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Tau Inhibitors

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64

Inhibitors & Agonists

2

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2

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4

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-146005
    Tau-aggregation and neuroinflammation-IN-1

    		Microtubule/Tubulin Neurological Disease Inflammation/Immunology
    Tau-aggregation and neuroinflammation-IN-1 is a potent tau-aggregation and neuroinflammation inhibitor. Tau-aggregation and neuroinflammation-IN-1 exhibits remarkable inhibitory activities against AcPHF6 and full-length tau aggregation. Tau-aggregation and neuroinflammation-IN-1 has a low cytotoxicity and reduced NO release in LPS-stimulated BV2 cells. Tau-aggregation and neuroinflammation-IN-1 can reverse okadaic acid-induced memory impairment in rats .
    Tau-aggregation and neuroinflammation-IN-1
  • HY-141661
    Aβ/tau aggregation-IN-1

    		Amyloid-β Neurological Disease
    Aβ/tau aggregation-IN-1 is a potent Aβ1-42 β-sheets formation and tau aggregation inhibitor. The KD values of Aβ/tau aggregation-IN-1 with Aβ1-42 and tau are 160 μM and 337 μM, respectively. Aβ/tau aggregation-IN-1 can permeate the blood-brain barrier .
    Aβ/tau aggregation-IN-1
  • HY-13486
    TAU-IN-1

    		Tau Protein Neurological Disease
    TAU-IN-1 (compound 051) is a TAU protein inhibitor with an EC50 value of 325 nM. TAU-IN-1 can be used in the study of neurodegenerative diseases .
    TAU-IN-1
  • HY-156435
    tau protein/α-synuclein-IN-1

    		α-synuclein Neurological Disease
    tau protein/α-synuclein-IN-1 is a dual inhibitor of tau protein and α-synuclein. tau protein/α-synuclein-IN-1 reduces α-syn inclusions development in M17D neuroblastoma cells. tau protein/α-synuclein-IN-1 can be used in study Alzheimer’s disease .
    tau protein/α-synuclein-IN-1
  • HY-146135
    Tau-aggregation-IN-1

    		Microtubule/Tubulin Dopamine Receptor Neurological Disease
    Tau-aggregation-IN-1 (Compound D-519) is a tau441 protein aggregation inhibitor with an IC50 of 21 µM. Tau-aggregation-IN-1 is also a dopamine D2 and D3 receptor agonist .
    Tau-aggregation-IN-1
  • HY-P4832
    Acetyl-Tau Peptide (273-284) amide

    		Amyloid-β Neurological Disease
    Acetyl-Tau Peptide (273-284) amide is an acetylated Tau peptide fragment. Acetyl-Tau Peptide (273-284) amide limits the substantial aggregation of Ac-Aβ(25–35)-NH2 and can be used as an inhibitor of Ac-Aβ(25–35)-NH2. Acetyl-Tau Peptide (273-284) amide can be used as an experimental model to investigate the Aβ/Tau cross-interaction .
    Acetyl-Tau Peptide (273-284) amide
  • HY-153427
    Tau protein aggregation-IN-1

    		Tau Protein Neurological Disease
    Tau protein aggregation-IN-1 (Compound 0c) is a Tau protein aggregation inhibitor. Tau protein aggregation-IN-1 can be used in the study of protein folding disorders such as Alzheimer's disease, dementia, Parkinson's disease, Huntington's disease and prion-based spongiform encephalopathies .
    Tau protein aggregation-IN-1
  • HY-149233
    hAChE-IN-1

    		Cholinesterase (ChE) Tau Protein Neurological Disease
    hAChE-IN-1 (Compound 24) is a potent hAChE inhibitor with an IC50 of 1.09 μM. hAChE-IN-1 inhibits tau-oligomerization with an EC50 of 2.71 μM in cellular tau FRET assay .
    hAChE-IN-1
  • HY-149272
    tau/Aβ40 aggregation-IN-1

    		Tau Protein Amyloid-β Cholinesterase (ChE) Neurological Disease
    tau/Aβ40 aggregation-IN-1 (Compound 20) is a tau and Aβ40 aggregation inhibitor with IC50s of 1.8 μM and 1.3 μM, respectively .
    tau/Aβ40 aggregation-IN-1
  • HY-153431
    TRV-1387

    		Tau Protein Amyloid-β Neurological Disease
    TRV-1387 is a benzofurazan that inhibits the aggregation of tau and amyloid-β .
    TRV-1387
  • HY-153986
    AEP-IN-2

    		Others Neurological Disease
    AEP-IN-2 is an asparagine endopeptidase (AEP) inhibitor via block AEP cleavage of APP and Tau. AEP-IN-2 has oral activity and decreases Aβ40 and Aβ42 and p-Tau levels .
    AEP-IN-2
  • HY-141660
    BSc3094

    		Tau Protein Neurological Disease
    BSc3094 is a Tau aggregation inhibitor. BSc3094 can be used for the research of Alzheimer's disease (AD) .
    BSc3094
  • HY-153430
    Aβ/tau aggregation-IN-3

    		Amyloid-β Neurological Disease
    Aβ/tau aggregation-IN-3 is a potent amyloid protein aggregation inhibitor with an IC50 of 0.85 μM by Aβ-Thioflavin T (Aβ-ThT) functional aggregation assay. Aβ/tau aggregation-IN-3 has anti-amyloid activity .
    Aβ/tau aggregation-IN-3
  • HY-12662
    PE859
    1 Publications Verification

    		 Microtubule/Tubulin Neurological Disease
    PE859 is a potent inhibitor of both tau and Aβ aggregation with IC50 values of 0.66 and 1.2 μM, respectively.
    PE859
  • HY-N0249
    Saikosaponin C

    		Amyloid-β Neurological Disease
    Saikosaponin C is a bioactive component found in radix bupleuri, targets amyloid beta and tau in Alzheimer's disease. Saikosaponin C inhibits the secretion of both Aβ1-40 and Aβ1-42, and suppresses abnormal tau phosphorylation, but shows no effect on BACE1 activity and expression .
    Saikosaponin C
  • HY-163145
    α-Synuclein inhibitor 11

    		α-synuclein Neurological Disease
    α-Synuclein inhibitor 11 (compound 1) is a selective α-synuclein (α-syn) oligomer formation inhibitor. α-Synuclein inhibitor 11 does not inhibits tau 4R (isoforms 0N4R, 2N4R) or p-tau (isoform 1N4R). α-Synuclein inhibitor 11 can be used for Parkinson's disease (PD) research .
    α-Synuclein <em>inhibitor</em> 11
  • HY-154988
    MARK4 inhibitor 4

    		Others Neurological Disease Cancer
    MARK4 inhibitor 4 is a MARK4 inhibitor with an IC50 of 1.49 μM. MARK4 inhibitor 4 can be used in cancer and tau lesion-related research .
    MARK4 <em>inhibitor</em> 4
  • HY-100348
    EPI-001

    EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer .
    EPI-001
  • HY-139307
    MG-2119

    		Tau Protein Neurological Disease
    MG-2119 is a potent monomeric tau and α-syn aggregation inhibitor. MG-2119 is a potential agent for neurological disorders research .
    MG-2119
  • HY-139830
    Dyrk1A-IN-1

    		DYRK Neurological Disease
    Dyrk1A-IN-1 is a triple inhibitor of Dyrk1A kinase activity (IC50 = 119 nM) and the aggregation of tau and α-syn oligomers.
    Dyrk1A-IN-1
  • HY-144290
    ARN25068

    		GSK-3 DYRK Neurological Disease
    ARN25068 is a sub-micromolar inhibitor of the three protein kinases, GSK-3β, FYN and DYRK1A to tackle tau hyperphosphorylation .
    ARN25068
  • HY-111935
    3,3'-Diethyl-9-methylthiacarbocyanine iodide

    		Microtubule/Tubulin Neurological Disease
    3,3'-Diethyl-9-methylthiacarbocyanine iodide is a cyanine dye, also a tau aggregation inhibitor, with an IC50 value of 0.28 μM for tau. 3,3'-Diethyl-9-methylthiacarbocyanine iodide can cause misfunction of the microtubule cytoskeleton. 3,3'-Diethyl-9-methylthiacarbocyanine iodide can be used for researching Alzheimer’s disease .
    3,3'-Diethyl-9-methylthiacarbocyanine iodide
  • HY-P3307
    Ac-Val-Gln-aIle-Val-aTyr-Lys-NH2

    		Tau Protein Neurological Disease
    Ac-Val-Gln-aIle-Val-aTyr-Lys-NH2 is serum stable, non-toxic to neuronal cells, and selectivity inhibits the fibrilization of tau over Aβ42.
    Ac-Val-Gln-aIle-Val-aTyr-Lys-NH2
  • HY-158030
    HDAC6-IN-37

    		HDAC Neurological Disease
    HDAC6-IN-37 (compound W5) is an inhibitor of HDAC6 and has neuroprotective effects. HDAC6-IN-37 can restore the morphology of hippocampal neurons, reduce the expression of Aβ, Tau, and p-Tau proteins in the hippocampus of AD rats, and inhibit the formation of senile plaques and neurofibrillary tangles. Thus, HDAC6-IN-37 improves the Aβ/Cu 2+-induced AD model in rats, regulates oxidative stress status, and balances neurotransmitter disorders in brain tissue .
    HDAC6-IN-37
  • HY-100348R
    EPI-001 (Standard)

    		Androgen Receptor PPAR Apoptosis Cancer
    EPI-001 (Standard) is the analytical standard of EPI-001. This product is intended for research and analytical applications. EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer .
    EPI-001 (Standard)
  • HY-149237
    hAChE-IN-2

    		Cholinesterase (ChE) Tau Protein Neurological Disease
    hAChE-IN-2 is a potent hAChE inhibitor, with an IC50 of 0.71 μM. hAChE-IN-2 can also inhibits tau-oligomerization, with an EC50 of 2.21 μM. hAChE-IN-2 exhibits neuroprotective activity .
    hAChE-IN-2
  • HY-124832
    δ-Secretase inhibitor 11

    		Caspase Amyloid-β Neurological Disease
    δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research .
    δ-Secretase <em>inhibitor</em> 11
  • HY-19738
    NQTrp

    NQTrp, an aromatic naphthoquinone-tryptophan hybrid molecule, an inhibitor of the aggregation of the tau protein with generic anti-amyloidogenic effects. NQTrp inhibits the in vitro aggregation of hexapeptide ( 41GCWMLY 46 within the N-terminus of γD-crystallin) as well as full-length γD-crystallin .
    NQTrp
  • HY-122243
    IU1-47

    		Deubiquitinase Neurological Disease
    IU1-47 is a potent and specific USP14 inhibitor with an IC50 of 0.6 μM. IU1-47 inhibits IsoT/USP5 with an IC50 of 20 μM. IU1-47 induces tau elimination in cultured neurons .
    IU1-47
  • HY-161328
    MAO-B-IN-31

    		Monoamine Oxidase α-synuclein Tau Protein Neurological Disease
    MAO-B-IN-31 (Compound 30) is an effective and selective inhibitor of monoamine oxidase B (monoamine oxidase B). The IC50 value is 41 nM. MAO-B-IN-31 also inhibits α-syn and tau aggregation. MAO-B-IN-31 has neuroprotective activity .
    MAO-B-IN-31
  • HY-139324
    Cu(II)GTSM
    1 Publications Verification

    		 GSK-3 Amyloid-β Neurological Disease
    Cu(II)GTSM, a cell-permeable Cu-complex, significantly inhibits GSK3β. Cu(II)GTSM inhibits Amyloid-β oligomers (AβOs) and decreases tau phosphorylation. Cu(II)GTSM also decreases the abundance of Amyloid-β trimers. Cu(II)GTSM is a potential anticancer and antimicrobial agent .
    Cu(II)GTSM
  • HY-19948
    Leucomethylene blue mesylate
    5 Publications Verification

    TRx0237 mesylate; Methylene blue leuco base mesylate

    		 Amyloid-β Neurological Disease
    Leucomethylene blue (TRx0237) mesylate, an orally active second-generation tau protein aggregation inhibitor (Ki of 0.12 μM), could be used for the study of Alzheimer's Disease. Leucomethylene blue mesylate is a common reduced form of Methylene Blue, Methylene Blue is a member of the thiazine class of dyes .
    Leucomethylene blue mesylate
  • HY-144775
    AChE-IN-10

    		Cholinesterase (ChE) Neurological Disease
    AChE-IN-10 (Compound 24r) is a potent inhibitor of AChE (IC50 = 2.4 nM). AChE-IN-10 potently inhibits AChE, reduces tau phosphorylation at S396 residue, provides neuroprotection by rescuing neuronal morphology and increasing cell viability. AChE-IN-10 is also found to reduce amyloid aggregation in the presence of AChE .
    AChE-IN-10
  • HY-103157
    PD146176
    2 Publications Verification

    NSC168807

    		 Autophagy Ferroptosis Cardiovascular Disease
    PD146176 (NSC168807), a 15-Lipoxygenase (15-LO) inhibitor, inhibits rabbit reticulocyte 15-LO (Ki=197 nM, IC50=0.54 μM). PD146176 reverses cognitive impairment, brain amyloidosis, and tau pathology by stimulating autophagy in aged triple transgenic mice .
    PD146176
  • HY-150585
    BuChE-IN-5

    		Amyloid-β Cholinesterase (ChE) Tau Protein Neurological Disease
    BuChE-IN-5 (compound 25b) is a potent BuChE inhibitor with an IC50 value of 1.94 μM. BuChE-IN-5 efficiently inhibits aggregation Aβ and tau protein in Escherichia coli. BuChE-IN-5 also has free radical scavenging capacity and antioxidant activity. BuChE-IN-5 can be used for researching Alzheimer’s disease .
    BuChE-IN-5
  • HY-N3187
    Nimbin

    		Flavivirus Dengue virus Fungal Bacterial Histamine Receptor Infection Neurological Disease Inflammation/Immunology Cancer
    Nimbin is a intermediate limonoid isolated from Azadirachta. Nimbin prevents tau aggregation and increases cell viability. Nimbin is effective inhibits the envelope protein of dengue virus. Nimbin has anti-inflammatory, antipyretic, antifungal, antihistamine, antiseptic, antioxidant, anti-cancer and anti-viral properties. Nimbin can across blood-brain barrier .
    Nimbin
  • HY-155366
    hAChE-IN-6

    		Cholinesterase (ChE) GSK-3 Neurological Disease
    hAChE-IN-6 (compound 51) is a brain penetrant AChE inhibitor with an IC50 of 0.16 μM. hAChE-IN-6 also inhibits hBuChE and GSK3β with IC50 values of 0.69 μM and 0.26 μM, respectively. hAChE-IN-6 inhibits tau protein and Aβ1-42 self-aggregation, and can be used for Alzheimer's disease (AD) research .
    hAChE-IN-6
  • HY-149273
    hBChE-IN-1

    		Cholinesterase (ChE) Amyloid-β Tau Protein Neurological Disease
    hBChE-IN-1 (compound 4), a quinolizidinyl derivative, is a potent hBChE inhibitor (IC50=7 nM) and highly selective over hAChE. hBChE-IN-1 shows inhibitory activity against tau and Aβ40 protein aggregation, with IC50 values of 20 and 4.3 μM, respectively. hBChE-IN-1 can be used for Alzheimer's disease research .
    hBChE-IN-1
  • HY-154852
    GSK-3 inhibitor 4

    		GSK-3 CDK Neurological Disease
    GSK-3 inhibitor 4 is an orally active and brain-penetrant inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM, and 0.68 μM, respectively. GSK-3 inhibitor 4 effectively reduces the phosphorylation level of Tau protein. GSK-3 inhibitor 4 can be used in Alzheimer's disease (AD) studies .
    GSK-3 <em>inhibitor</em> 4
  • HY-116753
    (-)Clausenamide

    		Amyloid-β Tau Protein Neurological Disease
    (-)Clausenamide is an active alkaloid isolated from the leaves of Clausena lansium (Lour.) Skeels, and improves cognitive function in both normal physiological and pathological conditions. (-)Clausenamide inhibits β-amyloid (Aβ) toxicity, blocking neurofibrillary tangle formation by inhibiting the phosphorylation of tau protein. (-)Clausenamide exerts a significant neuroprotective activity against Aβ25-35. (-)Clausenamide can be used for researching Alzheimer's disease (AD) .
    (-)Clausenamide
  • HY-151337
    Aha1/Hsp90-IN-1

    		Microtubule/Tubulin Neurological Disease Inflammation/Immunology
    Aha1/Hsp90-IN-1 (Compound 17) is an Aha1/Hsp90 complex inhibitor. Aha1/Hsp90-IN-1 disrupts Aha1/Hsp90 interactions with an IC50 of 3.32 μM. Aha1/Hsp90-IN-1 inhibits tau aggregation .
    Aha1/Hsp90-IN-1
  • HY-151873
    SZM679

    		RIP kinase Inflammation/Immunology
    SZM679 is a potent, orally active and selective RIPK1 inhibitor with Kd values of 8.6 nM and >5000 nM for RIPK1 and RIPK3, respectively. SZM679 reverses the tumor necrosis factor-induced systemic inflammatory response. SZM679 decreases the Tau hyperphosphorylation, neuroinflammation, and the RIPK1 phosphorylation level in the hippocampus and cortex. SZM679 can be used in research of Alzheimer's disease (AD) .
    SZM679
  • HY-154851
    GSK-3 inhibitor 3

    		GSK-3 CDK Tau Protein Neurological Disease
    GSK-3 inhibitor 3 is a selective, orally active and brain-penetrant inhibitor of GSK-3, with IC50s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively. GSK-3 inhibitor 3 lowers levels of tau protein phosphorylation at S396 in a triple-transgenic mouse Alzheimer’s disease model, with IC50 of 10 nM. GSK-3 inhibitor 3 can be used for neurological disease research .
    GSK-3 <em>inhibitor</em> 3
  • HY-138678
    (R,S,S)-VH032

    		Ligands for E3 Ligase Cancer
    (R,S,S)-VH032 is Ligand for E3 Ligase used in the synthesis of PROTACs. VH032 is a VHL ligand and VHL/HIF-1α interaction inhibitor that recruits von Hippel-Lindau (VHL) proteins. (R,S,S)-VH032 synthesizes the tau-targeting small molecule PROTAC C004019 (HY-138669) .
    (R,S,S)-VH032
  • HY-149054
    GSK-3β inhibitor 13

    		GSK-3 Tau Protein AAK1 Pim PKC Neurological Disease
    GSK-3β inhibitor 13 (compound 47) is an orally active and potent GSK-3β inhibitor with blood-brain permeability. GSK-3β inhibitor 13 inhibits GSK-3β and GSK-3α with IC50s of 0.73 nM and 0.35 nM, respectively. GSK-3β inhibitor 13 significantly decreases the phosphorylation of tau (IC50=58 nM), which leads the formation of the neurofibrillary tangles associated with Alzheimer's disease .
    GSK-3β <em>inhibitor</em> 13
  • HY-145313
    TTBK1-IN-2

    		Others Neurological Disease
    TTBK1-IN-2 (compound 29) is a potent Tau-Tubulin kinase (TTBK1) inhibitor with IC50s of 0.24 and 4.22 µM, respectively. TTBK1-IN-2 reveals good brain penetration in vivo and is able to reduce TDP-43 phosphorylation not only in cell cultures but also in the spinal cord of transgenic TDP-43 mice .
    TTBK1-IN-2
  • HY-16361A
    Omigapil maleate

    CGP3466B; CGP3446 maleate; TCH346 maleate
    Omigapil maleate, an orally bioavailable GAPDH nitrosylation inhibitor, abrogates Aβ1-42-induced tau acetylation, memory impairment, and locomotor dysfunction in mice. Omigapil maleate has the potential for the research of Alzheimer's disease . Omigapil maleate (CGP3446B maleate) is a apoptosis inhibitor. Omigapil maleate can be used for the research of congenital muscular dystrophy (CMD) . Omigapil (maleate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Omigapil maleate
  • HY-146221
    Dyrk1A-IN-5

    		DYRK Neurological Disease
    Dyrk1A-IN-5 (compound 5j) is a potent and selective DYRK1A inhibitor, with an IC50 of 6 nM. Dyrk1A-IN-5 dose-dependently reduces the phosphorylation of Thr434 in SF3B1, with an IC50 of 0.5 μM. Dyrk1A-IN-5 inhibits phosphorylation of tau at Thr212, with an IC50 of 2.1 μM. Dyrk1A-IN-5 can be used for Down syndrome research .
    Dyrk1A-IN-5
  • HY-136813
    Multitarget AD inhibitor-1

    		Beta-secretase Amyloid-β Cholinesterase (ChE) Neurological Disease
    Multitarget AD inhibitor-1 is a selective and reversible butyrylcholinesterase (BuChE) inhibitor with IC50s of 7.22 μM and 1.55 μM for hBuChE and eqBuChE (BuChE from equine serum), respectively. Multitarget AD inhibitor-1 inhibits β-secretase (IC50hBACE-1=41.60 μM), amyloid β aggregation (IC50Aβ=3.09 μM), tau aggregation. Multitarget AD inhibitor-1, a diphenylpropylamine derivative, has the potential for multifunctional disease-modifying anti-Alzheimer’s research .
    Multitarget AD <em>inhibitor</em>-1
  • HY-134968
    TTBK1-IN-1
    1 Publications Verification

    		 Tau Protein Neurological Disease
    TTBK1-IN-1 is a potent, selective and brain-penetrant tau tubulin kinase 1 (TTBK1) inhibitor with an IC50 of 2.7 nM. TTBK1-IN-1 can be used for the research of alzheimer’s disease and related tauopathies . TTBK1-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    TTBK1-IN-1

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