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Catalog No.
Product Name
Application
Product Information
Citations
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GABA-AT Inhibitor
GABA-AT-IN-1 is a potent inhibitor of γ-aminobutyric acid aminotransferase (GABA-AT), leading to a significant increase in GABA levels in the brain. This compound effectively crosses the blood-brain barrier, making it a valuable tool for research in anticonvulsant therapies. GABA-AT-IN-1 may be utilized in studies aimed at understanding GABAergic modulation in neurological disorders. -
GABA Receptor Inhibitor
Tiagabine hydrochloride hydrate is a potent and selective inhibitor of GABA uptake, primarily targeting the GABA receptor. It demonstrates significant anticonvulsant activity, with IC50 values of 67 nM in synaptosomes, 446 nM in neurons, and 182 nM in glial cells for [3H]GABA uptake. This compound is widely utilized in research focused on epilepsy and related neurological disorders. -
GABAAR Inhibitor
Org 21465 is a selective inhibitor of the GABA A receptor (GABA A R). It exhibits significant analgesic properties without inducing cardiovascular or respiratory depression, making it a valuable compound for pain research. This compound can be utilized in studies concerning the modulation of GABAergic neurotransmission and its effects on pain mechanisms in vivo. -
GABA-AT Inhibitor
GABA-AT-IN-2 is an inhibitor of GABA aminotransferase (GABA-AT) with an IC50 of 19.8 μM. This compound has demonstrated significant antianxiety effects in preclinical models, making it a valuable tool for investigating anxiety-related neurotic disorders. Its application in research may provide insights into therapeutic strategies for managing anxiety. -
GABA Uptake Inhibitor
CI-966 is a highly selective, orally active inhibitor of the GABA transporter GAT-1, with exceptional brain penetration. It displays IC50 values of 0.26 μM for human GAT-1 and 1.2 μM for rat GAT-1, demonstrating over 200-fold selectivity against GAT-2, GAT-3, and BGT-3. CI-966 is recognized for its anticonvulsant and neuroprotective properties, making it a valuable tool for neuropharmacological research. -
GABAA Inhibitor
AA29504 is an ethyl carbamate that functions as a GABAA receptor inhibitor. It effectively blocks the transmission of gamma-aminobutyric acid (GABA), a key neurotransmitter in the central nervous system, leading to its potential applications in the study of anxiety, insomnia, and other neuropsychiatric disorders. This compound serves as an important tool for researchers investigating GABAA receptor-mediated pathways and their role in various neurological conditions. -
GABA Receptor Inhibitor
CP-457920 is a potent GABA receptor inhibitor with a Ki value of approximately 1 ng/mL. This compound is primarily utilized in neurological research, particularly for studying pathways and mechanisms underlying diseases such as Alzheimer's disease. Its inhibitory action on GABA receptors makes it a valuable tool for investigating neuropharmacological processes and potential therapeutic interventions. -
GABA Receptor Inhibitor
DPNI-GABA is a nitroindoline derivative that selectively inhibits GABA(A) receptors, significantly decreasing GABA-evoked peak responses with an IC50 value of 0.5 mM. This compound serves as a valuable tool for researching the role of GABAergic signaling in various physiological and pathological processes, contributing to studies of neuronal excitability and synaptic transmission. Its inhibition of GABA(A) receptors makes it essential for elucidating mechanisms of action in neuropharmacology and related fields. -
GABA Receptor Inhibitor
SKF 89976A is a selective GABA transporter (GAT-1) inhibitor, displaying an IC50 of 0.28 μM for GAT-1 and significantly higher IC50 values of 137.34 μM and 202.8 μM for GAT-2 and GAT-3, respectively, in CHO cells. This compound is primarily utilized in neurological research focusing on the modulation of GABA neurotransmission. Its specificity for GAT-1 makes it a valuable tool for studying GABAergic signaling and related disorders. -
GABA-T Inhibitor
D-DABA is an enantiomeric form of L-DABA that acts as a weak inhibitor of GABA transaminase (GABA-T). Its inhibitory potency is approximately one-twentieth that of the L-isomer in reducing GABA uptake. This compound is useful in research applications involving GABA metabolism and neurotransmitter modulation. -
GABA/nACh Receptor Inhibitor
APS3 is a potent inhibitor of GABA and nicotinic acetylcholine (nACh) receptors, showcasing a lethal concentration (LC50) of 7.2423 μg/mL against the pest Plutella xylostella. This compound is useful for studying neuropharmacological pathways and assessing the impact of receptor inhibition on insect behavior and survival. Applications include research in insect physiology and the development of pest management strategies. -
GABA Aminotransferase Inhibitor
Gabaculine is a potent inhibitor of GABA aminotransferase, an enzyme responsible for the degradation of gamma-aminobutyric acid (GABA). This compound, derived from the microbial strain Streptomyces toyocaensis, effectively increases GABA levels, thereby modulating neurotransmission and exhibiting potential anxiolytic effects. Gabaculine is widely utilized in neurobiological research to study neurotransmitter dynamics and the role of GABA in various neurological disorders. -
NMDA Receptor Inhibitor
Pregnanolone sulfate (pyridinium) is an endogenous neurosteroid that functions as an inhibitor of NMDA receptors. This compound exhibits neuroprotective properties, making it a valuable tool for investigating neurodegenerative disorders and synaptic plasticity. Its ability to modulate excitatory neurotransmission highlights its potential applications in both basic research and therapeutic development. -
Acetylcholinesterase Inhibitor, Butyrylcholinesterase Inhibitor, Carbonic Anhydrase I/II Inhibitor, α-Glycosidase Inhibitor
Vescalagin is a hexahydroxyphenol that acts as an inhibitor of acetylcholinesterase and butyrylcholinesterase, as well as carbonic anhydrases I and II, and α-glycosidase. It demonstrates potent inhibitory activity with Ki values of 5.87 nM for AChE, 3.89 nM for BChE, 11.75 nM for hCA I, 16.23 nM for hCA II, and 16.08 nM for α-glycosidase. Vescalagin exhibits non-competitive inhibition for hCA I, hCA II, and α-glycosidase, while also reducing hyperglycemia and hypertriglyceridemia in dietary models. Additionally, it possesses anti-inflammatory and antioxidant activities, making it a valuable compound for research in diabetes and metabolic disorders. -
NMDA Receptor Inhibitor
Bupivacaine is an NMDA receptor inhibitor that modulates neuronal excitability by blocking sodium, L-calcium, and potassium channels. It exhibits potent inhibition of SCN5A channels, with an IC50 of 69.5 μM. This compound is primarily utilized in research focused on chronic pain mechanisms and therapeutic interventions. -
NMDA Receptor Inhibitor
Bupivacaine-d9 is a deuterium-labeled analog of Bupivacaine, primarily targeting NMDA receptors. This compound exhibits inhibitory effects on sodium, L-calcium, and potassium channels, with a notable potency against SCN5A channels, characterized by an IC50 value of 69.5 μM. Bupivacaine-d9 is utilized in research related to chronic pain mechanisms and the modulation of excitatory neurotransmission, offering valuable insights into therapeutic applications in pain management. -
CaMKK2 Inhibitor
CaMKK2-IN-1 is a selective inhibitor of calcium/calmodulin-dependent protein kinase kinase 2 (CaMKK2) with an IC50 of 7 nM. This compound displays high ligand efficiency, making it a valuable tool for investigating the role of CaMKK2 in cellular signaling pathways. Its application in research includes studies on metabolism, cancer, and neurological disorders where the modulation of CaMKK2 activity may provide insights into therapeutic interventions. -
CAMKK2 Inhibitor
SGC-CAMKK2-1 is a selective inhibitor of calcium/calmodulin-dependent protein kinase kinase 2 (CAMKK2), exhibiting an IC50 of 30 nM. This compound effectively inhibits AMPK phosphorylation in C4-2 cells with an IC50 of 1.6 μM. SGC-CAMKK2-1 serves as a valuable chemical probe for investigating the role of CAMKK2 in various biological processes and pathways related to cellular energy regulation and metabolism. -
AChE/BChE Inhibitor
1,2-Didehydrotanshinone IIA is an inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), demonstrating an IC50 value of 5.98 μM for BChE. Additionally, this compound acts as an indoleamine 2,3-dioxygenase (IDO) inhibitor, with an IC50 value of 4.68 µM. Its dual inhibitory activity positions 1,2-Didehydrotanshinone IIA as a valuable reagent for research into neurodegenerative diseases and immune modulation. -
α-amylase/α-glucosidase/Acetylcholinesterase Inhibitor
Kaempferol-3,7-di-O-β-glucoside is a flavonol that acts as an inhibitor of α-amylase, α-glucosidase, and acetylcholinesterase. This compound has demonstrated protective effects on differentiating neuronal cells, specifically SH-SY5Y, against injury induced by Amyloid β peptide. Its enzyme inhibitory properties and neuroprotective effects indicate potential applications in Alzheimer's disease research and therapeutics. -
α-glucosidase/Acetylcholinesterase Inhibitor
7β-Hydroxybufalin is a bufadienolide that acts as a potent inhibitor of α-glucosidase and acetylcholinesterase. Isolated from the venom of Bufo bufo gargarizans, this compound demonstrates significant biological activity relevant to the modulation of carbohydrate and neurotransmitter metabolism. 7β-Hydroxybufalin is utilized in research applications focused on metabolic disorders and neurodegenerative diseases. -
sEH/AChE Inhibitor
sEH/AChE-IN-3 is a potent dual inhibitor of soluble epoxide hydrolase (sEH) and acetylcholinesterase (AChE), demonstrating IC50 values of 0.4 nM for human sEH and 1.94 nM for human AChE. This compound also exhibits inhibitory activity against human butyrylcholinesterase with an IC50 of 615 nM, and shows strong inhibition in both mouse sEH and AChE with IC50 values of 4.3 nM and 2.61 nM, respectively. Due to its ability to penetrate the blood-brain barrier, sEH/AChE-IN-3 is suitable for research applications in neuropharmacology and the study of neurological disorders. -
sEH/AChE Inhibitor
sEH/AChE-IN-4 is a potent dual inhibitor targeting soluble epoxide hydrolase (sEH) and acetylcholinesterase (AChE). It demonstrates impressive inhibitory activity with IC50 values of 3.1 nM against human sEH, 1660 nM against human AChE, 179 nM against human butyrylcholinesterase (hBChE), 14.5 nM against murine sEH, and 102 nM against murine AChE. This compound has potential applications in research areas related to neurodegenerative diseases and pain modulation, effectively crossing the blood-brain barrier. -
CerS6 Inhibitor, Ceramide Synthesis Inhibitor, Acetylcholinesterase Inhibitor
FF-C1 is a non-competitive inhibitor of Ceramide Synthase 6 (CerS6), exhibiting an IC50 of 7.89 μM. By inhibiting intestinal CerS6, FF-C1 effectively lowers serum ceramide levels, offering protective effects against metabolic dysfunction-associated steatohepatitis. This compound is also reported to inhibit acetylcholinesterase, highlighting its potential applications in studying metabolic disorders and neurodegenerative diseases. -
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. -
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. -
Monoamine Oxidase Inhibitor
MAO-B-IN-2 is a selective and competitive inhibitor of monoamine oxidase B (MAO-B) with an IC50 value of 0.51 μM, and it also inhibits butyrylcholinesterase (BChE) with an IC50 of 7.00 μM. This compound plays a significant role in studying neurodegenerative disorders by modulating monoamine metabolism, making it valuable for research into conditions such as Parkinson's disease and Alzheimer's disease. Its specificity for MAO-B makes it an important tool for exploring therapeutic pathways involving neurotransmitter regulation. -
O-GlcNAcase Inhibitor
O-GlcNAcase-IN-5 is a selective inhibitor of O-GlcNAcase, a key enzyme involved in the removal of O-GlcNAc modifications from proteins. By inhibiting this enzyme, O-GlcNAcase-IN-5 effectively prevents the deacetylation of tau protein, thereby reducing its excessive phosphorylation. This compound is particularly relevant for research in Alzheimer's disease and other neurodegenerative conditions where tau protein modification plays a critical role. -
OGT Inhibitor
OGT-IN-1 is a selective inhibitor of O-GlcNAc transferase (OGT), with IC50 values of 27 μM for soluble OGT (sOGT) and 10 μM for nuclear OGT (ncOGT). This compound plays a crucial role in regulating protein O-GlcNAcylation, thereby influencing various cellular processes such as signal transduction and gene expression. OGT-IN-1 is valuable for research applications focused on studying OGT-related metabolic disorders, cancer biology, and neurodegenerative diseases. -
OGT Inhibitor
PG 34 is a selective inhibitor of O-GlcNAc transferase (OGT), exhibiting an IC50 value of 68 μM. This compound targets the OGT enzyme, playing a crucial role in the regulation of O-GlcNAcylation. PG 34 is primarily applied in studies of cellular signaling, metabolic processes, and glycosylation-related research, offering insights into the role of OGT in various biological contexts. -
OGT Inhibitor
OGT-IN-4 is a potent inhibitor of O-GlcNAc transferase (OGT), displaying a dissociation constant (Kd) of 8 nM. This compound is valuable for investigating the role of OGT in various biological processes and diseases, including metabolic disorders and cancer. Its specificity makes OGT-IN-4 a useful tool for researchers studying O-GlcNAcylation and its impact on cellular signaling pathways. -
OGT Inhibitor
BZX2 is an irreversible covalent inhibitor of O-GlcNAc transferase (OGT), demonstrating an IC50 of less than 10 µM. This compound is cell-permeable, allowing for effective intracellular delivery, though it may exhibit multiple off-target effects. BZX2 is primarily utilized in research applications focused on OGT-related signaling pathways and O-GlcNAcylation processes in various biological contexts. -
TTBK1 Inhibitor
TTBK1-IN-1 is a selective inhibitor of tau tubulin kinase 1 (TTBK1), exhibiting an impressive IC50 of 2.7 nM. This compound demonstrates significant potential for the investigation of Alzheimer's disease and associated tauopathies. Additionally, TTBK1-IN-1 features an alkyne functional group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a valuable tool for click chemistry applications in biological research. -
TTBK1 Inhibitor
TTBK1-IN-2 is a selective inhibitor of Tau-Tubulin kinase 1 (TTBK1), exhibiting IC50 values of 0.24 µM and 4.22 µM. This compound demonstrates significant brain penetration in vivo and effectively reduces TDP-43 phosphorylation in both cell culture models and the spinal cord of transgenic TDP-43 mice. TTBK1-IN-2 is valuable for research focused on neurodegenerative diseases, particularly those associated with TDP-43 pathology. -
Tau and α-syn Inhibitor
MG-2119 is a potent inhibitor of tau and α-synuclein aggregation, primarily acting on the monomeric forms of these proteins. This compound demonstrates significant potential in the study of neurological disorders, making it a valuable tool for researchers investigating the pathophysiology of tauopathies and synucleinopathies. Its inhibitory effects on protein aggregation could provide insights into therapeutic strategies for related neurodegenerative diseases. -
Tau Aggregation Inhibitor
BSc3094 acts as a Tau aggregation inhibitor, targeting the pathological accumulation of tau protein implicated in neurodegenerative diseases. This compound has shown potential in research focused on Alzheimer's disease, making it a valuable tool for studying tau-related mechanisms and therapeutic interventions for neurodegeneration. -
Tau Protein Inhibitor
NQTrp is a potent inhibitor of tau protein aggregation, functioning primarily through its interaction with amyloidogenic structures. This naphthoquinone-tryptophan hybrid exhibits significant anti-amyloidogenic properties, effectively inhibiting the in vitro aggregation of hexapeptide 41GCWMLY46, located in the N-terminus of γD-crystallin, as well as the full-length γD-crystallin. NQTrp is a valuable reagent for research applications focusing on neurodegenerative disorders, particularly those associated with tau pathology. -
Tau Aggregation Inhibitor
TAU-IN-4 is a potent inhibitor of tau aggregation, demonstrating a KD of 1.58 μM. This compound is primarily utilized in research focused on Alzheimer's disease, where it aids in the exploration of tau-related pathophysiological mechanisms. Its capability to inhibit tau aggregation makes it a valuable tool for studying neurodegenerative processes and potential therapeutic interventions. -
DYRK1A Inhibitor
ZJCK-6-46 is a potent DYRK1A inhibitor, demonstrating an IC50 of 0.68 nM. This compound exhibits high blood-brain barrier permeability, making it suitable for central nervous system applications. ZJCK-6-46 effectively reduces tau phosphorylation, contributing to the amelioration of cognitive dysfunction by decreasing phosphorylated tau levels and mitigating neuronal loss in vivo. Its biological activity positions it as a valuable tool for researching neurodegenerative diseases. -
Tau Protein Aggregation Inhibitor
Tau protein aggregation-IN-1 is an inhibitor of Tau protein aggregation. It has demonstrated significant potential in the study of neurodegenerative disorders associated with protein misfolding, including Alzheimer's disease, dementia, Parkinson's disease, Huntington's disease, and prion-induced spongiform encephalopathies. This compound is essential for researchers investigating the mechanisms of Tau pathology and the development of therapeutic strategies targeting aggregated proteins. -
TTBK1/2 Inhibitor
TTBK1/2-IN-3 is a selective inhibitor of tau tubulin kinase 1 (TTBK1) and TTBK2, demonstrating IC50 values of 579 nM and 258 nM, respectively. This compound inhibits TDP-43 phosphorylation, thereby influencing protein aggregation pathways associated with neurodegenerative diseases. Additionally, TTBK1/2-IN-3 has been shown to reduce the expression of primary cilia on the surface of induced pluripotent stem cells (iPSCs), making it a valuable tool for research into cellular signaling and neurodegeneration. -
TTBK1/TTBK2 Inhibitor
AMG28 is a selective inhibitor of Tau tubulin kinase 1 (TTBK1) and TTBK2, with IC50 values of 805 nM and 988 nM, respectively. This compound effectively inhibits tau phosphorylation at Ser422, demonstrating an IC50 of 1.85 μM. AMG28 is primarily utilized in research investigating tau-related pathologies and neurodegenerative disorders. -
TTBK1 Inhibitor
(R)-TTBK1-IN-1 is a selective inhibitor of tau tubulin kinase 1 (TTBK1), demonstrating potent activity in targeting this enzyme. Its brain-penetrant properties make it particularly useful for studying Alzheimer's disease and related tauopathies. Additionally, (R)-TTBK1-IN-1 is equipped with an alkyne group, facilitating click chemistry applications through copper-catalyzed azide-alkyne cycloaddition (CuAAc) for further biochemical research. -
tau Protein Inhibitor
Sabeluzole (R 58735) serves as a tau protein inhibitor, demonstrating significant neuroprotective effects. This benzothiazol derivative exhibits antiischemic, antiepileptic, and cognitive-enhancing properties by mitigating NMDA- and glutamate-induced neurotoxicity through the inhibition of tau expression. Additionally, Sabeluzole has been shown to enhance memory in animal models and counters the amnesic effects of Chlordiazepoxide. Its applications extend to research on Alzheimer's disease, making it a valuable tool for investigating tau-related neurodegenerative mechanisms. -
TAU Inhibitor
TAU-IN-1 is a selective inhibitor of TAU protein with an EC50 value of 325 nM. This compound is primarily utilized in research focused on neurodegenerative diseases, particularly those related to tau pathology. Its ability to modulate Tau protein activity makes it a valuable tool for investigating mechanisms of neurodegeneration and potential therapeutic interventions. -
TTBK1 Inhibitor
TTBK1-IN-4 is a potent inhibitor of TTBK1, exhibiting a biochemical IC₅₀ of 2.3 nM and a cellular IC₅₀ of 42 nM. This compound serves as a valuable tool for investigating the role of TTBK1 in neurodegenerative diseases, particularly Alzheimer's disease. Researchers can utilize TTBK1-IN-4 to explore its potential therapeutic implications and the underlying mechanisms associated with TTBK1 activity. -
Tau-aggregation Inhibitor
Tau-aggregation-IN-5 is a potent inhibitor of Tau aggregation with an EC50 of 0.31 μM, targeting P4HB covalently. This compound induces mild endoplasmic reticulum (ER) stress, making it valuable for investigating neurodegenerative diseases, including Alzheimer's and Pick's diseases. Its unique mechanism allows for detailed studies of Tau pathology and potential therapeutic strategies. -
Tau Protein Aggregation Inhibitor
ACI-3024 is a potent, orally active inhibitor of Tau protein aggregation. It effectively reduces the β-sheet content and seeding properties of abnormal Tau proteins associated with various Tauopathies, thereby significantly alleviating Tau-induced neurodegeneration and neuroinflammation in cellular models. ACI-3024 serves as a valuable tool for research into neurodegenerative diseases. -
TAU Inhibitor
TAU-IN-3 is an orally active inhibitor of tau protein. This compound effectively inhibits the expression of the MAPT exon 10 DDPAC mutant gene in HeLa cells, demonstrating an IC50 of 0.6 µM. It reduces the 4-repeat/3-repeat MAPT mRNA ratio in cells with wild-type or DDPAC minigenes and inhibits the insertion of endogenous MAPT exon 10, subsequently decreasing the production of 4-repeat tau protein. TAU-IN-3 also modulates tau splicing in htau mice, yielding improvements in associated behavioral phenotypes, making it a valuable reagent for studies on neurodegenerative diseases. -
Tau Fibrilization Inhibitor
Ac-Val-Gln-aIle-Val-aTyr-Lys-NH2 is a N-amino peptide that selectively inhibits tau protein fibrilization. This compound effectively prevents the cellular seeding of endogenous tau by binding to both monomeric and fibrillar forms of extracellular tau. Ac-Val-Gln-aIle-Val-aTyr-Lys-NH2 is valuable for research in neurodegenerative diseases, including Alzheimer's disease, providing insight into tau pathology and potential therapeutic interventions.
