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Bepranemab is a humanized IgG4 monoclonal antibody that binds to the central region of tauprotein. Bepranemab inhibits the seeding, aggregation of pathological tauprotein and the spread of tau pathology to distal brain regions. Bepranemab is applicable to research related to Alzheimer's disease .
QC-01-175 is a heterobifunctional molecule, which degrades aberrant tau. QC-01-175 reduces the levels of A152T and P301L mutant tauprotein and protects neurons from tau-mediated toxicity and improve cell survival (Pink: ligand for target protein Aberrant tau ligand 1 (HY-W453397); Black: linker NH2-PEG3 (HY-W007545); Blue: ligand for E3 ligase Pomalidomide (HY-10984)) .
Leucomethylene blue (TRx0237) mesylate, an orally active second-generation tauprotein 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 .
PHF6 (VQIVYK) is a self-assembly sequence capable of initiating the full-length tauprotein aggregation and is mapped to the third microtubule-binding repeat region of the tauprotein .
Azure C acts as a tau oligomer modulator and Aβ42 oligomerization inhibitor. It regulates hsp70 ATPase activity, thereby mediating the clearance of tauprotein. Azure C reduces the levels of toxic tau oligomers by promoting the formation of non-toxic tau aggregates, rescues neuroblastoma cells from tau oligomer-induced toxicity, and binds to and inhibits Aβ42 oligomerization without suppressing its fibrillization. Azure C is generated via sequential oxidation of methylene blue or Azure B through a horseradish peroxidase-mediated reaction, and accumulates in HRP reaction media. Azure C can be used in studies related to tauopathies, including Alzheimer's disease .
Simufilam (PTI-125) is an orally active FLNA modulator. Simufilam restores NMDAR signaling and Arc expression. Simufilam inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ42-induced neuroinflammation and tauprotein hyperphosphorylation.
Simufilam can be used for research of Alzheimer's disease .
Etalanetug (E2814) is a humanized high-affinity IgG1 antibody that targets tauprotein and can cross the blood-brain barrier. Etalanetug inhibits the spread of pathological tauprotein through high-affinity binding to the microtubule-binding region (MTBR). Etalanetug can be used in research related to Alzheimer's disease .
PhosTAC7 is a heterobifunctional molecule named as a Phosphorylation Targeting Chimera (PhosTAC). PhosTAC7 can dephosphorylate the PDCD4protein, FOXO3aprotein, and tauprotein by recruiting serine/threonine protein phosphatase 2A (PP2A). PhosTAC7 offers the advantage of selectively modulating the phosphorylation state of individual target proteins, making it a promising tool for research in cancer and tauprotein-related neurodegenerative diseases (Alzheimer's disease) .
C004019 is a BBB-penetrable and small-molecule PROTAC that targets tau. C004019 can simultaneously recruit tau and E3 ligase, and effectively clear tauproteins by promoting the ubiquitination and proteasome-dependent degradation of tau, thereby improving synaptic and cognitive functions in Alzheimer's disease (AD) mice. C004019 can be used in the research of AD and tauprotein-related diseases. (Pink: Ligand for target protein (HY-138679); Black: linker (HY-140189); Blue: E3 Ligase Ligand (HY-138678))
Semorinemab (RG 6100) is an anti-Tau humanized IgG4 monoclonal antibody, targets the N-terminal portion of the Tauprotein (amino acid residues 6-23). Semorinemab binds with human Tau with a Kd value of 3.8 nM. Semorinemab can be used for the research of Alzheimer's Disease .
T808 is a selective tauprotein-targeting ligand. T808 can be used to synthesize [ 18F]-T808, a highly selective tauprotein positron emission tomography (PET) tracer. T808 can also be used to synthesize [ 3H]-T808, a marker for in vitro experiments. T808 can be used for the research of alzheimer’s disease .
Tauprotein (592-597), human TFA is a peptide fragment of human Tauprotein. The dysfunction of Tauprotein is involved in neurodegeneration and dementia .
Posdinemab (JNJ-63733657) is a humanized IgG1/κ monoclonal antibody that selectively targets phosphorylated tau (pT217). Posdinemab specifically binds to the pT217+tau epitope rich in the proline domain, blocks tauprotein aggregation and seed propagation, and promotes the clearance of extracellular tau species. Posdinemab reduces the levels of free and total p217+tau in cerebrospinal fluid, thereby inhibiting the pathological propagation of tauprotein and the formation of neurofibrillary tangles. Posdinemab can be used for the study of progressive supranuclear palsy syndrome and Alzheimer's disease (AD), especially for prodromal or mild AD disease .
Diranersen (IONIS-MAPTRx) sodium is an antisense oligonucleotide that targets the human MAPT gene to inhibit the production of tauprotein. Diranersen sodium can be used in research related to Alzheimer's disease and tauopathies .
Florzolotau (APN1607) is a positron emission tomography (PET) ligand that can be used for the detection of Alzheimer's disease (AD) and other tau proteinopathies. Its binding sites are located in the β-sheet of paired helical filaments (PHFs) and straight filaments (SFs) of tauprotein, as well as in the C-shaped cavity of SFs. In addition, APN-1607 binds to intraneuronal inclusions in Alzheimer's disease (AD), primary age-related tauopathy (PART) and posterior cortical atrophy (PCA). Florzolotau shows promise for PET imaging studies of neurological disorders, particularly tau proteinopathies .
Aberrant tau ligand 1 is a tauprotein ligand. Aberrant tau ligand 1 engages tau and CRBN to trigger proteasomal degradation. Aberrant tau ligand 1 can be used for synthesis PROTACs, such as QC-01–175 (HY-134850) .
Gosuranemab (BMS-986168; IPN007; BIIB092) is a humanised IgG4 anti-tau monoclonal antibody. Gosuranemab neutralizes the extracellular tauprotein, inhibiting the spread and aggregation of pathological tauprotein. Gosuranemab can be used for the research of progressive supranuclear palsy and early Alzheimer’s disease .
Tilavonemab (ABBV-8E12) is a humanized anti-tau monoclonal antibody that binds to amino acids 25-30 near the N-terminus of the tauprotein. Tilavonemab can block the ability of human and mouse neurons to uptake tau aggregates. Tilavonemab can be used for research on Alzheimer’s disease and other tauopathies .
Diranersen (IONIS-MAPTRx) is an antisense oligonucleotide that targets the human MAPT gene to inhibit the production of tauprotein. Diranersen can be used in research related to Alzheimer's disease and tauopathies .
BSB is a Congo red-derived fluorescent probe. BSB binds not only to extracellular amyloid β protein, but also many intracellular lesions composed of abnormal tau and synuclein proteins. BSB acts as a prototype imaging agent for Alzheimer's disease .
REM127 is a small molecule compound capable of modulating calcium homeostasis in cells and possesses neuroprotective effects. REM127 can restore the calcium homeostasis imbalance in cellular models caused by pathological accumulation of tauprotein. REM127 can efficiently cross the blood-brain barrier, and it has the potential to rescue synaptic and cognitive deficits in Alzheimer's disease animal models, as well as to slow down the progression of amyloid-beta and tauprotein pathologies. REM127 can be used for research in neurodegenerative diseases .
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 .
NQTrp, an aromatic naphthoquinone-tryptophan hybrid molecule, an inhibitor of the aggregation of the tauprotein 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 .
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 .
Zagotenemab (LY3303560) is a humanized anti-tau antibody that selectively binds and neutralises tau deposits in the brain. Zagotenemab can be used in Alzheimer's disease research .
Simufilam hydrochloride (PTI-125 hydrochloride) is an orally active FLNA modulator. Simufilam hydrochloride restores NMDAR signaling and Arc expression. Simufilam hydrochloride inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ42-induced neuroinflammation and tauprotein hyperphosphorylation. Simufilam hydrochloride can be used for research of Alzheimer's disease .
Tau Peptide (255-314) (Repeat 2 Domain) (human) (Tau-F protein (255-314)) is a polypeptide. Tau Peptide (255-314) (human) is the 255-314 fragment of Tau-F (also known as Tau-4, the 2N4 isoform), a major isoform of the Tauprotein. Tau Peptide (255-314) (human) contains two core driving sequences for Tau aggregation, namely PHF6* (275-280, VQIINK) and PHF6 (306-311, VQIVYK), and spans the C-terminal half of repeat domain R1, the entire repeat domain R2, and the N-terminal half of repeat domain R3 within the microtubule-binding region (MTBR).
PHF6 (VQIVYK) TFA is a self-assembly sequence capable of initiating the full-length tauprotein aggregation. PHF6 TFA is mapped to the third microtubule-binding repeat region of the tauprotein .
Nimbin is an orally active intermediate limonoid found in 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 is promising for research of neurodegenerative diseases and viral infections .
Tauprotein aggregation-IN-1 (Compound 0c) is a Tauprotein aggregation inhibitor. Tauprotein 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 .
DN5355 is a small molecule compound that targets amyloid β protein (Aβ) and hyperphosphorylated tauprotein. DN5355 can inhibit the aggregation of Aβ and tauprotein and disaggregate the formed Aβ and tauprotein fibers. DN5355 can be used in the study of Alzheimer's disease .
TAU-IN-5 (compound 13) is a TAUprotein inhibitor with an EC50 of 0.81 μM. TAU-IN-5 inhibits the formation of tau (2N4R isoform) oligomers and reduces the formation of tau dimers. TAU-IN-5 can be used in the study of Alzheimer's disease (AD) and Parkinson's disease (PD) .
Tau ligand-1 (Compound 75) is a ligand for aggregated tauprotein that can penetrate the blood-brain barrier . In tissues from patients with Alzheimer's disease, progressive supranuclear palsy, corticobasal degeneration, and Pick's disease, Tau ligand-1 exhibits high affinity for aggregated tauprotein, with equilibrium dissociation constant (KD) values ranging from 1 to 3.8 nM . Tau ligand-1 can serve as a potential positron emission tomography (PET) tracer and holds promise for application in positron emission tomography imaging studies of tau-related diseases in the central nervous system .
TAU-IN-3 (Compound 2) is an orally active TAU inhibitor. TAU-IN-3 inhibits the expression of MAPT exon 10 DDPAC mutant gene in HeLa cells (IC50: 0.6 µM). TAU-IN-3 reduces the 4R/3R MAPT mRNA ratio in HeLa cells transfected with WT or DDPAC minigenes. TAU-IN-3 inhibits the insertion of endogenous MAPT exon 10 and the production of 4R tauprotein in cells. TAU-IN-3 modulates tau splicing in htau mice and improves the associated behavioral phenotypes. TAU-IN-3 can be used to study neurodegenerative diseases .
N-Boc-trans-4-fluoro-L-proline is a non-natural amino acid substitute used to construct monoclonal antibodies that specifically target the seed conformation of tauprotein .
BF-170 is a selective tau fibril binding agent with an EC50 of 221 nM. It exhibits good blood-brain barrier permeability, and after intravenous injection in mice, the concentration in brain tissue reaches 9.1% ID/g within 2 minutes (with a brain clearance rate of 0.25% ID/g after 30 minutes). BF-170 can be used as a probe for tauprotein pathology imaging in Alzheimer's disease (AD). It plays an important role in early-stage AD research and holds potential for imaging studies of tau-related neurodegenerative diseases .
AO-365/43472821 is a selective, brain-penetrant Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitor (IC50 = 0.29 μM) and shows a significant inhibitory effect on (CDC-like kinase 1) CLK1 (IC50 = 0.08 μM). AO-365/43472821 could protect the human neuroblastoma cell line SH-SY5Y from Okadaic acid (HY-N6785) (OA)-induced injury. AO-365/43472821 decreased tau(pSer396)/tau and Aβ1-42protein expression. AO-365/43472821 can be used for the study of Alzheimer's disease .
Simufilam dihydrochloride (PTI-125 dihydrochloride) is an orally active FLNA modulator. Simufilam dihydrochloride restores NMDAR signaling and Arc expression. Simufilam dihydrochloride inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ42-induced neuroinflammation and tauprotein hyperphosphorylation. Simufilam dihydrochloride can be used for research of Alzheimer's disease .
Tau Peptide (275-305) (Repeat 2 domain) is the Alzheimer's Tau fragment R2, corresponding to the second repeat unit of the microtubule-binding domain, which is believed to be pivotal to the biochemical properties of full tauprotein. Tau Peptide (275-305) specifically coordinates with group IIB metal ions (Zn²⁺, Cd²⁺, Hg²⁺), which can induce their conformational changes and significantly promote their pathological accumulation. Tau Peptide (275-305) can be used to study the role of heavy metals in neurodegenerative diseases .
ACI-3024 is an an orally active and highly selective Tauprotein aggregation inhibitor. ACI-3024 decrease the β-sheet content and seeding properties of pathological Tau from different Tauopathies, leading to a significant rescue of the Tau-induced neurodegeneration and neuroinflammation in a cellular model. ACI-3024 is promising for research of neurodegenerative diseases .
MRL828 combines a Tau pathology-binding ligand and modified guanine moiety based on the ATTEC technology to selectively designate aggregated tauproteins for clearance via the ALP. MRL828 decreases intracellular Tau aggregates and promotes the secretion of Tau .
AMG28 is an ATP-competitive inhibitor targeting TTBK1 and TTBK2, with IC50 values of 805 nM and 988 nM, respectively. AMG28 inhibits the phosphorylation of tauprotein at the Ser422 site .
MAO-B-IN-45 is a dual inhibitor of ferroptosis and MAO-B. MAO-B-IN-45 shows selectivity towards MAO-B with an IC50 of 87.47 nM and selectivity exceeding 229-fold for MAO-B over MAO-A. MAO-B-IN-45 has excellent antiferroptosis activity through modulation of the iron metabolic pathway and GSH-GPX4 axis in vitro. MAO-B-IN-45 improves cognitive and behavioral impairments in 3×Tg (APP/Tau/Ps1) AD mouse and significantly reduced the levels of ferritin heavy chain 1 (FTH1), APP, and Tau phosphorylation (p-Tau) proteins in the brain.
Salpyran dihydrochloride is a Cu(II) selective chelator with therapeutic potential. Salpyran dihydrochloride prevents the formation of reactive oxygen species from the binary Cu(II)/H2O2 system .
Hydromethylthionine dihydrobromide (Leukomethylene blue dihydrobromide) is a potent inhibitor of TAUprotein aggregation. Hydromethylthionine dihydrobromide reduces neurodegeneration by interacting with TAUproteins and preventing them from forming neurotoxic aggregates. Hydromethylthionine dihydrobromide can be used in the study of Alzheimer's disease and other TAU related disorders .
Aberrant tau ligand 2 (Compound 4-12) is the ligand for tauprotein and can be used as target protein ligand for synthesis of PROTAC degrader C004019 (HY-138669) .
Tau-aggregation-IN-1 (Compound D-519) is a tau441protein aggregation inhibitor with an IC50 of 21 µM. Tau-aggregation-IN-1 is also a dopamine D2 and D3 receptor agonist .
THK-5117, an arylquinoline derivative, displays high binding affinity to tau fibrils with a Ki of 10.5 nM. THK-5117 has high binding affinity to tauprotein aggregates and tau-rich Alzheimer disease (AD) brain homogenates. 18F-THK-5117 has the potential to act as a tau imaging PET probe .
Tau Peptide (337-368) (Repeat 4 Domain) is a 32-amino acid peptide derived from the fourth microtubule-binding repeat sequence (R4) of the tauprotein. Tau Peptide (337-368) (Repeat 4 Domain) can be used in research on neurodegenerative diseases .
TTBK2 is a tau tubulin kinase. Mutations in TTBK2 cause spinocerebellar ataxia type 11, a disorder exhibiting both loss of Purkinje cells and widespread deposition of tau. TTBK2 Recombinant Human Active Protein Kinase is a recombinant TTBK2 protein that can be used to study TTBK2-related functions .
TauProtein Phosphorylation-IN-1 is a tauprotein phosphorylation inhibitor that potently protects PC12 cells against Aβ25–35-induced cytotoxicity (EC50 = 1.93 μM), and can penetrate the blood-brain barrier (BBB).TauProtein Phosphorylation-IN-1 reverses the hyperphosphorylation of tau, significantly inhibits the expression of certain immune-related cytotoxic factors, suppresses the MAPK and NF-κB signaling pathways, and significantly inhibits the expression of RAGE and the apoptosis factors Bax/Bcl-2, both in vitro and in vivo. TauProtein Phosphorylation-IN-1 relieves nerve damage, and improves learning and memory in an Alzheimer’s disease (AD) mouse model. TauProtein Phosphorylation-IN-1 can be used for AD research .
MPT0G413 (Compound 6) is a potent, selective, orally active and brain-penetrant HDAC6 inhibitor with an IC50 of 3.92 nM. MPT0G413 decreases not only the level of phosphorylation of tauproteins but also the aggregation of tauproteins. MPT0G413 can ameliorate the impaired learning and memory. MPT0G413 can be used for the research of neurological disease, such as Alzheimer's disease .
GSK-3β inhibitor 24 (Compound 41) is a potent GSK-3β inhibitor with an IC50 of 0.22 nM. GSK-3β inhibitor 24 increases GSK-3β phosphorylation at Ser9 site dose-dependently. GSK-3β inhibitor 24 inhibits the hyperphosphorylation of tauprotein by decreasing the p-tau-Ser396 abundance. GSK-3β inhibitor 24 up-regulates β-catenin and neurogenesis-related markers (GAP43 and MAP-2). GSK-3β inhibitor 24 demonstrates remarkable anti-Alzheimer's disease (AD) effects .
TauProtein/α-synuclein-IN-2 (Compound 14T) is a blood-brain barrier penetrating tau and α-syn inhibitor. Through its thiourea linker structure, TauProtein/α-synuclein-IN-2 dose-dependently reduces α-syn oligomerization. In biosensor cells, TauProtein/α-synuclein-IN-2 prevents the seeding effect of tau aggregation. In the M17D neuroblastoma model, TauProtein/α-synuclein-IN-2 exhibits anti-inclusion effects. Additionally, TauProtein/α-synuclein-IN-2 reduces Aβ plaque formation. TauProtein/α-synuclein-IN-2 holds promise for Alzheimer's disease and Parkinson's disease research.
tauprotein/α-synuclein-IN-1 is a dual inhibitor of tauprotein and α-synuclein. tauprotein/α-synuclein-IN-1 reduces α-syn inclusions development in M17D neuroblastoma cells. tauprotein/α-synuclein-IN-1 can be used in study Alzheimer’s disease .
Microtubule-associated proteintau (26-44) is a synthetic peptide chain with an amine group attached to glutamine and an carboxyl group attached to lysine.
Ac-Val-Gln-aIle-Val-aTyr-Lys-NH2 is a N-amino peptide that selectivity inhibits the fibrilization of tauprotein. Ac-Val-Gln-aIle-Val-aTyr-Lys-NH2 is effective at blocking the cellular seeding of endogenous tau by interacting with monomeric or fibrillar forms of extracellular tau. Ac-Val-Gln-aIle-Val-aTyr-Lys-NH2 can be used for the study of neurodegenerative diseases, such as Alzheimer’s disease .
Anti-Mouse/Human PrP/prion protein Antibody (TW1) is a mouse-derived IgG2a type antibody inhibitor, targeting to mouse/human PrP/prion protein. Anti-Mouse/Human PrP/prion protein Antibody (TW1) binds to both PrPc (cellular prion protein) and PrPSc (Scrapie Prion Protein) and blocks the interaction of prion protein with tauprotein. Anti-Mouse/Human PrP/prion protein Antibody (TW1) can be used for the researches of Alzheimer’s disease (AD) .
GSK-3β inhibitor 27 (Compound 1c) is a reversible and competitive GSK-3β inhibitor with an IC50 value of 2.2 μM. GSK-3β inhibitor 27 inhibits tau hyperphosphorylation, reduces Aβ protein aggregation and possesses metal chelation and neuroprotective potential. GSK-3β inhibitor 27 is promising for research of neurodegenerative diseases (such as Alzheimer’s 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 tauprotein and Aβ1-42 self-aggregation, and can be used for Alzheimer's disease (AD) research .
hAChE-IN-5 (compound 49) is a potent hAChE and hBuChE inhibitor with IC50 values of 0.17 μM and 0.17 μM, respectively. hAChE-IN-5 shows potent GSK3β inhibition with an IC50 value of 0.21 μM. hAChE-IN-5 is used as tauprotein aggregation and Aβ1-42 self-aggregation inhibitor. hAChE-IN-5 can bind virtually with the PAS affecting Aβ aggregation, thus preventing Aβ-dependent neurotoxicity. hAChE-IN-5 can penetrate BBB and has the potential for multi-targeted anti-Alzheimer's agents research .
2N4R Tau/α-Syn against-1 (Compound 4d) targets α-synuclein and tauprotein, inhibits the fibrillation and oligomer formation of α-synuclein and tauproteins, exhibits disaggregation activity on Aβ fibers. 2N4R Tau/α-Syn against-1 can be used in research of Parkinson's disease and Alzheimer's disease .
Tau-aggregation-IN-3 (compound 9) a Tauprotein aggregation inhibitor (TAI). Tau-aggregation-IN-3 shows activity in cell-based aggregation inhibition experiments (EC50=4.816 μM). Tau-aggregation-IN-3 can be used in Alzheimer's disease research .
THK-5105, an arylquinoline derivative, displays high binding affinity to tau fibrils. THK-5105 has high binding affinity to tauprotein aggregates and tau-rich Alzheimer disease (AD) brain homogenates. 18F-THK-5105 has the potential to act as a tau imaging PET probe .
D-688 is an inhibitor of Tau and Aβ. D-688 can reverse Aβ1–42-induced toxicity in SH-SH5Y cells and has significant neuroprotective properties. D-688 can improve the survival rate of Drosophila melanogaster expressing the human tauprotein isoform (2N4R) .
CDK18 is a neuronal kinase that phosphorylates TAUprotein when overexpressed in human brain. CDK18 shares a conserved PCTAIRE amino acid sequence in the helical α-C region of the kinase N-lobe. CDK18/CycY Recombinant Human Active Protein Kinase is an ortholog of CDK18 .
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-Tauproteins 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 .
Tau Peptide (274-288) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
BChE-IN-39 (Compound 7c) is a selective inhibitor for butyrylcholinesterase (BChE) with an IC50 of 0.08 μM (IC50=3.98 μM for AChE). BChE-IN-39 downregulates the GSK-3β expression, inhibits the hyperphosphorylation of tauprotein .
Dyrk1A-IN-9 (Compound L9) is a moderately active DYRK1A inhibitor (IC50: 1.67 μM). L9 shows neuroprotective activity by regulating the expression of Aβ and phosphorylation of Tauprotein. Dyrk1A-IN-9 can be used for research of Alzheimer's disease .
RA-PR058 is an orally active Ramalin derivative with blood-brain barrier permeability, exhibiting multi-target regulatory effects and favorable pharmacokinetic properties. RA-PR058 demonstrates potential as a multi-target modulator for Alzheimer's disease by reducing the expression of BACE1, tauprotein hyperphosphorylation, and anxiety-like behaviors .
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 Aβ40protein aggregation, with IC50 values of 20 and 4.3 μM, respectively. hBChE-IN-1 can be used for Alzheimer's disease research .
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 tauprotein 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 .
Etalanetug (Mouse IgG2a) (7G6 Antibody) is a mouse monoclonal antibody targeting the HVPGG motif in the microtubule-binding domain of tauprotein. Etalanetug (Mouse IgG2a) reduces the levels of insoluble tauprotein in multiple brain regions and inhibits the seeding and spread of pathological tauprotein. Etalanetug (Mouse IgG2a) is applicable to research related to Alzheimer's disease .
JNJ-64326067 is an aggregated tau-binding agent with blood-brain barrier permeability, with a Ki of 2.4 nM. JNJ-64326067 selectively binds to aggregated tauprotein but does not bind to aggregated β-amyloid protein, and shows no significant off-target binding to the tested receptors, ion channels, transporters, kinases or monoamine oxidases. JNJ-64326067 is applicable to the research of Alzheimer's disease .
8-F-2-(Me-Pip-Me)-Tryptanthrin is a tryptanthrin derivative with blood-brain barrier penetration. 8-F-2-(Me-Pip-Me)-Tryptanthrin protects neurons from Aβ-induced apoptosis, inhibits Aβ-induced Tauprotein hyperphosphorylation and neuronal synaptic damage, and improves learning and memory abilities in Alzheimer's disease mice. 8-F-2-(Me-Pip-Me)-Tryptanthrin can be used for the research of nervous system diseases, including diseases related to abnormal Tauprotein phosphorylation and abnormal PSD-95 function .
Phenchlobenpyrrone is a highly selective neuronal calcium antagonist that crosses the blood-brain barrier. Phenchlobenpyrrone mildly inhibits AChE activity. Phenchlobenpyrrone inhibits Aβ aggregation and promotes the clearance of Aβ oligomers. Phenchlobenpyrrone reduces abnormal phosphorylation of Tauprotein. Phenchlobenpyrrone may be used in research on Alzheimer's disease .
TAU-IN-6 (Compound 13) is a Tauprotein misfolding and aggregation inhibitor. TAU-IN-6 inhibits stress granules composed of tau and TIA1. TAU-IN-6 is applicable for Alzheimer's disease research .
SGK1-IN-7 is a blood-brain barrier-permeable SGK1 inhibitor with an IC50 of 0.72 μM. SGK1-IN-7 reduces the phosphorylation level of TAUprotein at the Ser396 and Ser214 epitopes. SGK1-IN-7 antagonizes the toxicity induced by Okadaic acid (HY-N6785). SGK1-IN-7 can be used in the research of Alzheimer's disease .
CLR01 sodium is a blood-brain barrier-permeable anti-aggregation agent. CLR01 sodium inhibits the de novo aggregation of Amyloid-β 40/42, α-synuclein, IAPP, tauprotein and SOD1. CLR01 sodium reduces amyloid plaque burden in the cortex of triple-transgenic mice and improves the memory and motor abilities of these mice. CLR01 sodium can be used in research related to Alzheimer's disease, Parkinson's disease, and amyotrophic lateral sclerosis (ALS) .
SGK1-IN-8 (compound 55) is a SGK1 and GSK3β inhibitor, with an IC50 of 0.11 μM against human SGK1 and an IC50 of 3.39 μM against human GSK3β. SGK1-IN-8 inhibits the catalytic activities of SGK1 and GSK3β, and reduces the phosphorylation level of TAUprotein at the Ser214 site. SGK1-IN-8 is available for the research of Alzheimer's disease .
Gosuranemab (BMS-986168; IPN007; BIIB092) (powder) is a humanised IgG4 anti-tau monoclonal antibody. Gosuranemab (powder) neutralizes the extracellular tauprotein, inhibiting the spread and aggregation of pathological tauprotein. Gosuranemab (powder) can be used for the research of progressive supranuclear palsy and early Alzheimer’s disease .
Armanezumab is a pathological tauprotein inhibitor that specifically binds to the N-terminal domain exposed by pathological tauprotein (epitope covering amino acids 4-8: PRQEF). Armanezumab is applicable to research related to Alzheimer's disease, frontotemporal dementia, and Pick's disease .
O-GlcNAcase-IN-5 (Compound 1) is a selective O-GlcNAcase inhibitor. O-GlcNAcase-IN-5 can prevent the enzyme from removing the O-GlcNAc modification on tauprotein, thus avoiding excessive phosphorylation of tauprotein. O-GlcNAcase-IN-5 can be used for the research of Alzheimer's disease .
ADEL-Y01 is a humanized and parental murine blood-brain barrier-penetrating monoclonal antibody against tau-acK280. ADEL-Y01 specifically recognizes tau-acK280 and its surrounding residues, mediates the neutralization and phagocytosis of acetylated tau aggregates, and interferes with the activity of pathological tauprotein. ADEL-Y01 prevents the progression of tauopathies, increases neuronal survival rate, reduces tau-related pathological changes, and improves memory impairment. ADEL-Y01 can be used in research related to Alzheimer's disease and tauopathies .
AChE/BuChE/BACE-1-IN-1 is a blood-brain barrier-permeable multi-target inhibitor of AChE/BuChE/BACE, with IC50 values of 0.387 μM, 0.430 μM, and 0.531 μM against AChE, BuChE, and BACE-1, respectively. AChE/BuChE/BACE-1-IN-1 reduces the aggregation of β-amyloid protein (Aβ) and hyperphosphorylated tauprotein(p-tau). AChE/BuChE/BACE-1-IN-1 can be used for the research of Alzheimer's disease .
TPSLP{pT}PPTR- 13C6, 15N4 TFA is the 13C- and 15N-labeled TPSLP{pT}PPTR TFA. TPSLP{pT}PPTR TFA is a tauprotein fragment phosphorylated in the central region.
(E/Z)-Florzolotau ((E/Z)-APN1607) is a mixed configuration or unspecified configuration of Florzolotau (HY-137557). Florzolotau (APN1607) is a positron emission tomography (PET) ligand that can be used for the detection of Alzheimer's disease (AD) and other tau proteinopathies. Its binding sites are located in the β-sheet of paired helical filaments (PHFs) and straight filaments (SFs) of tauprotein, as well as in the C-shaped cavity of SFs. In addition, APN-1607 binds to intraneuronal inclusions in Alzheimer's disease (AD), primary age-related tauopathy (PART) and posterior cortical atrophy (PCA). Florzolotau shows promise for PET imaging studies of neurological disorders, particularly tau proteinopathies .
PAV-174 is a potent antiviral agent that targets a host protein. PAV-174 prevents Herpes simplex virus (HSV-1) infection in cells (IC50 of 0.02 μM in Vero cells) and human brain organoids. PAV-174 inhibits oxidized macrophage migration inhibitory factor (oxMIF)-induced tau phosphorylation in vitro and in vivo independent of infection. PAV-174 reduces HSV-1-induced tau phosphorylation via the Akt/GSK3β signaling pathway. PAV-174 can be used for Alzheimer’s disease research .
Lu AF87908 is an IgG1 monoclonal antibody targeting the p-Ser396/404 epitope of tauprotein, which mainly binds to the pSer396 region. Lu AF87908 can be used in the research of Alzheimer's disease. The recommended isotype control is human IgG1 kappa (HY-P99001) .
SK-129 is a blood-brain barrier-permeable inhibitor of α-synuclein (αS) oligomers with a Kd of 221 nM. SK-129 preferentially binds to neurotoxic αS oligomers over physiological αS monomers, inhibits αS aggregation, blocks the interaction and co-aggregation of αS with tauprotein, and prevents the maturation of αS-tau condensates into amyloid aggregates. SK-129 reduces ROS production, rescues dopaminergic neuron degeneration, improves motor function, restores endogenous dopamine synthesis, increases the number of Tyrosine Hydroxylase-positive neurons, prevents brain histopathological changes, alleviates neuroinflammation, and improves survival rates in relevant models. SK-129 can be used in research related to Parkinson's disease (PD) and Lewy body dementia (LBD) .
GSK3β-IN-3 is an ATP-competitive GSK-3β inhibitor (IC50 = 0.90 μM). GSK3β-IN-3 can reduce the phosphorylation level of tauprotein in the BR5706 strain and reduce the deposition of Aβ aggregates in the CL2006 strain, and can be used to research Alzheimer's disease (AD) .
PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay. PF-04802367 shows desirable central nervous system (CNS) properties and potency. PF-04802367 is equally effective at inhibition of the two known GSK-3 isoforms (GSK-3α and GSK-3β) with IC50 values of 10.0 and 9.0 nM in mobility shift assays, respectively .
(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) .
OX-201 is an orally active, blood-brain barrier-permeable OX2R agonist with an EC50 of 8.0 nM. OX-201 activates OX2R to induce wakefulness and neuronal activation. OX-201 promotes the release of neuron activity-dependent tauprotein from neurons into the interstitial fluid of hippocampal tissues. OX-201 is applicable to research related to Alzheimer's disease and tauopathies .
(-)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 tauprotein. (-)Clausenamide exerts a significant neuroprotective activity against Aβ25-35. (-)Clausenamide can be used for researching Alzheimer's disease (AD) .
Egalognastat (ASN90) is a selective, brain-penetrant and orally active O-GlcNAcase (OGA) enzyme inhibitor with an IC50 value of 10.2 nM. Egalognastat increases O-GlcNAcylation of intracellular proteins like tau and α-synuclein, preventing their aggregation and toxicity. Egalognastat does not inhibit hexosaminidase (Hex). Egalognastat can be used for the research of neurodegenerative diseases, such as tauopathies and α-synucleinopathies (e.g., Alzheimer’s disease and Parkinson’s disease) .
Okadaic acid, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid increases of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter. Okadaic acid induces tau phosphorylation .
Okadaic acid sodium, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid (sodium) has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid sodium increases of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter. Okadaic acid sodium induces tau phosphorylation .
ACI-19278 is a TDP-43 PET tracer with an average Kd of 25 nM. ACI-19278 only binds to pathological TDP-43 aggregates and does not cross-react with Aβ, Tau, etc. [ 18F]ACI-19278 successfully visualized the TDP-43 pathology in the human brain through positron emission computed tomography. ACI-19278 can be used for in vivo diagnosis of TDP-43 protein lesions .
O-GlcNAcase-IN-4 (compound T-110) is a O-GlcNAcase inhibitor. O-GlcNAcase-IN-4 modulates the activity of O-GlcNAcase. O-GlcNAcase-IN-4 is applicable to the research of neurodegenerative diseases and disorders, Alzheimer's disease, and tau-mediated neurodegenerative diseases or disorders .
Okadaic acid ammonium salt, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid ammonium salt has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid ammonium salt increases of phosphorylation of a number of proteins by inhibiting PP, and acts as a tumor promoter. Okadaic acid ammonium salt induces tau phosphorylation .
ARN25699 is a kinase inhibitor with an IC50 of 5.5 nM against GSK-3β, 2.2 nM against FYN-α, and 242.3 nM against DYRK1A, and it exhibits oral bioavailability. ARN25699 reduces hyperphosphorylation of tauprotein and promotes microtubule bundle formation. ARN25699 has a broader kinome inhibitory profile and targets kinases associated with the pathogenic mechanisms linked to Alzheimer's disease. ARN25699 can be used in the research of Alzheimer's disease and related tauopathies .
hAChE/hBuChE/GSK-3β-IN-1 (Compound 6c) is a BBB-penetrable and multi-target anti-Alzheimer's disease compound. hAChE/hBuChE/GSK-3β-IN-1 is the inhibitors of hAChE (IC50: 28.88 nM), hBuChE (IC50: 131.90 nM) and GSK-3β (IC50: 51.42 nM). hAChE/hBuChE/GSK-3β-IN-1 is the tau and Aβprotein aggregation inhibitors .
Hepta-histidine is an inhibitor of Ku70-Huntingtin protein interaction. Hepta-histidine can reverse the morphological abnormalities of primary neurons differentiatied from hiPSCs. Hepta-histidine prolongs the lifespan in severe Huntington’s disease R6/2 mouse model. Hepta-histidine ameliorates DNA damage in vitro. Hepta-histidine can be used to study anti-aggregation agent against Tau-associated neurodegenerative diseases such as Alzheimer’s disease and Huntington’s 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 Tauprotein. GSK-3 inhibitor 4 can be used in Alzheimer's disease (AD) studies .
MAO-B-IN-50 (Compound C20) is a selective MAO-B inhibitor with an IC50 value of 0.06 μM. MAO-B-IN-50 shows good inhibitory effects on the aggregation of Aβ40/42 and Tauproteins, with overall IC50 values around 1 μM. MAO-B-IN-50 exhibits potent and selective AChE inhibition (IC50 = 1.78 μM). MAO-B-IN-50 can be used in the research of Alzheimer's disease .
AChE/BChE-IN-29 is an AChE/BChE inhibitor. AChE/BChE-IN-29 exhibits balanced dual cholinesterase inhibitory activity with IC50 values of 2.1 μM for Electrophorus electricus AChE (eeAChE) and 6.3 μM for equine serum butyrylcholinesterase (eqBChE). AChE/BChE-IN-29 effectively inhibits amyloid-β (Aβ42) aggregation and tauprotein aggregation in E. coli cell models. AChE/BChE-IN-29 can be used for the study of Alzheimer’s disease (AD) .
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 tauprotein 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 .
ONC-841 is a blood-brain barrier-permeable, humanized monoclonal antibody targeting SIGLEC10. As an immune checkpoint inhibitor, ONC-841 restores the functions of immune effector cells such as T cells and enhances anti-tumor immune responses by blocking inhibitory signals mediated by SIGLEC10. ONC-841 restores the phagocytic and migratory activities of microglia, and promotes the phagocytosis of Amyloid-β and Tauprotein aggregates by microglia. ONC-841 is applicable to research related to solid tumors and Alzheimer's disease .
BRI-50460 is an inhibitor of cytosolic calcium-dependent phospholipase A2 (cPLA2) that has the ability to penetrate the blood-brain barrier, with an IC50 of 0.88 nM. BRI-50460 exerts the activities of regulating neuroinflammation and restoring lipid homeostasis by inhibiting cPLA2, regulating the downstream inflammatory lipid signaling pathway, and alleviating the effects of amyloid β42 oligomers on the activation of cPLA2, the hyperphosphorylation of tauprotein, and the reduction of synapses and dendrites. BRI-50460 can be applied to the research in the fields of Alzheimer's disease and other neurodegenerative diseases .
DYRK2-IN-2 (Compound C17) is a selective inhibitor of DYRK2, with its IC50 value being 40.3 nM. The inhibitory activity of DYRK2-IN-2 on DYRK1A (IC50 = 1842 nM), DYRK1B (IC50 = 1335 nM), DYRK4 (IC50 = 1931 nM), DYRK3 (IC50 = 112 nM), and CLKs (IC50 = 540-6496 NM) is relatively low. DYRK2-IN-2 inhibits the phosphorylation of Tauprotein at Thr212 and shows moderate cytotoxicity in HT22 cells. DYRK2-IN-2 can be used in cancer research .
O-GlcNAcase-IN-2 (compound 81) is an orally effective, blood-brain barrier-permeable OGA inhibitor (IC50=4.93 nM). O-GlcNAcase-IN-2 can increase the O-GlcNAcylation level of proteins and phosphorylation of tau (p-Ser199, p-Thr205 and p-Ser396) in the OA-damaged SH-SY5Y cell model. O-GlcNAcase-IN-2 can also improve cognitive impairment in APP/PS1 mice and has potential anti-Alzheimer's disease (AD) effects .
Aha1/Hsp90-IN-2 is a selective inhibitor of the Hsp90/Aha1 interaction, with its IC50 being 1.46 μM. Aha1/Hsp90-IN-2 inhibits the activation of Hsp90 ATPase activity mediated by Aha1 by specifically blocking the binding of Hsp90 to Aha1, thereby reducing tauprotein aggregation. Aha1/Hsp90-IN-2 can be used for the study of neurodegenerative diseases, such as Alzheimer's disease .
Punicic acid is a bioactive compound of pomegranate seed oil. Punicic acid is an isomer of conjugated α-linolenic acid and ω-5 polyunsaturated fatty acids. Punicic acid has anti-inflammatory and antioxidant activities and can inhibit the expression of inflammatory mediators such as tumor necrosis factor α (TNF-α). Punicic acid can also reduce the formation of β-amyloid deposits and hyperphosphorylation of tau by increasing the expression of GLUT4 protein and inhibiting the overactivation of calpain, and is used to prevent and treat neurodegenerative diseases. In addition, punicic acid also has breast cancer inhibitor properties that depend on lipid peroxidation and PKC pathways .
Apomorphine ((-)-Apomorphine) is a potent dopamine receptor agonist. Apomorphine also inhibit MAO-A and MAO-B.Apomorphine exerts neuroprotective effect and can relax rat corpus cavernosum. Apomorphine can inhibit ROS production, DNA fragmentation and inibit JNK and ERK1/2 phosphorylation. Apomorphine can enhance degradation of intracellular Aβ40 and Aβ42, reducestauprotein levelsandinhibit MMP-9 expression. Apomorphine is a highly potent radical scavenger and iron chelator. Apomorphine can be used for the researches of dementia, parkinson's disease, alzheimer disease, breast carcinoma, and erectile dysfunction .
CS640 (Compound 19) is a chemical probe and a calmodulin-dependent kinase inhibitor. CS640 inhibits CaMK1D, CaMK1B, CaMK1A, CaMK1G, MEK5, RIPK4, mLK3 and PIP5K1, with IC50 values of 8, 3, 1, 1, 25 nM, 5.69, 2.75 and 11.2 μM, respectively. CS640 blocks Aβ-induced hyperphosphorylation of tauprotein at the Thr181 site, but fails to protect primary mouse cortical neurons from Aβ-induced toxic damage. CS640 is applicable to research related to Alzheimer's disease .
Schisantherin B (Gomisin-B) is a lignan compound and one of the active components of Schisandra chinensis. Schisantherin B activates the PI3K/AKT signaling pathway, restores the activity of GSK3β, and reduces the hyperphosphorylation of tauprotein in hippocampal and cerebral cortical tissues. Schisantherin B upregulates the level of GLT-1, decreases the expression of pro-inflammatory cytokines TNF-α/IL-1β/IL-6, upregulates the expression of IL-10, and inhibits cell apoptosis. Schisantherin B is applicable to the research of spinal cord injury, Alzheimer's disease and depression .
AChE/MAO-B-IN-9 (Compound E12) is an orally active, selective, reversible, non-competitive AChE and MAO-B inhibitor, with an IC50 of 0.156 μM against electric eel AChE. AChE/MAO-B-IN-9 inhibits Aβ40/42 fibril formation, promotes Aβ fibril depolymerization, and inhibits Tauprotein fibril formation. AChE/MAO-B-IN-9 exerts antioxidant and neuroprotective effects, and improves scopolamine (HY-N0296)-induced memory impairment in mice. AChE/MAO-B-IN-9 can be used for the research of Alzheimer's disease .
AChE/BChE-IN-23 (Compound 6e) is an AChE/BChE inhibitor (IC50: 0.91 μM, 1.19 μM and 1.01 μM for hAChE, eq BChE and hBChE, respectively). AChE/BChE-IN-23 has antioxidant activity and inhibits Aβ1-42 and Tauprotein aggregation. AChE/BChE-IN-23 also inhibits microglial activation by reducing ROS release and mitochondrial injury. AChE/BChE-IN-23 suppresses NLRP3 inflammasome and pro-inflammatory cytokines in human microglial cells. AChE/BChE-IN-23 also reverses the Scopolamine (HY-N0296)-induced memory impairment in mice model .
MNP2 is a NLRP3-ASC interaction inhibitor. MNP2 selectively binds to the PYD domain of ASC (Ka=149 nM) and blocks ASC-PYM binding (Ka=58 nM), thereby inhibiting the interaction between ASC and NLRP3 and suppressing the formation of the NLRP3 inflammasome. MNP2 inhibits IL-1β release and caspase-1 maturation, and reduces the efflux of potassium and chloride ions. MNP2 prevents mitochondrial damage and reactive oxygen species production, and significantly decreases NLRP3 inflammasome formation in neurodegenerative pathologies induced by β-amyloid, Tauprotein and α-synuclein. MNP2 is applicable for the research of neurodegenerative diseases .
Mouse Serum Albumin is most abundant protein in plasma, which leaks into the brain parenchyma when the blood-brain barrier (BBB) is impaired. Mouse Serum Albumin induces astrocytes to A1 phenotype to remarkably increase levels of Elovl1. Mouse Serum Albumin promotes VLSFAs secretion and causes neuronal lippoapoptosis through endoplasmic reticulum stress response pathway. MSA-activated microglia triggeres remarkable tau phosphorylation at multiple sites (Ser202/Thr205) through NLRP3 inflammasome pathway. Mouse Serum Albumin decreases the spatial learning and memory abilities in mice. Mouse Serum Albumin can be used for the study of neurodegenerative diseases like Alzheimer’s disease (AD) and frontotemporal dementia (FTD) .
Myricanol is a diarylheptanoid and a Nampt activator. Myricanol exerts anti-inflammatory effects and alleviates glucocorticoid-induced muscle atrophy by increasing Sirtuin 1 (SIRT1) and PRDX5 activities while regulating inflammatory factors. Myricanol exhibits growth inhibition and induces apoptosis in human lung adenocarcinoma A549 cells. Myricanol promotes autophagy-mediated clearance of microtubule-associated proteintau to exert neuroprotective effects. Myricanol protects cardiovascular function by inhibiting PDGFRβ and NF-κB signaling pathways. Myricanol activates mitochondrial transcription factor A (TFAM) expression to exert anti-renal fibrosis effects. Myricanol improves insulin resistance through AMPK activation .
Apomorphine ((-)-Apomorphine) (Standard) is the analytical standard of Apomorphine (HY-12723). This product is intended for research and analytical applications. Apomorphine is a potent dopamine receptor agonist. Apomorphine also inhibit MAO-A and MAO-B.Apomorphine exerts neuroprotective effect and can relax rat corpus cavernosum. Apomorphine can inhibit ROS production, DNA fragmentation and inibit JNK and ERK1/2 phosphorylation. Apomorphine can enhance degradation of intracellular Aβ40 and Aβ42, reducestauprotein levelsandinhibit MMP-9 expression. Apomorphine is a highly potent radical scavenger and iron chelator. Apomorphine can be used for the researches of dementia, parkinson's disease, alzheimer disease, breast carcinoma, and erectile dysfunction .
GSK-3β inhibitor 15 (Compound 54) is a GSK-3β inhibitor (IC50: 3.4 nM). GSK-3β inhibitor 15 inhibits Aβ1-42-induced GSK-3β and tauprotein phosphorylation. GSK-3β inhibitor 15 inhibits LPS-induced iNOS expression. GSK-3β inhibitor 15 has neuroprotective effects on Aβ1-42-induced neurotoxicity. GSK-3β inhibitor 15 can be used for research of Alzheimer’s disease (AD) .
Schisantherin B (Gomisin-B) (Standard) is the analytical standard of Schisantherin B. This product is intended for research and analytical applications. Schisantherin B is a lignan compound and one of the active components of Schisandra chinensis. Schisantherin B activates the PI3K/AKT signaling pathway, restores the activity of GSK3β, and reduces the hyperphosphorylation of tauprotein in hippocampal and cerebral cortical tissues. Schisantherin B upregulates the level of GLT-1, decreases the expression of pro-inflammatory cytokines TNF-α/IL-1β/IL-6, upregulates the expression of IL-10, and inhibits cell apoptosis. Schisantherin B is applicable to the research of spinal cord injury, Alzheimer's disease and depression.
Drofenine (Cycloadiphene; Hexahydroadiphenine) hydrochloride is an brain-penetrant antispasmodic agent. Drofenine hydrochloride is a Kv2.1 channel inhibitor with human IC50 of 9.53 μM. Drofenine hydrochloride is a butyrylcholinesterase (BChE) inhibitor with Ki of 0.003 mM, and is a TRPV3 activator. Drofenine hydrochloride blocks Kv2.1-dependent potassium efflux, inhibits Kv2.1/JNK/NF-κB and IkBa/NF-kB signaling, suppresses Kv2.1 mRNA/protein expression. Drofenine suppresses oligomeric Aβ-induced microglial NLRP3 inflammasome activation and neuronal Tau hyperphosphorylation, improves cognitive impairment, promotes neurite outgrowth. Drofenine hydrochloride induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine hydrochloride ameliorates diabetic peripheral neuropathy -like pathology. Drofenine hydrochloride can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm .
Drofenine (Cycloadiphene; Hexahydroadiphenine) is an brain-penetrant antispasmodic agent. Drofenine is a Kv2.1 channel inhibitor with human IC50 of 9.53 μM. Drofenine is a butyrylcholinesterase (BChE) inhibitor with Ki of 0.003 mM, and is a TRPV3 activator. Drofenine blocks Kv2.1-dependent potassium efflux, inhibits Kv2.1/JNK/NF-κB and IkBa/NF-kB signaling, suppresses Kv2.1 mRNA/protein expression. Drofenine suppresses oligomeric Aβ-induced microglial NLRP3 inflammasome activation and neuronal Tau hyperphosphorylation, improves cognitive impairment, promotes neurite outgrowth. Drofenine induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine ameliorates diabetic peripheral neuropathy -like pathology. Drofenine can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm .
17β-HSD10-IN-4 is a selective brain-penetrant 17β-HSD10 inhibitor with an IC50 of 6.33 μM. 17β-HSD10-IN-4 forms key interactions with the 17β-HSD10 catalytic triad to functionally inhibit the enzyme, without altering its protein levels. 17β-HSD10-IN-4 restores mitochondrial function, reduces ROS levels, increases ATP production, and suppresses cytochrome c release. 17β-HSD10-IN-4 attenuates CDK5/p25 activation, reduces Tau hyperphosphorylation, Aβ plaque load and restores brain-derived neurotrophic factor levels. 17β-HSD10-IN-4 improves cognitive function.17β-HSD10-IN-4 can be used for the research of Alzheimer's disease .
TDI-6570 (TDI-006570) is a blood-brain barrier-permeable, orally active cGAS inhibitor with an IC50 of 1.64 μM. TDI-6570 exhibits high gastrointestinal absorption and a long brain half-life in mice, and shows no toxicity to primary neurons. By inhibiting the cGAS-STING-IFN signaling pathway, TDI-6570 reduces STING levels and the activation of TBK1, blocks double-stranded DNA-induced cGAS activation and downstream interferon-stimulated gene expression, thereby reducing tauprotein spread and improving synaptic loss. TDI-6570 reverses memory deficits, increases the amplitude of long-term potentiation, enhances the MEF2C transcriptional network, restores PSD-95 and vGAT punctate structures, and significantly improves cognitive resilience. TDI-6570 can be applied to the research of Alzheimer's disease, Parkinson's disease, systemic lupus erythematosus, as well as various central nervous system and autoimmune diseases .
IU1 is a selective, reversible USP14 inhibitor with an IC50 of 4-5 μM. IU1 binds USP14’s catalytic cleft to block deubiquitinase activity. IU1 induces calpain-dependent Tau cleavage, causes ATP deficits, reduces E1~Ub thioester levels and 26S proteasome assembly. IU1 enhances 26S proteasome chymotrypsin-like activity, modulates LC3B-dependent autophagy flux, reduces cancer cell proliferation and migration, and blocks G0/G1 to S phase cell cycle transition in follicular thyroid cancer cells. IU1 activates autophagy-lysosomal and ubiquitin-proteasome pathways, triggers apoptosis, and reduces cervical cancer cell growth. IU1 enhances degradation of proteasome substrates linked to neurodegenerative disease, accelerates oxidized protein degradation, and increases oxidative stress resistance. IU1 can be used for the research of Alzheimer’s disease, follicular thyroid cancer, ischemic stroke, cervical cancer, and neurodegenerative disease .
Pongamol is an orally active flavonoid with an IC50 of 75 μM and a Ki of 58 μM against PTPase-1B, and an IC50 of 103.5 μM against intestinal α-Glycosidase. Pongamol reduces the release of IL‑1β, TNF‑α, COX‑2 and iNOS in cells, reverses the nuclear translocation of NF‑κB, and upregulates the levels of Beclin 1 and LC3 Ⅱ/LC3 Ⅰ. Pongamol promotes glucose uptake by increasing the level of GLUT4 on the surface of skeletal muscle cells. Pongamol inhibits epithelial-mesenchymal transition by suppressing the FAK/Akt-mTOR signaling pathway. Pongamol inhibits neuronal cytotoxicity, suppresses cell apoptosis and extends the lifespan of Caenorhabditis elegans by activating the MAPKs/Nrf2 signaling pathway. Pongamol exerts hypoglycemic effects in diabetic mouse models. Pongamol alleviates oxidative stress, neuroinflammation, Aβ deposition and excessive phosphorylation of TauProtein, and restores autophagy function in Alzheimer's disease mouse models by inhibiting the Akt/mTOR signaling pathway. Pongamol is applicable to research related to Alzheimer's disease, type 2 diabetes, non-small cell lung cancer and postprandial hyperglycemia .
H3R antagonist 4 (compound 11L) was a dual inhibitor of cholinesterase and histamine receptor (H3R), with corresponding IC50 of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible) and 1.09 nM (H3R) , respectively. H3R antagonist 4 inhibited the aggregation of Aβ1-42 induced by itself and Cu 2+ (95.48% and 88.63%) , and degraded the Aβ1-42 fibrils induced by itself and Cu 2+ (80.16% and 89.30%) . H3R antagonist 4 chelate biometals such as Cu 2+, Zn 2+, Al 3+, and Fe 2+. H3R antagonist 4 significantly reduced tauprotein hyperphosphorylation induced by Aβ1-42 and inhibited RSL-3-induced apoptosis and ferroptosis in PC12 cells. H3R antagonist 4 had the best blood-brain barrier permeability and intestinal absorption in hCMEC/D3 and hPepT1-MDCK cells.H3R antagonist 4 ameliorates learning and memory impairment in a mouse model of Alzheimer's disease induced by scopolamine (HY-N0296) .
COX-2/HDAC6-IN-1 (Compound 11e) is a dual COX-2 and HDAC6 inhibitor, with an IC50 of 0.12 μM against HDAC6 and an IC50 of 0.66 μM against COX-2. COX-2/HDAC6-IN-1 enhances the acetylation level of α-tubulin, regulates epigenetic gene expression, and inhibits the expression of pro-inflammatory mediators (COX-2, IL-1β, IL-6 and TNF-α). COX-2/HDAC6-IN-1 promotes Amyloid-β clearance and reduces excessive phosphorylation of Tauprotein. COX-2/HDAC6-IN-1 maintains neuronal morphology by stabilizing MAP2, protects synaptic integrity by regulating synapsin, and restores the expression of memory-related genes. COX-2/HDAC6-IN-1 possesses neuroprotective activity and improves learning and memory abilities in Scopolamine (HY-N0296)-induced Alzheimer's disease mouse models. COX-2/HDAC6-IN-1 is applicable to research related to Alzheimer's disease .
Leucomethylene blue (TRx0237) mesylate, an orally active second-generation tauprotein 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 .
BSB is a Congo red-derived fluorescent probe. BSB binds not only to extracellular amyloid β protein, but also many intracellular lesions composed of abnormal tau and synuclein proteins. BSB acts as a prototype imaging agent for Alzheimer's disease .
Mouse Serum Albumin is most abundant protein in plasma, which leaks into the brain parenchyma when the blood-brain barrier (BBB) is impaired. Mouse Serum Albumin induces astrocytes to A1 phenotype to remarkably increase levels of Elovl1. Mouse Serum Albumin promotes VLSFAs secretion and causes neuronal lippoapoptosis through endoplasmic reticulum stress response pathway. MSA-activated microglia triggeres remarkable tau phosphorylation at multiple sites (Ser202/Thr205) through NLRP3 inflammasome pathway. Mouse Serum Albumin decreases the spatial learning and memory abilities in mice. Mouse Serum Albumin can be used for the study of neurodegenerative diseases like Alzheimer’s disease (AD) and frontotemporal dementia (FTD) .
PHF6 (VQIVYK) is a self-assembly sequence capable of initiating the full-length tauprotein aggregation and is mapped to the third microtubule-binding repeat region of the tauprotein .
Tauprotein (592-597), human TFA is a peptide fragment of human Tauprotein. The dysfunction of Tauprotein is involved in neurodegeneration and dementia .
Tau Peptide (255-314) (Repeat 2 Domain) (human) (Tau-F protein (255-314)) is a polypeptide. Tau Peptide (255-314) (human) is the 255-314 fragment of Tau-F (also known as Tau-4, the 2N4 isoform), a major isoform of the Tauprotein. Tau Peptide (255-314) (human) contains two core driving sequences for Tau aggregation, namely PHF6* (275-280, VQIINK) and PHF6 (306-311, VQIVYK), and spans the C-terminal half of repeat domain R1, the entire repeat domain R2, and the N-terminal half of repeat domain R3 within the microtubule-binding region (MTBR).
PHF6 (VQIVYK) TFA is a self-assembly sequence capable of initiating the full-length tauprotein aggregation. PHF6 TFA is mapped to the third microtubule-binding repeat region of the tauprotein .
N-Boc-trans-4-fluoro-L-proline is a non-natural amino acid substitute used to construct monoclonal antibodies that specifically target the seed conformation of tauprotein .
Tau Peptide (275-305) (Repeat 2 domain) is the Alzheimer's Tau fragment R2, corresponding to the second repeat unit of the microtubule-binding domain, which is believed to be pivotal to the biochemical properties of full tauprotein. Tau Peptide (275-305) specifically coordinates with group IIB metal ions (Zn²⁺, Cd²⁺, Hg²⁺), which can induce their conformational changes and significantly promote their pathological accumulation. Tau Peptide (275-305) can be used to study the role of heavy metals in neurodegenerative diseases .
(Ser(PO3H2)202,Thr(PO3H2)205)-Tau Peptide (194-213) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
Tau Peptide (307-321) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
Tau Peptide (301-315) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
Tau Peptide (277-291) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
Tau Peptide (512-525) amide is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
Tau Peptide (337-368) (Repeat 4 Domain) is a 32-amino acid peptide derived from the fourth microtubule-binding repeat sequence (R4) of the tauprotein. Tau Peptide (337-368) (Repeat 4 Domain) can be used in research on neurodegenerative diseases .
Microtubule-associated proteintau (26-44) is a synthetic peptide chain with an amine group attached to glutamine and an carboxyl group attached to lysine.
Ac-Val-Gln-aIle-Val-aTyr-Lys-NH2 is a N-amino peptide that selectivity inhibits the fibrilization of tauprotein. Ac-Val-Gln-aIle-Val-aTyr-Lys-NH2 is effective at blocking the cellular seeding of endogenous tau by interacting with monomeric or fibrillar forms of extracellular tau. Ac-Val-Gln-aIle-Val-aTyr-Lys-NH2 can be used for the study of neurodegenerative diseases, such as Alzheimer’s disease .
(Ser(PO3H2)396,404)-Tau Peptide (379-408) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
Tau Peptide (298-312) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
Tau Peptide (306-317) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
Tau Peptide (304-318) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
Tau Peptide (274-288) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
Tau Peptide (295-309) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
Tau Peptide (268-282) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
TPSLP{pT}PPTR- 13C6, 15N4 TFA is the 13C- and 15N-labeled TPSLP{pT}PPTR TFA. TPSLP{pT}PPTR TFA is a tauprotein fragment phosphorylated in the central region.
Acetyl-Tau Peptide (244-274) (Repeat 1 Domain) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
Hepta-histidine is an inhibitor of Ku70-Huntingtin protein interaction. Hepta-histidine can reverse the morphological abnormalities of primary neurons differentiatied from hiPSCs. Hepta-histidine prolongs the lifespan in severe Huntington’s disease R6/2 mouse model. Hepta-histidine ameliorates DNA damage in vitro. Hepta-histidine can be used to study anti-aggregation agent against Tau-associated neurodegenerative diseases such as Alzheimer’s disease and Huntington’s disease .
MNP2 is a NLRP3-ASC interaction inhibitor. MNP2 selectively binds to the PYD domain of ASC (Ka=149 nM) and blocks ASC-PYM binding (Ka=58 nM), thereby inhibiting the interaction between ASC and NLRP3 and suppressing the formation of the NLRP3 inflammasome. MNP2 inhibits IL-1β release and caspase-1 maturation, and reduces the efflux of potassium and chloride ions. MNP2 prevents mitochondrial damage and reactive oxygen species production, and significantly decreases NLRP3 inflammasome formation in neurodegenerative pathologies induced by β-amyloid, Tauprotein and α-synuclein. MNP2 is applicable for the research of neurodegenerative diseases .
Bepranemab is a humanized IgG4 monoclonal antibody that binds to the central region of tauprotein. Bepranemab inhibits the seeding, aggregation of pathological tauprotein and the spread of tau pathology to distal brain regions. Bepranemab is applicable to research related to Alzheimer's disease .
Etalanetug (E2814) is a humanized high-affinity IgG1 antibody that targets tauprotein and can cross the blood-brain barrier. Etalanetug inhibits the spread of pathological tauprotein through high-affinity binding to the microtubule-binding region (MTBR). Etalanetug can be used in research related to Alzheimer's disease .
Semorinemab (RG 6100) is an anti-Tau humanized IgG4 monoclonal antibody, targets the N-terminal portion of the Tauprotein (amino acid residues 6-23). Semorinemab binds with human Tau with a Kd value of 3.8 nM. Semorinemab can be used for the research of Alzheimer's Disease .
ONC-841 is a blood-brain barrier-permeable, humanized monoclonal antibody targeting SIGLEC10. As an immune checkpoint inhibitor, ONC-841 restores the functions of immune effector cells such as T cells and enhances anti-tumor immune responses by blocking inhibitory signals mediated by SIGLEC10. ONC-841 restores the phagocytic and migratory activities of microglia, and promotes the phagocytosis of Amyloid-β and Tauprotein aggregates by microglia. ONC-841 is applicable to research related to solid tumors and Alzheimer's disease .
Posdinemab (JNJ-63733657) is a humanized IgG1/κ monoclonal antibody that selectively targets phosphorylated tau (pT217). Posdinemab specifically binds to the pT217+tau epitope rich in the proline domain, blocks tauprotein aggregation and seed propagation, and promotes the clearance of extracellular tau species. Posdinemab reduces the levels of free and total p217+tau in cerebrospinal fluid, thereby inhibiting the pathological propagation of tauprotein and the formation of neurofibrillary tangles. Posdinemab can be used for the study of progressive supranuclear palsy syndrome and Alzheimer's disease (AD), especially for prodromal or mild AD disease .
Gosuranemab (BMS-986168; IPN007; BIIB092) is a humanised IgG4 anti-tau monoclonal antibody. Gosuranemab neutralizes the extracellular tauprotein, inhibiting the spread and aggregation of pathological tauprotein. Gosuranemab can be used for the research of progressive supranuclear palsy and early Alzheimer’s disease .
Tilavonemab (ABBV-8E12) is a humanized anti-tau monoclonal antibody that binds to amino acids 25-30 near the N-terminus of the tauprotein. Tilavonemab can block the ability of human and mouse neurons to uptake tau aggregates. Tilavonemab can be used for research on Alzheimer’s disease and other tauopathies .
Zagotenemab (LY3303560) is a humanized anti-tau antibody that selectively binds and neutralises tau deposits in the brain. Zagotenemab can be used in Alzheimer's disease research .
Anti-Mouse/Human PrP/prion protein Antibody (TW1) is a mouse-derived IgG2a type antibody inhibitor, targeting to mouse/human PrP/prion protein. Anti-Mouse/Human PrP/prion protein Antibody (TW1) binds to both PrPc (cellular prion protein) and PrPSc (Scrapie Prion Protein) and blocks the interaction of prion protein with tauprotein. Anti-Mouse/Human PrP/prion protein Antibody (TW1) can be used for the researches of Alzheimer’s disease (AD) .
Etalanetug (Mouse IgG2a) (7G6 Antibody) is a mouse monoclonal antibody targeting the HVPGG motif in the microtubule-binding domain of tauprotein. Etalanetug (Mouse IgG2a) reduces the levels of insoluble tauprotein in multiple brain regions and inhibits the seeding and spread of pathological tauprotein. Etalanetug (Mouse IgG2a) is applicable to research related to Alzheimer's disease .
Gosuranemab (BMS-986168; IPN007; BIIB092) (powder) is a humanised IgG4 anti-tau monoclonal antibody. Gosuranemab (powder) neutralizes the extracellular tauprotein, inhibiting the spread and aggregation of pathological tauprotein. Gosuranemab (powder) can be used for the research of progressive supranuclear palsy and early Alzheimer’s disease .
Armanezumab is a pathological tauprotein inhibitor that specifically binds to the N-terminal domain exposed by pathological tauprotein (epitope covering amino acids 4-8: PRQEF). Armanezumab is applicable to research related to Alzheimer's disease, frontotemporal dementia, and Pick's disease .
ADEL-Y01 is a humanized and parental murine blood-brain barrier-penetrating monoclonal antibody against tau-acK280. ADEL-Y01 specifically recognizes tau-acK280 and its surrounding residues, mediates the neutralization and phagocytosis of acetylated tau aggregates, and interferes with the activity of pathological tauprotein. ADEL-Y01 prevents the progression of tauopathies, increases neuronal survival rate, reduces tau-related pathological changes, and improves memory impairment. ADEL-Y01 can be used in research related to Alzheimer's disease and tauopathies .
Lu AF87908 is an IgG1 monoclonal antibody targeting the p-Ser396/404 epitope of tauprotein, which mainly binds to the pSer396 region. Lu AF87908 can be used in the research of Alzheimer's disease. The recommended isotype control is human IgG1 kappa (HY-P99001) .
Okadaic acid, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid increases of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter. Okadaic acid induces tau phosphorylation .
Punicic acid is a bioactive compound of pomegranate seed oil. Punicic acid is an isomer of conjugated α-linolenic acid and ω-5 polyunsaturated fatty acids. Punicic acid has anti-inflammatory and antioxidant activities and can inhibit the expression of inflammatory mediators such as tumor necrosis factor α (TNF-α). Punicic acid can also reduce the formation of β-amyloid deposits and hyperphosphorylation of tau by increasing the expression of GLUT4 protein and inhibiting the overactivation of calpain, and is used to prevent and treat neurodegenerative diseases. In addition, punicic acid also has breast cancer inhibitor properties that depend on lipid peroxidation and PKC pathways .
Schisantherin B (Gomisin-B) is a lignan compound and one of the active components of Schisandra chinensis. Schisantherin B activates the PI3K/AKT signaling pathway, restores the activity of GSK3β, and reduces the hyperphosphorylation of tauprotein in hippocampal and cerebral cortical tissues. Schisantherin B upregulates the level of GLT-1, decreases the expression of pro-inflammatory cytokines TNF-α/IL-1β/IL-6, upregulates the expression of IL-10, and inhibits cell apoptosis. Schisantherin B is applicable to the research of spinal cord injury, Alzheimer's disease and depression .
Myricanol is a diarylheptanoid and a Nampt activator. Myricanol exerts anti-inflammatory effects and alleviates glucocorticoid-induced muscle atrophy by increasing Sirtuin 1 (SIRT1) and PRDX5 activities while regulating inflammatory factors. Myricanol exhibits growth inhibition and induces apoptosis in human lung adenocarcinoma A549 cells. Myricanol promotes autophagy-mediated clearance of microtubule-associated proteintau to exert neuroprotective effects. Myricanol protects cardiovascular function by inhibiting PDGFRβ and NF-κB signaling pathways. Myricanol activates mitochondrial transcription factor A (TFAM) expression to exert anti-renal fibrosis effects. Myricanol improves insulin resistance through AMPK activation .
(-)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 tauprotein. (-)Clausenamide exerts a significant neuroprotective activity against Aβ25-35. (-)Clausenamide can be used for researching Alzheimer's disease (AD) .
Pongamol is an orally active flavonoid with an IC50 of 75 μM and a Ki of 58 μM against PTPase-1B, and an IC50 of 103.5 μM against intestinal α-Glycosidase. Pongamol reduces the release of IL‑1β, TNF‑α, COX‑2 and iNOS in cells, reverses the nuclear translocation of NF‑κB, and upregulates the levels of Beclin 1 and LC3 Ⅱ/LC3 Ⅰ. Pongamol promotes glucose uptake by increasing the level of GLUT4 on the surface of skeletal muscle cells. Pongamol inhibits epithelial-mesenchymal transition by suppressing the FAK/Akt-mTOR signaling pathway. Pongamol inhibits neuronal cytotoxicity, suppresses cell apoptosis and extends the lifespan of Caenorhabditis elegans by activating the MAPKs/Nrf2 signaling pathway. Pongamol exerts hypoglycemic effects in diabetic mouse models. Pongamol alleviates oxidative stress, neuroinflammation, Aβ deposition and excessive phosphorylation of TauProtein, and restores autophagy function in Alzheimer's disease mouse models by inhibiting the Akt/mTOR signaling pathway. Pongamol is applicable to research related to Alzheimer's disease, type 2 diabetes, non-small cell lung cancer and postprandial hyperglycemia .
Nimbin is an orally active intermediate limonoid found in 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 is promising for research of neurodegenerative diseases and viral infections .
Schisantherin B (Gomisin-B) (Standard) is the analytical standard of Schisantherin B. This product is intended for research and analytical applications. Schisantherin B is a lignan compound and one of the active components of Schisandra chinensis. Schisantherin B activates the PI3K/AKT signaling pathway, restores the activity of GSK3β, and reduces the hyperphosphorylation of tauprotein in hippocampal and cerebral cortical tissues. Schisantherin B upregulates the level of GLT-1, decreases the expression of pro-inflammatory cytokines TNF-α/IL-1β/IL-6, upregulates the expression of IL-10, and inhibits cell apoptosis. Schisantherin B is applicable to the research of spinal cord injury, Alzheimer's disease and depression.
Microtubule-associated protein tau (MAPT) plays a key role in promoting microtubule assembly and stability, suggesting its potential contribution to the establishment of neuronal polarity.The C terminus binds to axonal microtubules, whereas the N terminus interacts with neuroplasmic membrane components, serving as a key linker protein between these structures.PNS-Tau/MAPT Protein, Mouse (P.pastoris, His) is the recombinant mouse-derived Microtubule-associated protein tau protein, expressed by P.pastoris , with N-6*His labeled tag.
Tau/0N3R protein is encoded by the Tau/0N3R gene and undergoes regulated alternative splicing to produce different mRNA species.Its expression varies in the nervous system according to the maturation and type of neurons.Fetal-tau/0N3R Protein, Human (His) is the recombinant human-derived Fetal-tau/0N3R protein, expressed by E.coli , with N-6*His labeled tag.
Microtubule-associated protein tau (MAPT) critically promotes microtubule assembly and stability, influencing neuronal polarity by acting as an important junction protein. Its dual role involves C-terminal binding to axonal microtubules and N-terminal binding to neuroplasmic membrane components. Tau-A/SC1 Protein, Rat (P.pastoris, His) is the recombinant rat-derived Microtubule-associated protein tau protein, expressed by P. pastoris , with N-His labeled tag.
Tau/0N3R protein is encoded by the Tau/0N3R gene and undergoes regulated alternative splicing to produce different mRNA species. Its expression varies in the nervous system according to the maturation and type of neurons. Tau/0N3R Protein, Human (His, solution) is the recombinant human-derived Tau/0N3R protein, expressed by E. coli , with N-His labeled tag.
Microtubule-associated protein tau is a microtubule-associated protein found in large numbers in neurons of the central nervous system (CNS). MAPT promotes microtubule assembly and stability and may be involved in the establishment and maintenance of neuronal polarity. Overexpression of MAPT is associated with a poor prognosis of prostate cancer. MAPT has been linked to neurological disorders such as Alzheimer's and Parkinson's disease. Tau-D/0N4R Protein, Human (133a.a, His) is the recombinant human-derived Tau-D/0N4R protein, expressed by E. coli , with C-6*His labeled tag.
Microtubule-associated protein tau (MAPT) plays a key role in promoting microtubule assembly and stability, suggesting its potential contribution to the establishment of neuronal polarity.The C terminus binds to axonal microtubules, whereas the N terminus interacts with neuroplasmic membrane components, serving as a key linker protein between these structures.PNS-Tau/MAPT Protein, Mouse (HEK293, His) is the recombinant mouse-derived PNS-Tau/MAPT protein, expressed by HEK293 , with N-10*His labeled tag.
Microtubule-associated protein tau is a microtubule-associated protein found in large numbers in neurons of the central nervous system (CNS). MAPT promotes microtubule assembly and stability and may be involved in the establishment and maintenance of neuronal polarity. Overexpression of MAPT is associated with a poor prognosis of prostate cancer. MAPT has been linked to neurological disorders such as Alzheimer's and Parkinson's disease. Tau-F/2N4R Protein, Human (HEK293, His) is the recombinant human-derived Tau-F/2N4R protein, expressed by HEK293 , with N-10*His labeled tag.
Tau/MAPT proteins crucially promote microtubule assembly and stability, which are critical for neuronal polarity. Structurally, its C terminus binds to axonal microtubules and its N terminus binds to neuroplasmic membrane components, suggesting its role as a connexin connecting microtubules to the plasma membrane. Tau-A/MAPT Protein, Macaca mulatta (HEK293, His) is the recombinant Rhesus Macaque-derived Tau-A/MAPT protein, expressed by HEK293 , with N-10*His labeled tag.
Microtubule-associated protein tau (MAPT) critically promotes microtubule assembly and stability, influencing neuronal polarity by acting as an important junction protein. Its dual role involves C-terminal binding to axonal microtubules and N-terminal binding to neuroplasmic membrane components. Tau-A/SC1 Protein, Rat (HEK293, His) is the recombinant rat-derived Tau-A/SC1 protein, expressed by HEK293 , with N-10*His labeled tag.
Microtubule-associated protein tau is a microtubule-associated protein found in large numbers in neurons of the central nervous system (CNS). MAPT promotes microtubule assembly and stability and may be involved in the establishment and maintenance of neuronal polarity. Overexpression of MAPT is associated with a poor prognosis of prostate cancer. MAPT has been linked to neurological disorders such as Alzheimer's and Parkinson's disease. Tau-441/2N4R Pre-formed Fibrils Protein, Human is the recombinant human-derived Tau-441/2N4R Pre-formed Fibrils protein, expressed by E. coli, with tag free.
Microtubule-associated protein tau is a microtubule-associated protein found in large numbers in neurons of the central nervous system (CNS). MAPT promotes microtubule assembly and stability and may be involved in the establishment and maintenance of neuronal polarity. Overexpression of MAPT is associated with a poor prognosis of prostate cancer. MAPT has been linked to neurological disorders such as Alzheimer's and Parkinson's disease. Tau-F/2N4R Protein, Human is the recombinant human-derived Tau-F/2N4R protein, expressed by E. coli , with tag free.
Interferon tau-1 (IFNT1) serves as an important paracrine hormone that initiates maternal recognition of pregnancy. After interacting with endometrial receptors, possibly type I interferon receptors, IFNT1 blocks estrogen receptor expression and prevents estrogen-induced upregulation of oxytocin receptor expression. Interferon tau-1/IFNT1 Protein, Bovine (P.pastoris, His) is the recombinant bovine-derived Interferon tau-1/IFNT1 protein, expressed by P. pastoris , with N-His labeled tag.
14-3-3 theta proteins are adapters in multiple signaling pathways that recognize phosphoserine or phosphothreonine motifs and modulate chaperone activity upon binding. It negatively regulates PDPK1 kinase activity, forms homodimers, and interacts with CDK16, phosphorylated RGS7, SSH1, phosphorylated CDKN1B, GAB2, phosphorylated PDPK1, and phosphorylated DAPK2. 14-3-3 theta Protein, Human (His) is the recombinant human-derived 14-3-3 theta protein, expressed by E. coli , with N-6His labeled tag.
14-3-3 theta proteins are adapters in multiple signaling pathways that recognize phosphoserine or phosphothreonine motifs and modulate chaperone activity upon binding. It negatively regulates PDPK1 kinase activity, forms homodimers, and interacts with CDK16, phosphorylated RGS7, SSH1, phosphorylated CDKN1B, GAB2, phosphorylated PDPK1, and phosphorylated DAPK2. 14-3-3 theta Protein, Human (GST) is the recombinant human-derived 14-3-3 theta protein, expressed by E. coli , with N-GST labeled tag.
The CK1d protein is an important serine/threonine protein kinase that complexly controls cellular processes such as Wnt signaling, DNA repair, and circadian rhythms. Its versatility is evident in phosphorylating a variety of proteins, including connexin-43/GJA1, MAP1A, p53/TP53, and YAP1. CK1d Protein, Human (sf9, GST) is the recombinant human-derived CK1d protein, expressed by sf9 insect cells , with N-GST labeled tag.
CDK5 is a proline-directed serine/threonine protein kinase that critically regulates neuronal cell cycle, differentiation and potential apoptosis in neuronal diseases by preventing cell cycle re-entry. It interacts with numerous proteins involved in neuronal development and coordinates processes such as survival, migration, differentiation, axonal growth, synaptogenesis, and neurotransmission. CDK5-p25 Protein, Human (sf9, GST, His, Flag) is the recombinant human-derived CDK5-p25, expressed by Sf9 insect cells, with N-GST, N-His, N-Flag labeled tag.
CDK5 is a proline-directed serine/threonine protein kinase that critically regulates neuronal cell cycle, differentiation and potential apoptosis in neuronal diseases by preventing cell cycle re-entry. It interacts with numerous proteins involved in neuronal development and coordinates processes such as survival, migration, differentiation, axonal growth, synaptogenesis, and neurotransmission. CDK5-p35 Protein, Human (sf9, GST, His, Flag) is the recombinant human-derived CDK5-p35, expressed by Sf9 insect cells, with N-His, N-GST, N-Flag labeled tag.
TPSLP{pT}PPTR- 13C6, 15N4 TFA is the 13C- and 15N-labeled TPSLP{pT}PPTR TFA. TPSLP{pT}PPTR TFA is a tauprotein fragment phosphorylated in the central region.
Phospho-Tau (Ser202/Thr205) Antibody (YA3436) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Phospho-Tau (Ser202/Thr205).
Phospho-Tau (Ser202/Thr205) Antibody (YA3436) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Phospho-Tau (Ser202/Thr205).
Diranersen (IONIS-MAPTRx) sodium is an antisense oligonucleotide that targets the human MAPT gene to inhibit the production of tauprotein. Diranersen sodium can be used in research related to Alzheimer's disease and tauopathies .
Diranersen (IONIS-MAPTRx) is an antisense oligonucleotide that targets the human MAPT gene to inhibit the production of tauprotein. Diranersen can be used in research related to Alzheimer's disease and tauopathies .
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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