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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 protein (592-597), human TFA is a peptide fragment of human Tau protein. The dysfunction of Tau protein is involved in neurodegeneration and dementia.
- Tau Peptide (306–317) is a synthetic polypeptide fragment identified through peptide screening, a research technique that pools and evaluates active peptides—primarily via immunoassays. Peptide screening is widely used for studying protein–protein interactions, functional analysis, and epitope mapping, making Tau Peptide (306–317) a valuable tool in the research and development of therapeutic agents, particularly in neurodegenerative disease studies.
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Tau Scavenger
C004019 is a small-molecule PROTAC designed to target tau, functioning as a tau scavenger. This compound effectively recruits tau and E3 ligase, promoting the ubiquitination and proteasome-dependent degradation of tau proteins. C004019 has demonstrated the potential to enhance synaptic and cognitive functions in models of Alzheimer's disease, making it a valuable tool for research into Alzheimer's and tau protein-related pathologies. -
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. -
Tau ATTEC
MRL828 is a Tau pathology-binding compound that employs the ATTEC technology to selectively target aggregated tau proteins for degradation via the autophagic lysosomal pathway. This reagent effectively decreases intracellular tau aggregates while promoting the secretion of tau from cells. Its unique mechanism makes MRL828 a valuable tool for research on tau-related pathologies and neurodegenerative diseases. -
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. -
Anti-aggregation Agent
CLR01 sodium is an anti-aggregation agent that effectively penetrates the blood-brain barrier. It inhibits the de novo aggregation of key proteins, including Amyloid-β 40/42, α-synuclein, IAPP, tau protein, and SOD1. CLR01 sodium has demonstrated the ability to reduce amyloid plaque burden in the cortex of triple-transgenic mice, resulting in improvements in memory and motor functions. This compound is applicable in research focused on neurodegenerative disorders such as Alzheimer's disease, Parkinson's disease, and amyotrophic lateral sclerosis (ALS). -
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 Tracer
Tau Tracer 2 (PI-2620) is a selective imaging agent targeting Tau protein aggregates. It is designed for the visualization and diagnosis of neurodegenerative diseases, aiding in the assessment of Tau pathology. This reagent is valuable for researchers exploring Tau-related mechanisms and monitoring the progression of Tau-associated disorders. -
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. -
Tau Binding Drug
THK-5117 is an arylquinoline derivative that exhibits a strong binding affinity to tau fibrils, with a Ki of 10.5 nM. It shows remarkable specificity for tau protein aggregates, making it a valuable tool for studying tau pathology in Alzheimer's disease. Additionally, 18F-THK-5117 has potential applications in tau imaging as a PET probe, providing insights into tau-related neurodegenerative processes. -
Tau Tracer
Tau Tracer 1 is a selective imaging agent designed for the visualization of Tau protein aggregates, a hallmark of neurodegenerative diseases. This compound enables the detection and quantification of Tau pathology, facilitating the diagnosis and study of conditions such as Alzheimer's disease. Its application is crucial in both preclinical and clinical research settings, allowing for a better understanding of Tau-related pathologies. -
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. -
Tau Imaging Probe
THK-5105 is an arylquinoline derivative that serves as a tau imaging probe, exhibiting high binding affinity for tau fibrils and protein aggregates. Its specific interaction with tau-rich Alzheimer disease brain homogenates makes it a valuable tool for studying tau pathology. The radiofluorinated derivative, 18F-THK-5105, is particularly promising for use as a positron emission tomography (PET) imaging probe in Alzheimer's research. -
FLNA Modulator
Simufilam hydrochloride is an orally active modulator of filamin A (FLNA) that targets neuronal signaling pathways. This compound restores NMDAR signaling and Arc expression while inhibiting dysregulated mTOR activity. Additionally, it enhances insulin sensitivity and mitigates Aβ42-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam hydrochloride is applicable in research related to Alzheimer's disease, particularly in understanding the underlying mechanisms of neurodegeneration. -
FLNA Modulator
Simufilam is an orally active modulator of filamin A (FLNA) that restores NMDA receptor (NMDAR) signaling and Arc expression. It effectively inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, which results in improved insulin sensitivity and a reduction in Aβ42-induced neuroinflammation and tau protein hyperphosphorylation. This compound is particularly valuable for research applications focused on Alzheimer's disease and related neurodegenerative disorders. -
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. -
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. -
α-Synuclein/Tau Degrader
PROTAC α-Synuclein/Tau degrader 1 targets α-synuclein and tau for degradation through the ubiquitin-proteasome system. This dual PROTAC degrader demonstrates effective binding with dissociation constants of 0.47 μM and 2.78 μM for α-synuclein and tau, respectively, and has DC50 values of 1.57 μM and 4.09 μM. Its ability to penetrate the blood-brain barrier makes it a valuable tool for research into neurodegenerative diseases, particularly Parkinson's disease. The compound's design includes components for ligand binding and a linker optimized for efficient degradation. -
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. -
PET Tracer
PBB3 is a positron emission tomography (PET) tracer that targets tau protein accumulation. It is utilized in the detection and quantification of tau levels in neurodegenerative diseases, including Alzheimer's disease as well as other tauopathies. PBB3 serves as a valuable tool in research aimed at understanding tau pathology and its implications in cognitive decline. -
Tau-lowering Antisense Oligonucleotide
Diranersen is a Tau-lowering antisense oligonucleotide designed to target and inhibit tau protein expression. This compound holds potential for advancing research in Alzheimer’s disease and related neurodegenerative conditions. By reducing tau levels, Diranersen aims to facilitate studies focused on tau pathology and its implications in Alzheimer's progression. -
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 Fibrils Decomposing Agent
CNS-11 is a tau fibril-degrading agent that effectively penetrates the blood-brain barrier. This compound demonstrates the ability to reduce α-synuclein levels, making it a valuable tool in the study of neurodegenerative disorders. CNS-11 is applicable in research focused on Alzheimer's and Parkinson's diseases, contributing to the understanding of tau pathology and its implications in these conditions. -
Tau Ligand
Florzolotau is a tau ligand designed for positron emission tomography (PET) imaging, targeting the β-sheet region of paired helical filaments (PHFs) and straight filaments (SFs) of tau protein. Its binding affinity extends to intraneuronal inclusions present in Alzheimer's disease, primary age-related tauopathy, and posterior cortical atrophy. This compound shows significant potential in the diagnosis and study of tau proteinopathies, facilitating improved imaging of neurological disorders associated with tau aggregation. -
Secreted Clusterin Enhancer
DDL-357 is a potent enhancer of secreted clusterin, targeting key pathways involved in neurodegenerative processes. It effectively reduces levels of phosphorylated tau in the brain, contributing to memory improvement in the murine 3xTg-AD model. This compound is a valuable tool for researching therapeutic strategies in Alzheimer's disease and related cognitive disorders. -
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 Ligand
Tau Ligand-1 is a specific ligand that targets aggregated tau protein and is capable of crossing the blood-brain barrier. Demonstrating high affinity for aggregated tau in brain tissues from Alzheimer's disease and other tauopathies, it displays equilibrium dissociation constant (KD) values between 1 and 3.8 nM. This compound shows potential as a positron emission tomography (PET) tracer, offering valuable applications in imaging studies related to tau-associated neurodegenerative diseases in the central nervous system. -
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. -
THK5351 R enantiomer
THK5351 (R enantiomer) is a selective ligand for the translocator protein (TSPO), which is involved in neuroinflammation. This compound exhibits high affinity for TSPO and is utilized in research related to neurodegenerative diseases, allowing for the visualization of neuroinflammatory processes in vivo. THK5351 (R enantiomer) serves as an invaluable tool in studying the role of inflammation in the pathogenesis of disorders such as Alzheimer's disease and other neurodegenerative conditions. -
THK5351 R enantiomer
THK5351 is a selective radiolabeled ligand targeting tau pathology in the brain. This compound serves as a radiotracer for in vivo imaging, facilitating the study of tau-related neurodegenerative diseases such as Alzheimer's. The application of THK5351 in research enables the visualization and quantification of tau aggregation, providing essential insights into disease progression and potential therapeutic interventions. -
Tau fragment R2
Tau Peptide (275-305) targets the second repeat domain of the tau protein, which plays a critical role in microtubule binding and is implicated in Alzheimer's disease. This peptide specifically interacts with group IIB metal ions (Zn²⁺, Cd²⁺, Hg²⁺), facilitating conformational changes and promoting pathological accumulation. Research applications include investigating the effects of heavy metals on tau protein dynamics and their contributions to neurodegenerative disease mechanisms. -
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. -
Tau Fragment
Tau Peptide (273-284) is a truncated fragment of the Tau protein, primarily involved in neurofibrillary tangles associated with tauopathies. This peptide is valuable for studying the molecular mechanisms of Alzheimer's disease and other related neurodegenerative disorders. It serves as a tool for elucidating Tau aggregation processes and investigating potential therapeutic interventions targeting Tau-related pathologies. -
Tau Protein
JG-23 is a 4-chloro modified analog that effectively promotes the degradation of tau protein. Demonstrating good metabolic stability, JG-23 has a half-life of 36 minutes in mouse liver microsome assays. This compound is valuable for research focused on tau-related neurodegenerative diseases and the underlying mechanisms of tau protein regulation. -
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. -
Polypeptide
Tau Peptide (255-314) (Repeat 2 Domain) (human) is a polypeptide derived from the Tau-F protein, specifically the 255-314 fragment of this key isoform. This peptide encompasses critical aggregation sequences PHF6* (275-280, VQIINK) and PHF6 (306-311, VQIVYK), which play a significant role in Tau aggregation. It spans the C-terminal half of the repeat domain R1, the entire repeat domain R2, and the N-terminal half of repeat domain R3, making it vital for studies on Tau-related neurodegenerative processes and microtubule dynamics. -
MAPT Splicing Modulator
PTC-700 is a potent modulator of microtubule-associated protein tau (MAPT) splicing. This compound effectively reduces 4-repeat isoform MAPT levels in P301L and S305N neuronal models, exhibiting EC50 values of 1.3-1.8 nM and 0.5-2.6 nM, respectively. PTC-700 is utilized in research applications focused on tauopathies and neurodegenerative disorders, contributing to the understanding of tau protein dynamics and potential therapeutic avenues. -
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 Ligand
T808 is a selective ligand targeting tau protein, crucial in Alzheimer's disease research. This compound can be utilized to synthesize [18F]-T808, a highly selective tau protein positron emission tomography (PET) tracer, facilitating in vivo imaging studies. Additionally, T808 serves in the synthesis of [3H]-T808, a radioactive marker suitable for in vitro experiments, further advancing our understanding of tau-related pathologies. -
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.

