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BACE1/2-IN-1 (compound 34) is a potent BACE1 and BACE2 inhibitor, with an IC50 of 0.01 and 0.0053 μM, respectively. BACE1/2-IN-1 shows a combination of lower Pgp efflux ratio and improved passive permeability. BACE1/2-IN-1 displays reduced liver microsomal metabolic stability .
BACE1-IN-11 is a BACE1 inhibitor. BACE1-IN-11 has the BACE1 inhibitory activity with an IC50 value of 72 μM. BACE1-IN-11 can be used for the research of Alzheimer’s disease (AD) .
BACE1-IN-14 (compound 27f) is a BACE1 inhibitor, with the EC50 values of 0.7 μM and 1.6 μM for BACE1 and BACE2. BACE1-IN-14 is can be used in Alzheimer's disease (AD) research .
BACE1-IN-12 (compound 7g) is a potent and BBB-penetrated BACE1 inhibitor, with an IC50 of 8.9 µM. BACE1-IN-12 shows selective BuChE (butyrylcholinesterase) inhibitory activity with an IC50 of 3.2 µM. BACE1-IN-12 shows effective antioxidant effect with an IC50 of 10.2 μM (DPPH). BACE1-IN-12 might be served as a potential anti-Alzheimer agent .
BACE1-IN-4 is a potent and highly selective BACE1 inhibitor, with an IC50 of 3.8 nM and a Ki of 1.9 nM, more selective at BACE1 over BACE2. Anti-Alzheimer’s disease .
BACE1-IN-13 (Compound 36) is an orally active BACE1 inhibitor with an IC50 value of 2.9 nM. BACE1-IN-13 is highly potent in hAβ42 cell (IC50 = 1.3 nM). BACE1-IN-13 has cardiovascularly safty and elicits sustained Aβ42 reduction in mouse and dog animal models .
BACE2-IN-1 (compound 3l) is a highly selective BACE2 inhibitor with a K i value of 1.6 nM. BACE2 inhibitors can be used to research of Type 2 Diabetes .
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 .
BACE-IN-1 (Compound 13) is a substituted lmidazo[1 ,2-a]pyridine derivative which can inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease.
BACE1 Human Pre-designed siRNA Set A contains three designed siRNAs for BACE1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Bace1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Bace1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Bace1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Bace1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
BACE2 Human Pre-designed siRNA Set A contains three designed siRNAs for BACE2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Bace2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Bace2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Bace2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Bace2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
AChE/BChE/BACE-1-IN-2 (Compound 4o) is an orally active inhibitor of AChE, BChE, and BACE-1 with IC50 values of 0.069, 0.127 and 0.097 μM against hAChE, hBChE and hBACE-1, respectively. AChE/BChE/BACE-1-IN-2 shows considerable PAS-AChE binding capability, excellent brain permeation, potential disassembly of Aβ aggregates, and neuroprotective activity against Aβ-induced stress. AChE/BChE/BACE-1-IN-2 has remarkable antioxidant potential .
AChE/BChE/BACE-1-IN-1 (Compound 4k) is an orally active inhibitor of AChE, BChE, and BACE-1 with IC50 values of 0.058, 0.082 and 0.115 μM against hAChE, hBChE and hBACE-1, respectively. AChE/BChE/BACE-1-IN-1 shows considerable PAS-AChE binding capability, excellent brain permeation, potential disassembly of Aβ aggregates, and neuroprotective activity against Aβ-induced stress. AChE/BChE/BACE-1-IN-1 has remarkable antioxidant potential .
AChE/BACE1/GSK3β-IN-1 is an orally active triple inhibitor of AChE/BACE1/GSK3β. AChE/BACE1/GSK3β-IN-1 has effective inhibitory activity against AChE, BACE1 and GSK3β with IC50 values of 1.0 μM, 20 μM and 15 μM, respectively. AChE/BACE1/GSK3β-IN-1 has good blood-brain barrier penetrability, suitable bioavailability. AChE/BACE1/GSK3β-IN-1 can be used for the research of Alzheimer's disease (AD) .
Umibecestat (CNP520) is a beta-site amyloid precursor protein 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.
β-Secretase Inhibitor IV is a potent, cell-active BACE-1 inhibitor with IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively.
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 .
AMG-8718 is a potent, selective and orally active BACE1 inhibitor with IC50 values of 0.0007, 0.005 µM for BACE1 and BACE2, respectively. AMG-8718 significantly decreases Aβ40 levels in the CSF and brain .
Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor. Elenbecestat has the potential for Alzheimer's disease (AD) research .
RE (EDANS) EVNLDAEFK (DABCYL) R is an EDANS and DABCYL double-labeled peptide,serves as a fluorescent substrate for BACE1(Em=360nm,Ex=528nm). RE (EDANS) EVNLDAEFK (DABCYL) R can be used for BACE1 activity measurement and the enzyme activity level is directly proportional to the fluorescence reaction .
PF-06751979 is a potent, brain penetrant, β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 7.3 nM in BACE1 binding assay.
LY2811376 is the first orally available non-peptidic β-secretase (BACE1) inhibitor with IC50 of 239 nM-249 nM, that acts to decrease Aβ secretion with EC50 of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.
Verubecestat (MK-8931) is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat effectively reduces Aβ40 and has the potential for Alzheimer's Disease .
LY2886721 is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1. 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 .
LY2886721 hydrochloride is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1. 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 .
Verubecestat (MK-8931) TFA is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat TFA effectively reduces Aβ40 and has the potential for Alzheimer's Disease .
Cbz-Gly-Pro-Ala-O-cinnamyl (compound 25) is a small peptide targeting BACE-1 and AChE with the IC50 values of 0.02 μM and 1 μM, respectively. Cbz-Gly-Pro-Ala-O-cinnamyl shows neuroprotective effect and can be used for study of Alzheimer’s disease .
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 .
Memoquin is an anti-amyloid and anti-oxidant multi-target-directed ligand. Memoquin is an orally active inhibitor of BACE-1 and AChE with IC50 values of 108 and 1.55 nM, respectively. Memoquin is a cognitive enhancer that prevents the Aβ-induced neurotoxicity mediated by oxidative stress. Memoquin can be used for the research of Alzheimer’s disease (AD) .
Mca-SEVNLDAEFK(Dnp)-NH2 contains a highly fluorescent 7-methoxycoumarin group that is efficiently quenched by resonance energy transfer to the 2,4-dinitrophenyl group. It can be used to measure the activities of peptidases that are capable of cleaving an amide bond between the fluorescent group and the quencher group, causing an increase in fluorescence, such as can be used to measure the activity of BACE-1 .
Lanabecestat (AZD3293) is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM. Lanabecestat is used for the research of Alzheimer's disease .
AM-6494 is a potent and orally active BACE1 (efficacious β-site amyloid precursor protein 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.
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 .
Mca-SEVNLDAEFK(Dnp) is a Beta-secretase 1 (BACE-1) peptide FRET substrate, containing the 'Swedish' Lys-Met/Asn-Leu mutation of the amyloid precursor protein (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.
Aloveroside A is a triglucosylnaphthalene derivative isolated from ethanolic extract of aloe vera. Aloveroside A has weak bACE inhibitory activity (inhibition rate at a dose of 100 μg/mL is approximately 18.68%) .
AZD3839 free base is a potent and selective orally active, brain-permeable BACE1 inhibitor (Ki=26 nM). AZD3839 free base shows 14 and >1000-fold selectivity against BACE2 and cathepsin D, respectively. AZD3839 free base exhibits dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate. AZD3839 free base can be used for the research of Alzheimer's disease .
hAChE-IN-3 (compounds 5c) is a potent and blood-brain barrier permeable AChE, BuChE, MAO-B-IN-1 and BACE-1 inhibitor, with IC50 values of 0.44, 0.08, 5.15 and 0.38 μM, respectively. hAChE-IN-3 has antioxidant activity and metal chelating ability. In addition, hAChE-IN-3 can bind to peripheral anion sites, and affect β amyloid and reduce Alzheimer's-associated neurodegeneration. hAChE-IN-3 has the potential for the research of Alzheimer's disease .
hAChE-IN-7 (compound 5s) is a mixed inhibitor affecting both the catalytic active site (CAS) and peripheral anionic site (PAS) of hAChE. hAChE-IN-7 displays the balanced inhibitory effect on hAChE (IC50=69.8 nM) and hBuChE (IC50=68.0 nM), and exhibits inhibitory activity against β-secretase-1 (BACE-1) (IC50=3.6 μM). hAChE-IN-7 has the potential for Alzheimer's disease (AD) research .
Scoulerine ((-)-Scoulerine), an isoquinoline alkaloid, is a potent antimitotic compound. Scoulerine is also an inhibitor of BACE1 (ß-site amyloid precursor protein cleaving enzyme 1). Scoulerine inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells .
Kushenol C, isolated from the roots of Sophora flavescens, shows anti-Inflammatory and anti-oxidative stress activities. Kushenol C inhibits BACE1 (β-site APP cleaving enzyme 1) with an IC50 of 5.45 µM .
Aloenin (Aloenin A) is a kind of natural product, has effective clearing and free radical activity, and has moderate inhibitory activity on β-secretion (BACE) (IC50=14.95 μg/mL). Aloenin suppresses peritoneal hypertrophy in large rats and suppresses its release.
BuChE-IN-8 (compound 19c) is a butyrylcholinesterase (BuChE) inhibitor with an IC50 of 559 nM. BuChE-IN-8 possesses human β-secretase (BACE1) and Aβ40 aggregation inhibitory activities. BuChE-IN-8 has significant antiamnesic properties .
LX2343 is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K inhibitor with an IC50 of 15.99±3.23 μM. LX2343 stimulates autophagy in its promotion of Aβ clearance.
OM99-2, an eight residue peptidomimetic, tight-binding inhibitor of human brain memapsin 2 with a Ki value of 9.58 nM . OM99-2 is significantly advanced the development of BACE1 inhibitor . OM99-2 has the potential for the research of the 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 .
OM99-2 TFA, an eight residue peptidomimetic, tight-binding inhibitor of human brain memapsin 2 with a Ki value of 9.58 nM . OM99-2 TFA is significantly advanced the development of BACE1 inhibitor . OM99-2 has the potential for the research of the Alzheimer's disease .
BuChE-IN-9 (compound 22a) is a potent equine serum-derived BuChE (eqBuChE) inhibitor with an IC50 of 173 nM. BuChE-IN-9 also inhibits human BACE1, Aβ aggregation, mouse GABA transporter 1 (mGAT1) and mGAT4. BuChE-IN-9 has significant antiamnesic properties .
(1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) a less active enantiomer of Lanabecestat. Lanabecestat is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM .
Deoxyneocryptotanshinone, a natural tanshinone, is a high affinity BACE1 (Beta-secretase) inhibitor with an IC50 value of 11.53 μM. Deoxyneocryptotanshinone shows a promising dose-dependent inhibition of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 133.5 μM. Deoxyneocryptotanshinone can be used for Alzheimer's disease research .
TAK-070 Free base is a noncompetitive and orally active BACE1 inhibitor (IC50: 3.15 μM). TAK-070 Free base can be used for research of Alzheimer’s disease (AD). TAK-070 Free base inhibits brain levels of soluble Aβ, and improves cognitive impairments in AD model .
Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein 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 .
(Rac)-AZD3839 is an orally active beta-amyloid precursor protein 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 .
Sophoflavescenol is a prenylated flavonol, which shows great inhibitory activity with IC50 of 0.013 μM against Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE with IC50s of 0.30 µM, 0.17 µM, 17.89 µg/mL, 10.98 µM, 8.37 µM and 8.21 µM, respectively.
AChE-IN-11 (compound 5C) is a triple inhibitor targeting AChE/MAO-B/BACE1 (IC50=7.9 μM, 9.9 μM, 8.3 μM, respectively) and a selective metal ion chelators. AChE-IN-11 exhibits mixed AChE inhibitory effects, binding to both CAS and PAS of AChE. AChE-IN-11 also exhibits good antioxidant activity (ORAC=2.5 eq) and potential neuroprotective effects in Alzheimer's disease .
PD07 is an orally active AChE inhibitor (IC50: 0.29 μM for hAChE). PD07 also inhibits ChEs, BACE1 (IC50: 13.42 μM), and Aβ1–42 aggregation in in vitro. PD07 is an antioxidant, and shows DPPH inhibitory activity (IC50: 26.46 μM). PD07 improves memory and cognition in Scopolamine (HY-N0296)-induced amnesia rats. PD07 can be used for research of Alzheimer’s disease .
Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and can be used for the research of Alzheimer disease . Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberinecan be used for the research of diabetic disease .
Epiberberine chloride is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine chloride has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and may protect against Alzheimer disease . Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberine has the potential effect in the research of diabetic disease .
BACE1 (485-501) is the carboxyl terminal of BACE1 (Beta-site APP cleaving enzyme 1). BACE1 (485-501) can be used as antigen to produce anti-BACE1-C antibody .
RE (EDANS) EVNLDAEFK (DABCYL) R is an EDANS and DABCYL double-labeled peptide,serves as a fluorescent substrate for BACE1(Em=360nm,Ex=528nm). RE (EDANS) EVNLDAEFK (DABCYL) R can be used for BACE1 activity measurement and the enzyme activity level is directly proportional to the fluorescence reaction .
Mca-SEVNLDAEFK(Dnp)-NH2 contains a highly fluorescent 7-methoxycoumarin group that is efficiently quenched by resonance energy transfer to the 2,4-dinitrophenyl group. It can be used to measure the activities of peptidases that are capable of cleaving an amide bond between the fluorescent group and the quencher group, causing an increase in fluorescence, such as can be used to measure the activity of BACE-1 .
Mca-SEVNLDAEFK(Dnp) is a Beta-secretase 1 (BACE-1) peptide FRET substrate, containing the 'Swedish' Lys-Met/Asn-Leu mutation of the amyloid precursor protein (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.
OM99-2, an eight residue peptidomimetic, tight-binding inhibitor of human brain memapsin 2 with a Ki value of 9.58 nM . OM99-2 is significantly advanced the development of BACE1 inhibitor . OM99-2 has the potential for the research of the Alzheimer's disease .
OM99-2 TFA, an eight residue peptidomimetic, tight-binding inhibitor of human brain memapsin 2 with a Ki value of 9.58 nM . OM99-2 TFA is significantly advanced the development of BACE1 inhibitor . OM99-2 has the potential for the research of the Alzheimer's disease .
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 .
Scoulerine ((-)-Scoulerine), an isoquinoline alkaloid, is a potent antimitotic compound. Scoulerine is also an inhibitor of BACE1 (ß-site amyloid precursor protein cleaving enzyme 1). Scoulerine inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells .
Aloveroside A is a triglucosylnaphthalene derivative isolated from ethanolic extract of aloe vera. Aloveroside A has weak bACE inhibitory activity (inhibition rate at a dose of 100 μg/mL is approximately 18.68%) .
Kushenol C, isolated from the roots of Sophora flavescens, shows anti-Inflammatory and anti-oxidative stress activities. Kushenol C inhibits BACE1 (β-site APP cleaving enzyme 1) with an IC50 of 5.45 µM .
Aloenin (Aloenin A) is a kind of natural product, has effective clearing and free radical activity, and has moderate inhibitory activity on β-secretion (BACE) (IC50=14.95 μg/mL). Aloenin suppresses peritoneal hypertrophy in large rats and suppresses its release.
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 .
Deoxyneocryptotanshinone, a natural tanshinone, is a high affinity BACE1 (Beta-secretase) inhibitor with an IC50 value of 11.53 μM. Deoxyneocryptotanshinone shows a promising dose-dependent inhibition of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 133.5 μM. Deoxyneocryptotanshinone can be used for Alzheimer's disease research .
Sophoflavescenol is a prenylated flavonol, which shows great inhibitory activity with IC50 of 0.013 μM against Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE with IC50s of 0.30 µM, 0.17 µM, 17.89 µg/mL, 10.98 µM, 8.37 µM and 8.21 µM, respectively.
Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and can be used for the research of Alzheimer disease . Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberinecan be used for the research of diabetic disease .
Epiberberine chloride is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine chloride has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and may protect against Alzheimer disease . Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberine has the potential effect in the research of diabetic disease .
The BACE1 protein is an important member of the aspartic protease family and is critical in Alzheimer's disease pathology. Alternative splicing generates multiple transcript variants, at least one of which encodes a preproprotein that is proteolytically processed to produce the mature protease. BACE1 Protein, Human (HEK293) is the recombinant human-derived BACE1 protein, expressed by HEK293 , with tag free. The total length of BACE1 Protein, Human (HEK293) is 436 a.a., with molecular weight of ~65 kDa.
BACE1 protein is an important member of the peptidase A1 family and is involved in the pathogenesis of Alzheimer's disease. They produce mature proteases through proteolytic processing of preprotein, which catalyze the initial steps in the formation of amyloid beta peptide from the amyloid precursor protein. BACE1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived BACE1 protein, expressed by HEK293 , with C-His labeled tag. The total length of BACE1 Protein, Mouse (HEK293, His) is 436 a.a., with molecular weight of 60-76 kDa.
BACE1 protein is crucial in proteolytic processing of amyloid precursor protein (APP), initiating cleavage at the N-terminus of the A-beta peptide sequence. This process results in the extracellular release of beta-cleaved soluble APP and a cell-associated C-terminal fragment. BACE1's cleavage activity extends to CHL1, demonstrating its versatility in substrate processing. BACE1 Protein, Human (HEK293, N-His) is the recombinant human-derived BACE1 protein, expressed by HEK293 , with N-6*His labeled tag. The total length of BACE1 Protein, Human (HEK293, N-His) is 436 a.a., with molecular weight of 56-85 kDa.
The BACE1 protein is an important member of the aspartic protease family and is critical in Alzheimer's disease pathology. Alternative splicing generates multiple transcript variants, at least one of which encodes a preproprotein that is proteolytically processed to produce the mature protease. BACE1 Protein, Human (HEK293, His) is the recombinant human-derived BACE1 protein, expressed by HEK293 , with C-10*His labeled tag. The total length of BACE1 Protein, Human (HEK293, His) is 436 a.a., with molecular weight of 60-65 kDa.
BACE1 protein is crucial in proteolytic processing of amyloid precursor protein (APP), initiating cleavage at the N-terminus of the A-beta peptide sequence. This process results in the extracellular release of beta-cleaved soluble APP and a cell-associated C-terminal fragment. BACE1's cleavage activity extends to CHL1, demonstrating its versatility in substrate processing. BACE-1 Protein, Human (HEK293, Fc) is the recombinant human-derived BACE-1 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of BACE-1 Protein, Human (HEK293, Fc) is 436 a.a., with molecular weight of 85-100 kDa.
The BACE2 protein is critically involved in the proteolytic processing of amyloid precursor protein (APP), producing beta-cleaved soluble APP and a cell-associated C-terminal fragment. It cleaves APP at residues 690-691 and 671-672. BACE2 Protein, Mouse (HEK293, His) is the recombinant mouse-derived BACE2 protein, expressed by HEK293 , with C-His labeled tag. The total length of BACE2 Protein, Mouse (HEK293, His) is 443 a.a., with molecular weight of ~55 kDa.
AM-6494 is a potent and orally active BACE1 (efficacious β-site amyloid precursor protein 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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