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BMS 299897 is a sulfonamide γ-secretase inhibitor with an IC50 of 7 nM for Aβ production inhibition in HEK293 cells stably overexpressing amyloid precursorprotein (APP).
Latrepirdine dihydrochloride is a neuroactive compound with antagonist activity at histaminergic, α-adrenergic, and serotonergic receptors. Latrepirdine stimulates amyloid precursorprotein (APP) catabolism and amyloid-β (Aβ) secretion.
Buntanetap (L-Tartrate) is an orally administered small molecule inhibitor of several neurotoxic proteins. Buntanetap reduces amyloid precursorprotein (APP) production by blocking its mRNA translation .
PF-06751979 is a potent, brain penetrant, β-site amyloid precursorprotein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 7.3 nM in BACE1 binding assay.
Begacestat (GSI-953) is a selective thiophene sulfonamide inhibitor of amyloid precursorproteingamma-secretase (IC50Aβ40=15 nM) for the treatment of Alzheimer's 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 precursorprotein (APP) transgenic Mice .
Scoulerine ((-)-Scoulerine), an isoquinoline alkaloid, is a potent antimitotic compound. Scoulerine is also an inhibitor of BACE1 (ß-site amyloid precursorprotein cleaving enzyme 1). Scoulerine inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells .
α-Secretase Substrate II, Fluorogenic is an internally quenched fluorogenic peptide substrate for α-Secretase that contains the α-secretase cleavage site of β-Amyloid precursorprotein (APP) .Ex/Em = 340/490 nm
Fmoc-Ala-Glu-Asn-Lys-NH2 is a selective asparagine endopeptidase (AEP) inhibitor peptide and suppresses amyloid precursorprotein (APP) cleavage. AEP, a pH-controlled cysteine proteinase, is activated during ageing and mediates APP proteolytic processing .
BACE-IN-1 (Compound 13) is a substituted lmidazo[1 ,2-a]pyridine derivative which can inhibit β-site amyloid precursorprotein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease.
DSS30 is a P25/CDK5 inhibitor that reduces β-amyloid (Aβ) secretion by inhibiting amyloid precursorprotein lyase 1 (BACEl) phosphorylation. DSS30 can be used in the study of neurodegenerative diseases such as Alzheimer's disease .
Buntanetap ((+)-Phenserine) is a multiple neurotoxic protein translation inhibitor with oral activity, including amyloid precursorprotein (APP), α-synuclein (αSYN) and huntingtin protein (HTT). Buntanetap has anti-inflammatory effects and can be used in the study of Alzheimer's disease and Parkinson's disease .
Biotin-β-Amyloid (17-40) is a N-terminal-labelled biotinylated amyloid-ß-(1-40) peptide. β-Amyloid (17-40) is a 24-residue fragment of the Aβprotein via post-translational processing of amyloid precursorprotein (APP) .
Phenserine ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine reduces β-amyloid precursorprotein (APP) and β-amyloid peptide (Aβ) formation. Phenserine improves cognitive performance and attenuates the progression of Alzheimer's disease .
Umibecestat (CNP520) is a beta-site amyloid precursorprotein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively . Umibecestat can be used for the research of alzheimer's disease.
Aβ42-IN-5 (Compound 0152) is an oral active amyloid precursorprotein (APP) degrader that can reduce Aβ42 in Alzheimer's disease iPSC neurons. Aβ42-IN-5 can bind CAPRIN1 and APP and enhance the protein-protein interaction .
Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursorprotein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat s tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat has the potential for Alzheimer's Disease treatment .
TML-6-d3 is the deuterium labeled TML-6. TML-6, an orally active curcumin derivative, inhibits the synthesis of the β-amyloid precursorprotein and β-amyloid (Aβ). TML-6 can upregulate Apo E, suppress NF-κB and mTOR, and increase the activity of the anti-
(Rac)-AZD3839 is an orally active beta-amyloid precursorprotein cleaving enzyme (BACE1) inhibitor that is blood-brain barrier-permeable. (Rac)-AZD3839 has an affinity for the human ether-a-go-go related gene (hERG) ion channel. (Rac)-AZD3839 can be used in the research of Alzheimer's disease .
(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 precursorprotein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment .
BACE1-IN-5 (Compound 15) is a β-site amyloid precursorprotein 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 .
TML-6, an orally active curcumin derivative, inhibits the synthesis of the β-amyloid precursorprotein and β-amyloid (Aβ). TML-6 can upregulate Apo E, suppress NF-κB and mTOR, and increase the activity of the anti-oxidative Nrf2 gene. TML-6 has the potential for Alzheimer’s disease (AD) research .
Amyloid 17-42 (Aβ(17-42)) is a major constituent of diffuse plaques in Alzheimer's disease and cerebellar pre-amyloid in Down's syndrome, derived by alpha- and gamma-secretase cleavage of the amyloid precursorprotein (APP). Amyloid 17-42 can induce neuronal apoptosis via a Fas-like/caspase-8 activation pathway .
ELN318463 is an amyloid precursorprotein (APP) selective γ-secretase inhibitor. ELN318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC50s of 12 nM and 656 nM for PS1 and PS2, respectively. ELN318463 is 51-fold more selective for PS1 .
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 precursorprotein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment .
ELN318463 racemate is the racemate of ELN318463. ELN318463 is an amyloid precursorprotein (APP) selective γ-secretase inhibitor. ELN318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC50s of 12nM and 656 nM for PS1and PS2, respectively. ELN318463 is 51-fold more selective for PS1 .
LY2886721 is a potent, selective and orally active beta-site amyloid precursorprotein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant humanBACE1. LY2886721 is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 can across blood-brain barrier and has the potential for Alzheimer's disease treatment .
Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursorprotein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects .
LY2886721 hydrochloride is a potent, selective and orally active beta-site amyloid precursorprotein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant humanBACE1. LY2886721 hydrochloride is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 hydrochloride can across blood-brain barrier and has the potential for Alzheimer's disease treatment .
AM-6494 is a potent and orally active BACE1 (efficacious β-site amyloid precursorprotein cleaving enzyme 1) inhibitor (IC50=0.4 nM) with in vivo selectivity over BACE2 (IC50=18.6 nM) . AM-6494 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Mca-SEVNLDAEFK(Dnp) is a Beta-secretase 1 (BACE-1) peptide FRET substrate, containing the 'Swedish' Lys-Met/Asn-Leu mutation of the amyloid precursorprotein (APP) β-secretase cleavage site. Cleavage at -Leu-Asp- of Mca-SEVNLDAEFK(Dnp) liberates the highly fluorescent 7-methoxycoumarin (Mca) fragment from the proximity quenching effect of the 2,4-dinitrophenyl (Dnp) internal quencher resulting in a large and easily detectable increase in fluorescence intensity.
His-D-beta-Nal-Ala-Trp-D-Phe-Lys-NH2 TFA, is a growth hormone releasing peptide, as well as a metabolite of GHRP-1. GHRP-1, or Ala-His-D-beta Nal-Ala-Trp-D-Phe-Lys-NH2, has the effect of promoting the release of growth hormone (GH). GHRP-1 increases GH release and increases [Ca2+]i levels in static monolayer cells of rat pituitary gland, but does not affect cAMP levels .
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 precursorprotein(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 .
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 precursorprotein) 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 .
β-Amyloid precursorprotein (96-110), cyclized (human) is an amyloid precursorprotein. β-Amyloid precursorprotein (96-110), cyclized (human) can be used in study Alzheimer’s disease .
Mca-SEVKMDAEFRK(Dnp)RR-NH2, containing the wild-type amyloid precursorprotein (APP) beta-secretase cleavage site, is the substrate of thimet oligopeptidase (TOP). It is used for Alzheimer's disease 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 precursorprotein (APP) transgenic Mice .
α-Secretase Substrate II, Fluorogenic is an internally quenched fluorogenic peptide substrate for α-Secretase that contains the α-secretase cleavage site of β-Amyloid precursorprotein (APP) .Ex/Em = 340/490 nm
Fmoc-Ala-Glu-Asn-Lys-NH2 is a selective asparagine endopeptidase (AEP) inhibitor peptide and suppresses amyloid precursorprotein (APP) cleavage. AEP, a pH-controlled cysteine proteinase, is activated during ageing and mediates APP proteolytic processing .
Biotin-β-Amyloid (17-40) is a N-terminal-labelled biotinylated amyloid-ß-(1-40) peptide. β-Amyloid (17-40) is a 24-residue fragment of the Aβprotein via post-translational processing of amyloid precursorprotein (APP) .
[Arg6]-β-Amyloid (1-42), england mutation is a biological active peptide. (Several mutations in the betaamyloid precursor gene cause autosomal dominant Alzheimer's Disease in a number of kindreds.Tthe English (H6R) mutation will disrupt H6 interactions.)
Amyloid 17-42 (Aβ(17-42)) is a major constituent of diffuse plaques in Alzheimer's disease and cerebellar pre-amyloid in Down's syndrome, derived by alpha- and gamma-secretase cleavage of the amyloid precursorprotein (APP). Amyloid 17-42 can induce neuronal apoptosis via a Fas-like/caspase-8 activation pathway .
[Arg6]-β-Amyloid (1-40), england mutation is a biological active peptide. (Several mutations in the betaamyloid precursor gene cause autosomal dominant Alzheimer's Disease in a number of kindreds. Among them, the English mutation, with His at position 6 replaced with Arg, was reported to accelerate the kinetics of oligomers formation which act as fibril seeds and are more toxic to cultured neuronal cells.)
Mca-SEVNLDAEFK(Dnp) is a Beta-secretase 1 (BACE-1) peptide FRET substrate, containing the 'Swedish' Lys-Met/Asn-Leu mutation of the amyloid precursorprotein (APP) β-secretase cleavage site. Cleavage at -Leu-Asp- of Mca-SEVNLDAEFK(Dnp) liberates the highly fluorescent 7-methoxycoumarin (Mca) fragment from the proximity quenching effect of the 2,4-dinitrophenyl (Dnp) internal quencher resulting in a large and easily detectable increase in fluorescence intensity.
[Asn23]-beta-Amyloid (1-42), iowa mutation is a biological active peptide. (Several mutations in the betaamyloid precursor gene cause autosomal dominant Alzheimer's Disease in a number of kindreds. The Iowa mutation, where Asp 23 is replaced with Asn, is associated with severe cerebral amyloidbeta-protein angiopathy (CAA). The affected individuals share a missense mutation in APP at position 694. The mutated beta-amyloid peptide aggregates more rapidly and forms toxic fibrils.)
[Asn23] β-Amyloid (1-40), Iowa mutation is a biological active peptide. (Several mutations in the betaamyloid precursor gene cause autosomal dominant Alzheimer's Disease in a number of kindreds. The Iowa mutation, where Asp 23 is replaced with Asn, is associated with severe cerebral amyloidbeta-protein angiopathy (CAA). The affected individuals share a missense mutation in APP at position 694. The mutated beta-amyloid peptide aggregates more rapidly and forms toxic fibrils.)
His-D-beta-Nal-Ala-Trp-D-Phe-Lys-NH2 TFA, is a growth hormone releasing peptide, as well as a metabolite of GHRP-1. GHRP-1, or Ala-His-D-beta Nal-Ala-Trp-D-Phe-Lys-NH2, has the effect of promoting the release of growth hormone (GH). GHRP-1 increases GH release and increases [Ca2+]i levels in static monolayer cells of rat pituitary gland, but does not affect cAMP levels .
Scoulerine ((-)-Scoulerine), an isoquinoline alkaloid, is a potent antimitotic compound. Scoulerine is also an inhibitor of BACE1 (ß-site amyloid precursorprotein cleaving enzyme 1). Scoulerine inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells .
Amyloid Precursor Protein, Human (HEK293, Fc) is an Amyloid Precursor (APP) protein with C-Fc. Amyloid Precursor Protein can be used for the study of brain development, learning and memory, synaptic plasticity, and neurodegeneration.
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.
SNCA proteins are critical for synaptic activity and regulate vesicle trafficking and neurotransmitter release. As a monomer, it enhances the vesicle exocytosis process. SNCA Protein, Mouse is the recombinant mouse-derived SNCA protein, expressed by E. coli , with tag free. The total length of SNCA Protein, Mouse is 140 a.a., with molecular weight of ~17.0 kDa.
Alpha-synuclein (SNCA) is a key neuronal protein that regulates synaptic activity, including vesicle transport and neurotransmitter release. As a monomer, it enhances vesicle exocytosis, promotes fusion and fusion pore expansion, and increases local Ca(2+) release. SNCA Protein, Human is the recombinant human-derived SNCA protein, expressed by E. coli , with tag free. The total length of SNCA Protein, Human is 140 a.a., with molecular weight of ~17.0 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.
Alpha-synuclein (SNCA) is a key neuronal protein that regulates synaptic activity, including vesicle transport and neurotransmitter release. As a monomer, it enhances vesicle exocytosis, promotes fusion and fusion pore expansion, and increases local Ca(2+) release. SNCA Protein, Human (His) is the recombinant human-derived SNCA protein, expressed by E. coli , with N-6*His labeled tag. The total length of SNCA Protein, Human (His) is 140 a.a., with molecular weight of ~18.0 kDa.
TML-6-d3 is the deuterium labeled TML-6. TML-6, an orally active curcumin derivative, inhibits the synthesis of the β-amyloid precursorprotein and β-amyloid (Aβ). TML-6 can upregulate Apo E, suppress NF-κB and mTOR, and increase the activity of the anti-
AM-6494 is a potent and orally active BACE1 (efficacious β-site amyloid precursorprotein cleaving enzyme 1) inhibitor (IC50=0.4 nM) with in vivo selectivity over BACE2 (IC50=18.6 nM) . AM-6494 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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