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Catalog No.
Product Name
Application
Product Information
Citations
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tau protein aggregation inhibitor
TRx 0237 (LMT) mesylate is a second-generation tau protein aggregation inhibitor for the treatment of Alzheimer's disease (AD) and frontotemporal dementia. -
Tau Aggregation Inhibitor
Nimbin is a potent tau aggregation inhibitor derived from the limonoid class of compounds found in Azadirachta. It is shown to enhance cell viability while effectively inhibiting the envelope protein of the dengue virus. Additionally, Nimbin exhibits a range of biological activities, including anti-inflammatory, antifungal, antihistamine, antiseptic, antioxidant, anticancer, and antiviral properties. This diverse activity profile makes Nimbin a valuable reagent for research in neurodegenerative diseases and viral infections. -
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. -
GSK3β Inhibitor
GSK3β-IN-3 is an ATP-competitive inhibitor of glycogen synthase kinase 3 beta (GSK3β), exhibiting an IC50 of 0.90 μM. It effectively lowers the phosphorylation levels of tau protein in the BR5706 strain and reduces the accumulation of amyloid-beta (Aβ) aggregates in the CL2006 strain. This compound is essential for research applications focused on Alzheimer's disease (AD), aiding in the understanding of neurodegenerative mechanisms and potential therapeutic strategies. -
Tau-aggregation and Neuroinflammation Inhibitor
Tau-aggregation and neuroinflammation-IN-1 is an effective inhibitor of tau aggregation and neuroinflammation. This compound demonstrates significant inhibitory activity against both AcPHF6 and full-length tau aggregation, while exhibiting low cytotoxicity. Additionally, it reduces nitric oxide release in lipopolysaccharide-stimulated BV2 cells. Research applications include investigations into memory impairment, as Tau-aggregation and neuroinflammation-IN-1 has been shown to reverse okadaic acid-induced cognitive deficits in rat models. -
Tau Aggregation Inhibitor
3,3'-Diethyl-9-methylthiacarbocyanine iodide is a cyanine dye that functions as a tau aggregation inhibitor, exhibiting an IC50 value of 0.28 μM for tau proteins. It interferes with the proper functioning of the microtubule cytoskeleton, making it valuable for studies investigating tau pathologies. This compound is particularly relevant in Alzheimer's disease research, enabling the exploration of therapeutic strategies targeting tau aggregation. -
Tau441 Aggregation Inhibitor
Tau-aggregation-IN-1 is a potent inhibitor of tau441 protein aggregation, exhibiting an IC50 value of 21 µM. This compound also acts as an agonist for dopamine D2 and D3 receptors, making it relevant in studies of neurodegenerative diseases and tauopathies. Its dual mechanism offers potential for investigating tau-related pathologies and dopaminergic signaling in experimental research settings. -
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. -
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. -
Tau Inhibitor
TAU-IN-6 is a selective inhibitor of Tau protein misfolding and aggregation. It effectively inhibits the formation of stress granules comprising Tau and TIA1, making it a valuable tool in studying Tau pathology. This compound is particularly relevant for research related to Alzheimer's disease and other tauopathies. -
TTBK1/TTBK2 Inhibitor
TTBK1/2-IN-2 is a selective inhibitor of Tau tubulin kinase 1 (TTBK1) and TTBK2, exhibiting IC50 values of 384 nM and 175 nM, respectively. This compound has been shown to significantly influence ciliogenesis in human induced pluripotent stem cells (iPSCs), making it a valuable tool for studying the roles of TTBK1 and TTBK2 in cellular processes and related pathologies. Its potent inhibitory activity positions TTBK1/2-IN-2 as an important reagent for research in neurodegenerative diseases and cilia-related disorders. -
Tau-aggregation Inhibitor
Tau-aggregation-IN-3 is a potent inhibitor of Tau protein aggregation, demonstrating an EC50 value of 4.816 μM in cell-based assays. This compound is valuable for research into neurodegenerative diseases, particularly Alzheimer's disease, where Tau aggregation plays a critical role in pathogenesis. Its ability to inhibit Tau aggregation makes it a useful tool for investigating therapeutic strategies aimed at Tau-related mechanisms. -
TAU Inhibitor
TAU-IN-2 is a selective TAU inhibitor that demonstrates an EC50 value of 7.7 nM. This compound is primarily utilized in the investigation of neurodegenerative diseases, making it a valuable tool for researchers studying the role of TAU protein aggregation in conditions such as Alzheimer’s disease. Its potent inhibitory action allows for detailed exploration of TAU-related pathways and potential therapeutic interventions. -
Tau Protein Inhibitor
LDN-193665 is a potent inhibitor of Tau kinases, demonstrating significant tauopathy-modifying activity. This compound effectively reduces Tau phosphorylation and decreases Sarkosyl-insoluble Tau levels in preclinical models. Additionally, LDN-193665 has been shown to enhance cognitive function, restoring memory in animal studies and highlighting its potential application in researching tauopathies. -
TTBK1/TTBK2 Inhibitor
TTBK1/2-IN-1 is a selective inhibitor of Tau tubulin kinases TTBK1 and TTBK2, demonstrating IC50 values of 816 nM and 384 nM, respectively. This compound effectively interferes with tau phosphorylation, making it a valuable tool in research focused on tauopathies and neurodegenerative diseases. Its application can aid in understanding the role of TTBK1 and TTBK2 in cellular processes and serve as a basis for the development of therapeutics targeting tau-related pathologies. -
TTBK1 Inhibitor
TTBK1-IN-3 is a selective inhibitor of TTBK1, exhibiting a biochemical IC₅₀ of 18 nM and a cellular IC₅₀ of 259 nM. This compound is valuable for investigating the role of TTBK1 in Alzheimer's disease research. Its potency allows for detailed studies on the enzymatic pathways involved in neurodegenerative processes. -
Tau/pre-miRNA-146a Inhibitor
MG-1102 is a first-in-class dual binder targeting both monomeric tau and pre-miRNA-146a. It exhibits specific inhibition of pre-miRNA-146a, with IC50 values of 0.21 mM for double-labeled and 0.36 mM for mono-labeled forms. Additionally, MG-1102 shows a binding affinity for tau monomers, characterized by a Kd of 3.21 mM as determined by surface plasmon resonance (SPR). This compound serves as a potential multi-target-directed ligand (MTDL) for research applications related to Alzheimer’s disease. -
Tau Protein Aggregation Inhibitor
Hydromethylthionine dihydrobromide is a potent inhibitor of tau protein aggregation. By interacting with tau proteins, it effectively prevents the formation of neurotoxic aggregates, thereby reducing neurodegeneration. This compound is valuable for research involving Alzheimer's disease and other tau-related disorders, providing insights into the mechanisms of neurodegenerative processes. -
TTBK1 Inhibitor
TTBK1-IN-5 is a selective inhibitor of TTBK1, exhibiting an IC₅₀ value of 239 nM. It is designed for studies investigating the role of TTBK1 in neurodegenerative disorders, particularly Alzheimer's disease. This compound facilitates research aimed at understanding TTBK1's biological function and its potential as a therapeutic target in Alzheimer's pathology. -
Tau-0N4R Inhibitor
Tau-0N4R-IN-1 is an effective inhibitor of tau 0N4R oligomerization, capable of penetrating the blood-brain barrier. This compound demonstrates significant biological activity by inhibiting tau fibrosis across different isoforms, exhibiting anti-seeding effects on tau in vitro, and dose-dependently reducing α-synuclein oligomerization and inclusions. Additionally, Tau-0N4R-IN-1 is stable in mouse microsomes and has been shown to decrease amyloid-beta plaques in brain tissues from Alzheimer's disease patients, making it a valuable reagent for neurological research and drug development. -
Tau/Amyloid-β Aggregation Inhibitor
TRV-1387 is a benzofurazan compound that functions as an inhibitor of tau and amyloid-β aggregation. It demonstrates significant biological activity in preventing the formation of toxic aggregates associated with neurodegenerative diseases, making it a valuable tool for research in Alzheimer's disease and related pathologies. TRV-1387 can be utilized to study the mechanisms of amyloid-related toxicity and to explore potential therapeutic strategies targeting protein aggregation. -
Tau/Aβ Inhibitor
D-687 is a selective inhibitor of Tau and amyloid-beta (Aβ) aggregation. It has demonstrated the ability to reverse Aβ1–42-induced neurotoxicity in SH-SY5Y neuronal cells, highlighting its significant neuroprotective effects. This compound is valuable for research focused on Alzheimer's disease and related neurodegenerative disorders. -
Tau/Aβ Inhibitor
D-688 is a potent inhibitor of Tau and amyloid-beta (Aβ), demonstrating significant neuroprotective properties. This compound effectively reverses Aβ1–42-induced toxicity in SH-SY5Y neuronal cells, making it a valuable tool for studying neurodegenerative processes. Additionally, D-688 improves the survival rate of Drosophila melanogaster models expressing the human tau protein isoform (2N4R), underscoring its potential in Alzheimer's disease research and related disorders. -
Aβ40/tau Aggregation Inhibitor
Tau/Aβ40 aggregation-IN-1 is a potent inhibitor of tau and Aβ40 aggregation, exhibiting IC50 values of 1.8 μM and 1.3 μM, respectively. This compound is of significant interest in Alzheimer's disease research, as it targets the pathological aggregation of tau protein and amyloid-beta peptides. Its effectiveness in modulating these protein interactions makes it a valuable tool for studying neurodegenerative mechanisms and potential therapeutic interventions. -
MAO-B Inhibitor
MAO-B-IN-50 is a selective inhibitor of monoamine oxidase B (MAO-B), demonstrating an IC50 value of 0.06 μM. This compound is effective in inhibiting the aggregation of amyloid-beta (Aβ40/42) and Tau proteins, with overall IC50 values near 1 μM. Additionally, MAO-B-IN-50 shows potent selective inhibition of acetylcholinesterase (AChE) with an IC50 of 1.78 μM. It is suitable for use in research related to Alzheimer's disease. -
Aβ Fibrillogenic Inhibitor
Acetyl-Tau Peptide (273-284) amide is an acetylated fragment of the Tau protein that acts as an inhibitor of Aβ fibrillogenesis. It effectively reduces the aggregation of Ac-Aβ(25–35)-NH2, facilitating studies on the interplay between Aβ and Tau proteins. This peptide serves as a valuable experimental tool for investigating the mechanisms underlying Alzheimer's disease and related neurodegenerative conditions. -
Amyloid-Beta and Tau Inhibitor
Aβ/tau aggregation-IN-1 is a selective inhibitor of amyloid-beta (Aβ1-42) β-sheet formation and tau protein aggregation. With KD values of 160 μM for Aβ1-42 and 337 μM for tau, this compound demonstrates significant potential in research related to neurodegenerative disorders such as Alzheimer's disease. Its ability to cross the blood-brain barrier further supports its use in studies aimed at understanding the pathophysiology of amyloid and tau accumulation in the central nervous system. -
Aβ/tau Protein Aggregation Inhibitor
DN5355 is a small molecule inhibitor of amyloid β protein (Aβ) and hyperphosphorylated tau protein aggregation. It effectively inhibits the formation of Aβ and tau fibrils while also promoting the disaggregation of pre-formed aggregates. This compound is valuable for research applications focused on Alzheimer's disease and the underlying mechanisms of protein aggregation associated with neurodegeneration.
