a potent inhibitor of AP2-associated protein kinase 1 (AAK1), demonstrating an IC50 of 5.4 nM against AAK1 and a much higher IC50 of 11.9 μM against hERG. This compound has shown efficacy in alleviating pain in a chronic constriction injury model of the sciatic nerve in rats. HW161023 is valuable for research in pain mechanisms and the modulation of AAK1-related signaling pathways. -
AAK1 Inhibitor
AAK1-IN-10 is a selective inhibitor of adapter-associated kinase 1 (AAK1), exhibiting potent enzyme inhibitory activity with an IC50 of 9.62 nM. This compound primarily functions by impairing the activity of AAK1, a kinase involved in various cellular processes. AAK1-IN-10 demonstrates low cardiotoxicity, with an IC50 of 13.7 μM, making it a suitable candidate for research into conditions such as diabetic neuropathy and postherpetic pain. Its distinct mechanism and safety profile facilitate investigations into therapeutic applications targeting nerve pain and associated disorders. -
AAK1 Inhibitor
AAK1-IN-2 is a selective inhibitor of Adaptor Protein 2-Associated Kinase 1 (AAK1), exhibiting an IC50 of 5.8 nM. This compound demonstrates the ability to penetrate the blood-brain barrier, making it suitable for neurological research. AAK1-IN-2 is particularly relevant for studies investigating the mechanisms underlying neuropathic pain. -
AAK1 Inhibitor
AAK1-IN-5 is a selective inhibitor of adaptor protein-2-associated kinase 1 (AAK1), demonstrating an IC50 of 1.2 nM and a filtrate Ki of 0.05 nM, along with a cell-based IC50 of 0.5 nM. This compound is notable for its ability to penetrate the central nervous system and is orally active, making it suitable for in vivo studies. AAK1-IN-5 is primarily used in research focused on neuropathic pain, providing a valuable tool for understanding AAK1's role in pain pathways. -
PROTAC
PROTAC AAK1 Degrader-1 is a potent PROTAC designed to selectively degrade the AAK1 protein, a known modulator of clathrin-mediated endocytosis. This compound facilitates targeted protein degradation, thereby influencing cellular pathways critical in cancer research. Its application is valuable for studying the role of AAK1 in tumor biology and therapeutic resistance, potentially leading to innovative cancer treatment strategies.
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AAK1 Inhibitor
BMT-046091 is a selective inhibitor of adaptor-associated kinase 1 (AAK1), targeting its activity to modulate cellular processes. This compound effectively inhibits the phosphorylation of the μ2 peptide by AAK1, demonstrating an IC50 value of 2.8 nM. BMT-046091 is useful in research applications studying AAK1's role in endocytic trafficking and signaling pathways, contributing to a better understanding of its implications in various diseases. -
Aβ Aggregation Inhibitor
TDI-2760 is an Aβ aggregation inhibitor with an IC50 of 1.67 μM, specifically targeting the aggregation of amyloid-beta peptides. This compound effectively inhibits Aβ-fibrinogen interactions and modulates contact system activation induced by Aβ42. TDI-2760 is suitable for research focused on Alzheimer's disease, particularly in the study of vascular abnormalities associated with Aβ aggregation. -
Buffering Agent
HEPPS is a buffering agent with an effective pH range of 7.3 to 8.7. This compound has demonstrated the ability to reduce amyloid beta (Aβ) aggregate-induced memory deficits and improve cognitive functions in murine models. HEPPS is orally active and capable of crossing the blood-brain barrier, making it valuable for neuroscience research. -
TDP-43 Binder
rTRD01 is a selective TDP-43 binder that specifically targets the RRM1 and RRM2 domains of TDP-43, partially disrupting its interaction with c9orf72 repeat RNA while preserving binding to canonical sequences. This compound demonstrates significant neuroprotective effects in zebrafish models, improving motor function and providing protection against paraquat-induced neurodegeneration without teratogenic effects at elevated concentrations. rTRD01 is a valuable tool for investigating amyotrophic lateral sclerosis and related TDP-43 proteinopathies, offering insights into the molecular mechanisms involved in these conditions. -
β-amyloid (Aβ) Binder
Pittsburgh Compound B (PiB) is a targeted β-amyloid (Aβ) binder, designed as a PET tracer for the visualization of Aβ deposition in the brain. It exhibits a high affinity for Aβ(1-40) fibrils with a Ki value of 678.4 nM. The compound can be modified using click chemistry, allowing for the development of fluorescent conjugates for applications in fluorescence imaging and ultrastructural studies. Pittsburgh Compound B is particularly relevant for research focusing on Alzheimer's disease and the characterization of Aβ complexes. -
Amyloid-β 42 Inducer
Aftin-5 is an inducer of Amyloid-β 42 (Aβ42) that functions by modulating β-secretase and γ-secretase activity, leading to an increase in Aβ42 levels while decreasing Aβ38 levels. This compound affects mitochondrial ultrastructure, which is essential for its biological activity. Aftin-5 displays moderate cytotoxicity in various cell lines, including SH-SY5Y, HT22, N2a, and N2a-AβPP695, with IC50 values ranging from 150 μM to 194 μM. Its role in research makes it a valuable tool for studying Alzheimer's disease and related neurodegenerative conditions. -
BACE1/BACE2 Inhibitor
NB-360 is a potent dual inhibitor of β-secretase 1 and 2 (BACE1/BACE2) with IC50 values of 5 nM and 6 nM, respectively. This compound is brain-penetrable and orally active, effectively inhibiting the accumulation of amyloid-β proteins. NB-360 is valuable for research in inflammation and neurological diseases, particularly Alzheimer's disease. -
APP Degrader
APP degrader-1 is an orally active compound designed to target the amyloid precursor protein (APP). It induces the degradation of APP and effectively reduces the extracellular release of Aβ42. By binding to both CAPRIN1 and APP, APP degrader-1 enhances their interaction and facilitates CAPRIN1-mediated APP degradation via the endosome-lysosome pathway. This compound holds potential for research applications related to Alzheimer's disease and protein misfolding disorders. -
β-Amyloid
β-Amyloid (1-16) is a peptide fragment derived from β-Amyloid, known for its ability to bind various metal ions. This fragment plays a significant role in the formation of amyloid plaques, which are characteristic of Alzheimer's disease pathology. Researchers can utilize β-Amyloid (1-16) to investigate metal-induced aggregation mechanisms and assess its potential contributions to neurodegenerative processes associated with Alzheimer's disease. -
Amyloid Inhibitor
4-Hydroxyindole is an amyloid inhibitor that plays a critical role in the disruption of amyloid fibrillization. This compound has been shown to induce alterations in liver function, thyroid activity, and blood glucose levels in preclinical models. Its unique properties make 4-Hydroxyindole a valuable tool for investigating neurodegenerative diseases and metabolic disorders. Researchers can leverage its potential to explore therapeutic avenues for amyloid-related pathologies. -
TDP-43 Inhibitor
ACI-19626 is a TDP-43 inhibitor that targets TDP-43 aggregation. This compound is valuable for investigating the role of TDP-43 in neurodegenerative diseases, including amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD). Its utility in preclinical studies helps elucidate the molecular mechanisms underlying these conditions and aids in the identification of potential therapeutic strategies. -
Aβ1-42 Aggregation Inhibitor
Aβ1–42 aggregation inhibitor 1 is a potent inhibitor of Aβ1-42 aggregation, targeting its self-mediated aggregation pathway. This compound effectively inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) with IC50 values of 2.64 μM and 1.29 μM, respectively. At a concentration of 25 μM, it reduces Aβ1-42 aggregation by 51.29%. Aβ1–42 aggregation inhibitor 1 is suitable for research applications focused on the mechanisms of Alzheimer's disease and potential therapeutic interventions. -
AChE Inhibitor
Phenserine is a potent, noncompetitive inhibitor of acetylcholinesterase (AChE), derived from Physostigmine. It selectively targets AChE and has been shown to reduce the formation of β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ). This compound is primarily utilized in research related to cognitive function and the progression of Alzheimer's disease, demonstrating potential therapeutic benefits in enhancing cognitive performance. -
QPCTL Inhibitor
QP5038 is a specific inhibitor of the enzyme QPCTL, exhibiting an IC50 value of 3.8 nM. This compound demonstrates significant antitumor activity, making it a valuable tool for research in cancer biology. QP5038 can be utilized in studies focused on understanding the role of QPCTL in tumor metabolism and potential therapeutic strategies. -
PHF6/Tau Disrupter
Cl-NQTrp is a potent disrupter of preformed fibrillar aggregates associated with Tau-derived PHF6 (VQIVYK) peptides and full-length tau protein. This compound exhibits substantial activity in modulating tau aggregation, making it a valuable tool for research focused on tauopathies and Alzheimer's disease. Its role in disrupting tau pathology positions Cl-NQTrp as a key reagent for studies investigating therapeutic strategies against neurodegenerative disorders characterized by abnormal tau accumulation. -
Glutaminyl Cyclase Inhibitor
PBD-150 is a selective inhibitor of human glutaminyl cyclase (hQC), specifically targeting the Y115E-Y117E variant with a Ki value of 490 nM. This compound exhibits significant inhibitory activity, making it a valuable tool for studying the role of glutaminyl cyclase in neurodegenerative diseases. PBD-150 can be applied in research focused on pathologies associated with abnormal protein aggregation and its therapeutic potential. -
Aβ Aggregation Inhibtior
Dihydrochalcone is an Aβ aggregation inhibitor that destabilizes Aβ17-42 protofibrils by disrupting the β-sheet structure in the β1 region. This compound effectively targets both U-shaped Aβ40/Aβ42 and S-shaped Aβ42 protofibrils by binding to their respective protofibril cavities. Dihydrochalcone, primarily derived from the daemonorops draco tree, is of significant interest in Alzheimer's disease research and offers potential for studying therapeutic strategies aimed at preventing amyloid-beta aggregation. -
TFEB Activator
TFEB Activator 3 is a potent activator of TFEB, enhancing its nuclear translocation and promoting lysosome biogenesis. Demonstrated effects include a 44% increase in nuclear translocation at 10 µM after 3 hours and up to 97% at 30 µM under the same conditions. This compound is significant for research into Alzheimer’s disease, as it effectively crosses the blood-brain barrier, making it a valuable tool for studies on neurodegeneration and cellular clearance mechanisms. -
Bexarotene Derivative
OAB-14 is a derivative of Bexarotene that enhances the clearance of β-amyloid in APP/PS1 transgenic mice, addressing Alzheimer's disease-related pathologies and cognitive deficits. This compound demonstrates the ability to improve the functionality of the endosomal-autophagic-lysosomal pathway, making it a valuable tool for research into Alzheimer's disease mechanisms and potential therapeutic interventions. -
Amyloid-β Inhibitor
D-KLVFFA is a potent inhibitor of Amyloid-β assembly, exhibiting an IC50 value of 2.6 μM. This peptide is utilized in research focused on Alzheimer's disease, providing insights into the mechanisms of amyloid plaque formation and potential therapeutic interventions. Its application can contribute to the understanding of neurodegenerative processes and the development of Alzheimer’s disease treatments.

