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β-Amyloid (42-1), human is the inactive form of Amyloid β Peptide (1-42). β-Amyloid (42-1), human is a 42-amino acid peptide which plays a key role in the pathogenesis of Alzheimer disease .
β-Amyloid (42-1), human TFA is the inactive form of Amyloid β Peptide (1-42). β-Amyloid (42-1), human TFA is a 42-amino acid peptide which plays a key role in the pathogenesis of Alzheimer disease .
Citrullinated amyloid-β (1-40) peptide (human) (Citrullinated Aβ (1-40)) is a modified form of β-Amyloid (1-40) (HY-P0265) with a citrullination at the Arg5 site. Citrullinated amyloid-β (1-40) peptide (human) exhibits increased transient formation of soluble oligomers and insoluble aggregates composed of distorted parallel β-sheets compared with unmodified β-Amyloid (1-40) .
Citrullinated amyloid-β (1-42) peptide (human) (Citrullinated Aβ (1-42)) is a modified form of β-Amyloid (1-42) (HY-P1363) with a citrullination at the Arg5 site. Compared to the unmodified β-Amyloid (1-42), its formation of soluble low-molecular-weight oligomers is enhanced, the rate of fibril formation is reduced, and like unmodified Aβ42, it forms protofibrils comprised of parallel β-sheets .
AZD4694 Precursor (AZ13040214) is the precursor of [ 18F] AZD4694 for the synthesis of [ 18F] AZD4694, an amyloid-β imaging ligand with high affinity for amyloid-β plaques .
(Rac)-BIIB042 (Compound 10) is an modulator of γ-Secretase. (Rac)-BIIB042 reduces Amyloid-β 42 level with an EC50 value of 0.39 µM. (Rac)-BIIB042 can be used for the study of Alzheimer's disease .
NIAD-4 is a fluorophore for optical imaging of amyloid-β (Aβ) in the central nervous system (CNS) for Alzheimer’s disease (AD). NIAD-4 binds to the same Aβ site with the binding affinity (Ki) of 10 nM .
Santacruzamate A (CAY-10683, STA) is a potent and selective HDAC2 inhibitor with an IC50 of 119 pM. STA also exerts neuroprotective property against amyloid-β protein fragment 25–35. STA can be used for cancer and neurological disease research .
β-Amyloid (17-40) (Aβ(17-40)) is a fragment of Amyloid-β peptide that has shown neurotoxic activities in SH-SY5Y and IMR-32 cells. β-Amyloid (17-40) can be used for the research of neurological disease .
Stavudine (d4T) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine has activity against HIV-1 and HIV-2. Stavudine also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine induces apoptosis .
Stavudine (d4T) sodium is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine sodium has activity against HIV-1 and HIV-2. Stavudine sodium also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine sodium reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine sodium induces apoptosis .
Gantenerumab is a fully human anti-amyloid-β (Aβ) IgG1 monoclonal antibody demonstrates sustained cerebral amyloid-β binding. Gantenerumab can be used for Alzheimer's disease research .
Cu(II)GTSM, a cell-permeable Cu-complex, significantly inhibits GSK3β. Cu(II)GTSM inhibits Amyloid-β oligomers (AβOs) and decreases tau phosphorylation. Cu(II)GTSM also decreases the abundance of Amyloid-β trimers. Cu(II)GTSM is a potential anticancer and antimicrobial agent .
Aleplasinin is an orally active, potent, BBB-penetrated and selectiveSERPINE1 (PAI-1, Plasminogen activator inhibitor-1) inhibitor. Aleplasinin increases amyloid-β (Aβ) catabolism and ameliorates amyloid-related pathology. Aleplasinin improves memory deficiency. Aleplasinin can be used for Alzheimer's disease research .
AChE/BChE-IN-12 (compound 10b), a 3,5-dimethoxy analogue, is a potent AChE, BChE, and β-secretase-1 (BACE-1) inhibitor, with IC50 values of 2.57, 3.26, and 10.65 μM, respectively. AChE/BChE-IN-12 crosses the blood-brain barrier via passive diffusion and inhibits the self-aggregation of amyloid-β monomers. AChE/BChE-IN-12 can be used for Alzheimer’s disease (AD) research .
Glp-Amyloid-β (3-40) Peptide (human) (AβpE3-40) is a minor amounts of pyroglutamate-modified Aβ isolated from from 24-month-old Amyloid precursor protein (APP) transgenic Mice .
Latrepirdine dihydrochloride is a neuroactive compound with antagonist activity at histaminergic, α-adrenergic, and serotonergic receptors. Latrepirdine stimulates amyloid precursor protein (APP) catabolism and amyloid-β (Aβ) secretion.
Solanezumab is a humanized monoclonal IgG1 antibody directed against the mid-domain of the amyloid-β (Aβ) peptide. Solanezumab has the potential for the research of Alzheimer’s disease .
BChE-IN-31 (Compound 14d) is a selective BChE inhibitor with an IC50 of 65 nM. BChE-IN-31 inhibits the self-induced aggregation of neurotoxic amyloid-β (Aβ) peptide .
Dihydroergocristine mesylate (DHEC mesylate) is a inhibitor of γ-secretase (GSI), reduces the production of the Alzheimer's disease amyloid-β peptides, binds directly to γ-secretase and Nicastrin with equilibrium dissociation constants (Kd) of 25.7 nM and 9.8 μM, respectively .
JLK-6 markedly reduce the production of amyloid β-peptide (Aβ) by amyloid-β Precursor protein (APP) expressing HEK293 cells by affecting the γ-secretase cleavage of APP, with no effect on the cleavage of the Notch receptor .
Crocetin monomethyl ester, isolated from Crocus sativus, possesses anti-inflammatory, neuroprotective and antioxidant activity . Crocetin monomethyl ester promotes clearance of amyloid-β by inducing autophagy via the STK11/LKB1-mediated AMPK pathway .
AChE/Aβ-IN-5 (compound AV-2) is a bifunctional inhibitor that targets AChE and auto-induced Aβ (Amyloid-β) aggregation. AChE/Aβ-IN-5 can significantly improve scopolamine- and Aβ-induced cognitive impairment in mice .
Scyllo-Inositol, an amyloid inhibitor, potentialy inhibits α-synuclein aggregation. Scyllo-Inositol stabilizes a non-fibrillar non-toxic form of amyloid-β peptide (Aβ42) in vitro, reverses cognitive deficits, and reduces synaptic toxicity and lowers amyloid plaques in an Alzheimer's disease mouse model .
β-Amyloid peptide(16-20) is a amino acid sequences (KLVFF) of Amyloid-β (Abeta). β-Amyloid peptide(16-20) is an effective inhibitor of Abeta fibril formation, with RG-/-GR-NH2 residues added at N- and C-terminal ends to aid solubility) .
Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects .
Dihydroergocristine (mesylate) (Standard) is the analytical standard of Dihydroergocristine (mesylate). This product is intended for research and analytical applications. Dihydroergocristine mesylate (DHEC mesylate) is a inhibitor of γ-secretase (GSI), reduces the production of the Alzheimer's disease amyloid-β peptides, binds directly to γ-secretase and Nicastrin with equilibrium dissociation constants (Kd) of 25.7 nM and 9.8 μM, respectively .
Thiethylperazine dimaleate, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine dimaleate is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine dimaleate has anti-emetic, antipsychotic and antimicrobial effects .
(R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist . Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment .
BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC50 of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux .
DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC50s of 115 nM and 200 nM for total amyloid-β (Aβ) and Aβ42, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment .
Stavudine-d4 is the deuterium labeled Stavudine. Stavudine (d4T) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine has activity against HIV-1 and HIV-2. Stavudine also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine induces apoptosis[1][2][3][4].
Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment .
AChE/Aβ-IN-3 (compound AM5) is a dual inhibitor of AChE and Amyloid-β aggregation with IC50<.sub> values of 1.29 and 4.93 μM, respectively. AChE/Aβ-IN-3 has antioxidant properties that scavenge ROS and restore their normal levels. AChE/Aβ-IN-3 can be used in the study of neurological diseases, such as Alzheimer's disease .
Anti-Aβ agent 1A (compound M15) has potent activity against amyloid-β. Anti-Aβ agent 1A possesses can significantly inhibit LPS-induced levels of IL-1β, IL-6 and TNF-α, and reduces the apoptosis of SH-SY5Y induced by H2O2 through mitochondria pathway. Anti-Aβ agent 1A possesses antioxidant, anti-inflammatory, anti-Aβ toxicity and neuroprotective activities. Anti-Aβ agent 1A can be used for researching Alzheimer’s disease (AD) .
NB-360 is a potent, brain penetrable, and orally bioavailable dual BACE1/BACE2 inhibitor (IC50: mouse and human BACE1=5 nM; BACE2=6 nM). NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in amyloid precursor protein(APP) transgenic mice. NB-360 can completely block the progression of Aβ deposition in the brains of APP transgenic mice. NB-360 shows excellent selectivity over the related aspartyl proteases pepsin, cathepsin D and cathepsin E .
Buntanetap (L-Tartrate) is an orally administered small molecule inhibitor of several neurotoxic proteins. Buntanetap reduces amyloid precursor protein (APP) production by blocking its mRNA translation .
Aducanumab (BIIB037) is a human monoclonal antibody that selectively targets aggregated amyloid-beta (Aβ). Aducanumab shows brain penetration, and can be used for Alzheimer's disease (AD) research .
β-Amyrin, an ingredient of Celastrus hindsii, blocks amyloid β (Aβ)-induced long-term potentiation (LTP) impairment. β-amyrin is a promising candidate of treatment for AD .
Donanemab (LY3002813) is a humanized IgG1 monoclonal antibody directed at an N‐terminal pyroglutamate amyloid beta (Aβ) epitope. Donanemab has the potential for early Alzheimer's disease research .
Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE . Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity .
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 .
Trontinemab is a bispecific and humanizedized IgG1-κ antibody, targeting to amyloid beta A4 precursor protein (APP) and transferrin receptor, p90, CD71 (TFRC). Trontinemab can be used for research on Alzheimer disease (AD) .
Remternetug is a human immunoglobulin G1-kappa, anti-APP (amyloid beta A4 precursor protein) Aβ42 N3pGlu peptide monoclonal antibody. Remternetug recognizes a pyroglutamated form of Aβ that aggregates into amyloid plaques .
Artanin is a coumarin, has biological activities related to Alzheimer’s disease. Artanin exerts function including AChE inhibitory and AChE- and self-induced amyloid beta (Aβ) aggregation inhibitory activities, with IC50s of 51 μM, 98 μM, and 124 μM, respectively .
AChE-IN-47 (compound g17) is a AChE inhibitor with the IC50 of 0.24 μM. AChE-IN-47 inhibits amyloid β peptides self-aggregation. AChE-IN-47 displays neuroprotective effects and effectively suppresses the intracellular accumulation of reactive oxygen species .
LY2389575 hydrochloride is a selective and noncompetitive mGlu3 negative allosteric modulator (NAM), with an IC50 value of 190 nM. LY2389575 hydrochloride induces an increase in Mrc1 levels. LY2389575 hydrochloride also independently amplifies Amyloid beta (Aβ) toxicity and can be used in study of Alzheimer's disease .
Saikosaponin C is a bioactive component found in radix bupleuri, targets amyloid beta and tau in Alzheimer's disease. Saikosaponin C inhibits the secretion of both Aβ1-40 and Aβ1-42, and suppresses abnormal tau phosphorylation, but shows no effect on BACE1 activity and expression .
Ethyl ferulate, a naturally lipophilic derivative of ferulic acid originally derived from Rhizoma Chuanxiong, induces heme oxygenase-1 (HO-1) and protects rat neurons against oxidative stress . Ethyl ferulate also protects neurons against amyloid β peptide (1-42)-induced oxidative stress and neurotoxicity .
Semilicoisoflavone B, an isoflavone, mainly derived from Glycyrrhiza uralensis Fisch.. Semilicoisoflavone B reduces amyloid β (Aβ) secretion by inhibiting β-secretase-1 (BACE1) expression and activity. Semilicoisoflavone B decreases BACE1 expression mainly through increasing PPARγ expression and inhibiting STAT3 phosphorylation .
(R)-DRF053 dihydrochloride is a potent casein kinases 1 (CK1), CDK1/cyclin B and CDK5/p25 inhibitor with IC50s of 14 nM, 220 nM and 80 nM, respectively. (R)-DRF053 dihydrochloride prevents the CK1-dependent production of amyloid-beta in a cell model .
MAO-B-IN-10 (compound 4f) is a potent, selective, BBB-penetrated MAO-B (monoamine oxidase-B) inhibitor, with IC50 of 5.3 μM. MAO-B-IN-10 can inhibit (58.2%) and disaggregate (43.3%) self-mediated Aβ (amyloid β) aggregation. MAO-B-IN-10 can be use for Alzheimer’s disease research .
Aβ-IN-4 (compound 12) is a potent amyloid β (Aβ) inhibitor. Aβ-IN-4 inhibits Aβ42 aggregation. However, Aβ-IN-4 can not alleviate the neurotoxicity of Aβ42 in SH-SY5Y cells. Aβ-IN-4 can not change the aggregation state of Aβ42 into a nontoxic one .
Aβ-IN-3 (compound 1) is a potent amyloid β (Aβ) inhibitor. Aβ-IN-3 inhibits Aβ42 aggregation. However, Aβ-IN-3 can not alleviate the neurotoxicity of Aβ42 in SH-SY5Y cells. Aβ-IN-3 can not change the aggregation state of Aβ42 into a nontoxic one .
Kaempferol-3,7-di-O-β-glucoside (Kaempferol 3,7-diglucoside), a flavonol, possesses enzyme inhibition property towards α-amylase, α-glucosidase and Acetylcholinesterase. Kaempferol-3,7-di-O-β-glucoside protects differentiating neuronal cells, SH-SY5Y from Amyloid β peptide-induced injury. Kaempferol-3,7-di-O-β-glucoside has the potential for Alzheimer's research .
2-O-Acetyl-20-hydroxyecdysone, an ecdysterones in insects and terrestrial plants, inhibits amyloid-β42 (Aβ42)-induced cytotoxicity. 2-O-Acetyl-20-hydroxyecdysone could decrease Aβ oligomer formation through promotion of fibrogenesis, transforming Aβ oligomers to the low-toxicity fibrils .
OAB-14, is a Bexarotene (HY-14171) derivative, improves Alzheimer's disease-related pathologies and cognitive impairments by increasing β-amyloid clearance in APP/PS1 mice. OAB-14 effectively ameliorates the dysfunction of the endosomal-autophagic-lysosomal pathway in APP/PS1 transgenic mice .
γ-Secretase modulator 12 (Compound 1a) is a γ-secretase modulator that can selectively decrease amyloid-β42 (Aβ42) levels (IC50 of 0.39 µM). γ-Secretase modulator 12 can be used for Alzheimer’s disease research. γ-Secretase modulator 12 has a good brain/plasma ratio (Kp, brain = 0.72) in mice .
Licochalcone B is an extract from the root of Glycyrrhiza uralensis. Licochalcone B inhibits amyloid β (42) self-aggregation (IC50=2.16 μM) and disaggregate pre-formed Aβ42 fibrils, reduce metal-induced Aβ42 aggregation through chelating metal ionsLicochalcone B inhibits phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone B inhibits growth and induces apoptosis of NSCLC cells. Licochalcone B specifically inhibits the NLRP3 inflammasome by disrupting NEK7‐NLRP3 interaction .
Multitarget AD inhibitor-1 is a selective and reversible butyrylcholinesterase (BuChE) inhibitor with IC50s of 7.22 μM and 1.55 μM for hBuChE and eqBuChE (BuChE from equine serum), respectively. Multitarget AD inhibitor-1 inhibits β-secretase (IC50hBACE-1=41.60 μM), amyloid β aggregation (IC50Aβ=3.09 μM), tau aggregation. Multitarget AD inhibitor-1, a diphenylpropylamine derivative, has the potential for multifunctional disease-modifying anti-Alzheimer’s research .
Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) is a potent amyloid β (Aβ) inhibitor. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases the expression of acetylcholine (ACh) levels, choline acetyltransferase (ChAT) activity, and ChAT gene induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) decreases in acetyl cholinesterase (AChE) activity and AChE gene expression induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases muscarinic M1 receptor gene expression and muscarinic M1 receptor binding activity. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) can be used for Alzheimer's disease research .
YIAD-0205 is an orally available Aβ(1?42) aggregation inhibitor. YIAD-0205 demonstrated in vivo efficacy in an AD transgenic mouse model with five familial AD mutations (5XFAD) .
β-Sheet Breaker Peptide iAβ5 is a potent degrader of cerebral amyloid-beta (Abeta). Abeta deposition is associatied with the Alzheimer disease (AD), due to its related toxicity linked to its beta-sheet conformation and/or aggregation. β-Sheet Breaker Peptide iAβ5 reproducibly induces in vivo disassembly of fibrillar amyloid deposits. Thus, β-Sheet Breaker Peptide iAβ5 prevents and/or reverses neuronal shrinkage caused by Abeta, and reduces the extent of interleukin-1beta positive microglia-like cells that surround the Abeta deposits. β-Sheet Breaker Peptide iAβ5 reduces the size and/or number of cerebral amyloid plaques in AD. β-Sheet Breaker Peptide iAβ5 labeled by hydrophobic benzyl alcohol (HBA) tag, can be used for quantitative assay by showing vivid blue color under acidic conditions .
Alzheimer’s Disease (AD) is a progressive degenerative brain disease which causes mental and physical decline, gradually resulting in death. Despite the significant public health issue that it poses, only few medical treatments have been approved for Alzheimer’s Disease (AD) and these act to control symptoms rather than alter the course of the disease. Discovery of new therapeutic approaches depends on the study of pathology of AD. Recent research findings have led to greater understanding of disease neurobiology in Alzheimer's Disease (AD) and identification of unique targets for drug development. Several important mechanisms have been proposed to explain the underlying pathology of AD, such as Amyloid cascade hypothesis, Tau hypothesis and Cholinergic hypothesis, etc.
MCE offers a unique collection of 1374 compounds with anti-Alzheimer’s Disease activities or targeting the unique targets of AD. MCE Anti-Alzheimer’s Disease Compound Library is a useful tool for exploring the mechanism of AD and discovering new drugs for AD.
Neurodegenerative diseases are incurable and life-threatening conditions that result in progressive degeneration and/or death of nerve cells. Some common neurodegenerative diseases include Alzheimer’s Disease (AD), Parkinson’s Disease (PD), Motor Neuron Disease (MND), Huntington’s Disease (HD), Spino-Cerebellar Ataxia (SCA), Spinal Muscular Atrophy (SMA), and Amyotrophic Lateral Sclerosis (ALS). Because the pathophysiology of neurodegenerative disorders is generally poorly understood, it is difficult to identify promising molecular targets and validate them. At the same time, about 85% of the drugs fail in clinical trials. Therefore, validating new targets and discovering new drugs to mitigate neurodegenerative disorders is need of the hour.
MCE offers a unique collection of 2228 compounds with anti-Neurodegenerative Diseases activities or targeting the unique targets of neurodegenerative diseases. MCE Neurodegenerative Disease-related Compound Library is a useful tool for exploring the mechanism of neurodegenerative diseases and discovering new drugs for neurodegenerative diseases.
NIAD-4 is a fluorophore for optical imaging of amyloid-β (Aβ) in the central nervous system (CNS) for Alzheimer’s disease (AD). NIAD-4 binds to the same Aβ site with the binding affinity (Ki) of 10 nM .
β-Amyloid (42-1), human is the inactive form of Amyloid β Peptide (1-42). β-Amyloid (42-1), human is a 42-amino acid peptide which plays a key role in the pathogenesis of Alzheimer disease .
β-Amyloid (42-1), human TFA is the inactive form of Amyloid β Peptide (1-42). β-Amyloid (42-1), human TFA is a 42-amino acid peptide which plays a key role in the pathogenesis of Alzheimer disease .
Citrullinated amyloid-β (1-40) peptide (human) (Citrullinated Aβ (1-40)) is a modified form of β-Amyloid (1-40) (HY-P0265) with a citrullination at the Arg5 site. Citrullinated amyloid-β (1-40) peptide (human) exhibits increased transient formation of soluble oligomers and insoluble aggregates composed of distorted parallel β-sheets compared with unmodified β-Amyloid (1-40) .
Citrullinated amyloid-β (1-42) peptide (human) (Citrullinated Aβ (1-42)) is a modified form of β-Amyloid (1-42) (HY-P1363) with a citrullination at the Arg5 site. Compared to the unmodified β-Amyloid (1-42), its formation of soluble low-molecular-weight oligomers is enhanced, the rate of fibril formation is reduced, and like unmodified Aβ42, it forms protofibrils comprised of parallel β-sheets .
β-Amyloid (17-40) (Aβ(17-40)) is a fragment of Amyloid-β peptide that has shown neurotoxic activities in SH-SY5Y and IMR-32 cells. β-Amyloid (17-40) can be used for the research of neurological disease .
Glp-Amyloid-β (3-40) Peptide (human) (AβpE3-40) is a minor amounts of pyroglutamate-modified Aβ isolated from from 24-month-old Amyloid precursor protein (APP) transgenic Mice .
β-Amyloid peptide(16-20) is a amino acid sequences (KLVFF) of Amyloid-β (Abeta). β-Amyloid peptide(16-20) is an effective inhibitor of Abeta fibril formation, with RG-/-GR-NH2 residues added at N- and C-terminal ends to aid solubility) .
β-Sheet Breaker Peptide iAβ5 is a potent degrader of cerebral amyloid-beta (Abeta). Abeta deposition is associatied with the Alzheimer disease (AD), due to its related toxicity linked to its beta-sheet conformation and/or aggregation. β-Sheet Breaker Peptide iAβ5 reproducibly induces in vivo disassembly of fibrillar amyloid deposits. Thus, β-Sheet Breaker Peptide iAβ5 prevents and/or reverses neuronal shrinkage caused by Abeta, and reduces the extent of interleukin-1beta positive microglia-like cells that surround the Abeta deposits. β-Sheet Breaker Peptide iAβ5 reduces the size and/or number of cerebral amyloid plaques in AD. β-Sheet Breaker Peptide iAβ5 labeled by hydrophobic benzyl alcohol (HBA) tag, can be used for quantitative assay by showing vivid blue color under acidic conditions .
Gantenerumab is a fully human anti-amyloid-β (Aβ) IgG1 monoclonal antibody demonstrates sustained cerebral amyloid-β binding. Gantenerumab can be used for Alzheimer's disease research .
Solanezumab is a humanized monoclonal IgG1 antibody directed against the mid-domain of the amyloid-β (Aβ) peptide. Solanezumab has the potential for the research of Alzheimer’s disease .
Oloctinebart is a humanized immunoglobulin G4-kappa, anti-LGALS3 monoclonal antibody. Oloctinebart is used for reduction of amyloid beta oligomers formation .
Aducanumab (BIIB037) is a human monoclonal antibody that selectively targets aggregated amyloid-beta (Aβ). Aducanumab shows brain penetration, and can be used for Alzheimer's disease (AD) research .
Donanemab (LY3002813) is a humanized IgG1 monoclonal antibody directed at an N‐terminal pyroglutamate amyloid beta (Aβ) epitope. Donanemab has the potential for early Alzheimer's disease research .
Trontinemab is a bispecific and humanizedized IgG1-κ antibody, targeting to amyloid beta A4 precursor protein (APP) and transferrin receptor, p90, CD71 (TFRC). Trontinemab can be used for research on Alzheimer disease (AD) .
Remternetug is a human immunoglobulin G1-kappa, anti-APP (amyloid beta A4 precursor protein) Aβ42 N3pGlu peptide monoclonal antibody. Remternetug recognizes a pyroglutamated form of Aβ that aggregates into amyloid plaques .
Santacruzamate A (CAY-10683, STA) is a potent and selective HDAC2 inhibitor with an IC50 of 119 pM. STA also exerts neuroprotective property against amyloid-β protein fragment 25–35. STA can be used for cancer and neurological disease research .
Crocetin monomethyl ester, isolated from Crocus sativus, possesses anti-inflammatory, neuroprotective and antioxidant activity . Crocetin monomethyl ester promotes clearance of amyloid-β by inducing autophagy via the STK11/LKB1-mediated AMPK pathway .
Scyllo-Inositol, an amyloid inhibitor, potentialy inhibits α-synuclein aggregation. Scyllo-Inositol stabilizes a non-fibrillar non-toxic form of amyloid-β peptide (Aβ42) in vitro, reverses cognitive deficits, and reduces synaptic toxicity and lowers amyloid plaques in an Alzheimer's disease mouse model .
β-Amyrin, an ingredient of Celastrus hindsii, blocks amyloid β (Aβ)-induced long-term potentiation (LTP) impairment. β-amyrin is a promising candidate of treatment for AD .
Artanin is a coumarin, has biological activities related to Alzheimer’s disease. Artanin exerts function including AChE inhibitory and AChE- and self-induced amyloid beta (Aβ) aggregation inhibitory activities, with IC50s of 51 μM, 98 μM, and 124 μM, respectively .
Saikosaponin C is a bioactive component found in radix bupleuri, targets amyloid beta and tau in Alzheimer's disease. Saikosaponin C inhibits the secretion of both Aβ1-40 and Aβ1-42, and suppresses abnormal tau phosphorylation, but shows no effect on BACE1 activity and expression .
Ethyl ferulate, a naturally lipophilic derivative of ferulic acid originally derived from Rhizoma Chuanxiong, induces heme oxygenase-1 (HO-1) and protects rat neurons against oxidative stress . Ethyl ferulate also protects neurons against amyloid β peptide (1-42)-induced oxidative stress and neurotoxicity .
Semilicoisoflavone B, an isoflavone, mainly derived from Glycyrrhiza uralensis Fisch.. Semilicoisoflavone B reduces amyloid β (Aβ) secretion by inhibiting β-secretase-1 (BACE1) expression and activity. Semilicoisoflavone B decreases BACE1 expression mainly through increasing PPARγ expression and inhibiting STAT3 phosphorylation .
Kaempferol-3,7-di-O-β-glucoside (Kaempferol 3,7-diglucoside), a flavonol, possesses enzyme inhibition property towards α-amylase, α-glucosidase and Acetylcholinesterase. Kaempferol-3,7-di-O-β-glucoside protects differentiating neuronal cells, SH-SY5Y from Amyloid β peptide-induced injury. Kaempferol-3,7-di-O-β-glucoside has the potential for Alzheimer's research .
2-O-Acetyl-20-hydroxyecdysone, an ecdysterones in insects and terrestrial plants, inhibits amyloid-β42 (Aβ42)-induced cytotoxicity. 2-O-Acetyl-20-hydroxyecdysone could decrease Aβ oligomer formation through promotion of fibrogenesis, transforming Aβ oligomers to the low-toxicity fibrils .
Licochalcone B is an extract from the root of Glycyrrhiza uralensis. Licochalcone B inhibits amyloid β (42) self-aggregation (IC50=2.16 μM) and disaggregate pre-formed Aβ42 fibrils, reduce metal-induced Aβ42 aggregation through chelating metal ionsLicochalcone B inhibits phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone B inhibits growth and induces apoptosis of NSCLC cells. Licochalcone B specifically inhibits the NLRP3 inflammasome by disrupting NEK7‐NLRP3 interaction .
Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) is a potent amyloid β (Aβ) inhibitor. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases the expression of acetylcholine (ACh) levels, choline acetyltransferase (ChAT) activity, and ChAT gene induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) decreases in acetyl cholinesterase (AChE) activity and AChE gene expression induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases muscarinic M1 receptor gene expression and muscarinic M1 receptor binding activity. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) can be used for Alzheimer's disease research .
There is no specific Pubmed ID mentioned in the paragraph. Amyloid Precursor/Beta-APP42 Protein, Human (His-GST) is the recombinant human-derived Amyloid Precursor/Beta-APP42 protein, expressed by E. coli , with N-His, N-GST labeled tag. The total length of Amyloid Precursor/Beta-APP42 Protein, Human (His-GST) is 42 a.a., with molecular weight of ~27-31 KDa.
There is no specific Pubmed ID mentioned in the paragraph. APP/Protease Nexin-II Protein, Human (HEK293, Fc) is the recombinant human-derived APP/Protease Nexin-II protein, expressed by HEK293 , with C-hFc labeled tag. The total length of APP/Protease Nexin-II Protein, Human (HEK293, Fc) is 652 a.a., with molecular weight of 150-160 kDa.
The TM2D1 protein may be involved in amyloid beta-induced apoptosis by interacting with beta-APP42, especially amyloid beta protein 42 (APP beta-APP42). This suggests a role in molecular pathways associated with amyloid-induced cell death. TM2D1 Protein, Human (HEK293, Fc) is the recombinant human-derived TM2D1 protein, expressed by HEK293 , with C-mFc labeled tag. The total length of TM2D1 Protein, Human (HEK293, Fc) is 81 a.a., with molecular weight of 45-60 KDa.
There is no specific Pubmed ID mentioned in the paragraph. Amyloid Precursor/Beta-APP40 Protein, Human (His-GST) is the recombinant human-derived Amyloid Precursor/Beta-APP40 protein, expressed by E. coli , with N-His, N-GST labeled tag. The total length of Amyloid Precursor/Beta-APP40 Protein, Human (His-GST) is 40 a.a., with molecular weight of ~33 kDa.
APBA3 Protein, Human (rHuAPBA3, His; Amyloid beta A4 precursor protein-binding family A member 3; APBA3) is an approximately 20.0 kDa APBA3 protein fused to His-tag. APBA3 Protein, Human (His) is an adapter protein that belongs to the X11 family and is involved in signal transduction processes.
APLP-1 protein is involved in postsynaptic function and synaptic processes. Its processing produces ALID1, which activates transcription through APBB1 binding. APLP-1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived APLP-1 protein, expressed by HEK293 , with C-His labeled tag. The total length of APLP-1 Protein, Mouse (HEK293, His) is 584 a.a., with molecular weight of ~62.4 kDa.
Stavudine-d4 is the deuterium labeled Stavudine. Stavudine (d4T) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine has activity against HIV-1 and HIV-2. Stavudine also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine induces apoptosis[1][2][3][4].