β-secretase

gamma-secretase modulator 1 is a modulator of γ secretase and can be used in studies about the treatment of Alzheimer's disease.

BACE-IN-1 is amyloid precursor protein beta-secretase inhibitor

β-Secretase Inhibitor I is a highly potent inhibitor of the β-secretase enzyme. This compound exhibits exceptional inhibitory activity while also demonstrating a significant reduction in cardiovascular and liver toxicity.

gamma-Secretase Modulators serves as a useful treatment for Alzheimer's disease by inhibiting the production of Amyloid-β. Specifically, it acts as a gamma-Secretase Modulators with an IC50 value.

β-Secretase Inhibitor II is a tripeptide aldehyde compound that acts as an inhibitor of β-Secretase. It exhibits a simple structure and has an inhibitory potency of IC50 = 700 nM against total Aβ and IC50 = 2.5 μM specifically against Aβ 1-42. This compound is particularly useful in research related to Alzheimer's disease.

gamma-secretase modulator 5 (compound 22d) is a gamma-secretase modulator (GSMs) that crosses the blood-brain barrier and exhibits an inhibitory effect on the production of the aggregated amyloid β peptide Aβ42 (IC50: 60 nM). gamma-secretase modulator 5 can be used in the study of Alzheimer's disease. The gamma-secretase modulator 5 can be used to study Alzheimer's disease.

β-Secretase Inhibitor IV is a potent, cell-active inhibitor of BACE-1(IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively).

β-Secretase Inhibitor III is a highly selective inhibitor of BACE1 with a Ki value of 0.13 nM.

δ-secretase inhibitor 11 is an inhibitor of δ-secretase and can be used as a lead compound for translational development of AD treatment.

γ-Secretase modulator 12 (Compound 1a) is a selective compound that effectively reduces amyloid-β42 (Aβ42) levels with an IC50 of 0.39 μM. It is specifically designed for Alzheimer's disease research. Notably, γ-Secretase modulator 12 exhibits a favorable brain/plasma ratio (Kp, brain = 0.72) in mice [1].

γ-Secretase modulator 10 is a novel γ-secretase modulator.

γ-Secretase modulator 11 hydrochloride is a potent, orally active γ-secretase modulator (IC50: 0.029 μM). γ-Secretase modulator 11 hydrochloride significantly reduces brain Aβ42 levels and rescues the cognitive deficits exhibited by AD model mice. γ-Secretase modulator 11 hydrochloride has shown research potential in Alzheimer's disease.

5-{8-[(3,4'-Difluoro[1,1'-biphenyl]-4-yl)methoxy]-2-methylimidazo[1,2-a]pyridin-3-yl}-N-methylpyridine-2-carboxamide (1o) exhibited high in vitro potency and brain exposure, was able to cause a significant reduction in brain Aβ42 levels, and had no inhibitory effect on cytochrome p450 enzymes. In addition, compound 1o exhibited excellent anti-cognitive deficits in AD model mice.

γ-Secretase modulator 13 is a γ-secretase modulator (GSMs) that inhibits the production of amyloid β-peptide Aβ42 and can be used to study Alzheimer's disease and tumors.

γ-Secretase-IN-1 is a potent γ-secretase inhibitor that displays partial antiproliferative activity on T-47D cells and inhibits β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage.

γ-Secretase modulator 4 is a potent γ-secretase modulator, reduces the Aβ42 level with IC50s of 0.017 μM and 0.014 μM in mouse and human, respectively.

Gamma-secretase modulator 2 is a potent, selective compound for the treatment of Alzheimer's disease, specifically designed to modulate γ-secretase activity. This modulation selectively attenuates the production of Aβ(1-42), addressing diseases associated with Aβ deposition in the brain, particularly Alzheimer's disease.

gamma-secretase inhibitior-1 is a gamma-secretase modulator that is useful to Alzheimer's disease [1].

gamma-secretase modulator 3 is a gamma-secretase modulator.

DAPT (LY-374973) is a γ-secretase inhibitor that inhibits total Aβ and Aβ42 (IC50=115/200 nM) and is orally active. DAPT is also a Notch inhibitor. DAPT induces cell differentiation, autophagy and apoptosis.

Dihydroergocristine mesylate (DHEC (mesylate))(DHEC mesylate) is the methanesulfonic acid salt of dihydroergocristine. It has been used as the for the symptomatic treatment of mental deterioration associated with cerebrovascular insufficiency and in peripheral vascular disease. Dihydroergocristine 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[1]. It is also a component of ergoloid mesylate (codergocrine mesilate), a mixture of ergot alkaloid derivatives that is used as a vasodilator and has shown mild benefits in the treatment of vascular dementia. It has a role as a vasodilator agent, an alpha-adrenergic antagonist and a geroprotector. It contains a dihydroergocristine.

Phytic acid dipotassium salt is an endogenous metabolite that inhibits β-secretase 1 (BACE1).

SEW06622 is a potent inhibitor of acetylcholinesterase (AChE) and beta-secretase-1 (BACE-1) and is a potential candidate for the treatment of Alzheimer's disease.

JLK6 was a gamma-secretase inhibitor that does not interfere with Notch signalling

Amyloid β-Protein 10-20 acetate (Amyloid β-Protein 10-20 acetate (152286-31-2 free base)) is a fragment of Amyloid-β peptide, maybe used in the research of neurological disease.Amyloid β protein fragment containing the α-secretase processing site (Lys16-Leu17 bond). It also contains the HHQK domain (residues 13-16) responsible for binding to microglial cells.

Sophoflavescenol is a mixed inhibitor of PDE5 with a K(i) value of 0.005 microM. Sophoflavescenol has antioxidant, anti-inflammatory, and apoptotic effects , these effects might contribute to the antitumor activity without severe side effects. Sophoflaves

1. Aloenin (Aloenin A) and aloe-emodin are active principles for inhibition of c-ADH and c-ALDH activities in vitro.

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.

BuChE-IN-8 (compound 19c), a butyrylcholinesterase (BuChE) inhibitor, exhibits an IC50 value of 559 nM and concurrently inhibits human β-secretase (BACE1) and Aβ40 aggregation. It also demonstrates notable antiamnesic properties [1].

Tenuifolin has no inherent toxicity to either the transfected or wild type cells at the effective concentrations, it inhibits amyloid-β secretion in vitro.

AZD3839 free base is a potent and selective BACE1 inhibitor with Ki of 26.1 nM, about 14-fold selectivity over BACE2. Phase 1.

6,9-Dichloro-1,2,3,4-tetrahydroacridine is a synthetic intermediate in the synthesis of tacrine-based acetylcholinesterase (AChE) inhibitors.1It is also an intermediate in the synthesis of multifunctional tacrine hybrids that possess radical scavenging, amyloid-β aggregation inhibitory, and/or β-secretase 1 (BACE1) inhibitory activities in addition to their activity as AChE inhibitors.2,3 1.Recanatini, M., Cavalli, A., Belluti, F., et al.SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors: Synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMFA of tacrine analoguesJ. Med. Chem.43(10)2007-2018(2000) 2.Digiacomo, M., Chen, Z., Wang, S., et al.Synthesis and pharmacological evaluation of multifunctional tacrine derivatives against several disease pathways of ADBioorg. Med. Chem. Lett.25(4)807-810(2015) 3.Li, S.Y., Jiang, N., Xie, S.S., et al.Design, synthesis and evaluation of novel tacrine-rhein hybrids as multifunctional agents for the treatment of Alzheimer's diseaseOrg. Biomol. Chem.12(5)801-814(2014)

Potent and selective β-secretase (BACE) inhibitor (IC50 values are 10.2 and 20.3 nM for human BACE2 and BACE1, respectively). Displays >5,000-fold selectivity for BACE over other proteases including cathepsin D, pepsin and renin. Inhibits Aβ1-40 and Aβ1-42 production in cells expressing mutated APP. Reduces hippocampal and cortical Aβ and sAPPβ levels in an Alzheimer's disease mouse model.

Auraptene is a coumarin derived from citrus plants that bears a geranyloxyl moiety at its C-7. It has anti-inflammatory, anti-carcinogenic, anti-bacterial, neuroprotective, and hepatoprotective activities. It inhibits leukocyte activation and induces phas

1. Epiberberine may be caused drug interactions based on CYP2D6 enzyme. 2. Epiberberine has anti-adipogenic effect is mediated by downregulation of the Raf/MEK1/ERK1/2 and AMPKα/Akt pathways during 3T3-L1 adipocyte differentiation. 3. Epiberberine, as the brightest FSA emitter among the alkaloids, can also serve as an efficient conformation probe for HTG DNA and discriminate the DNA G-quadruplex from the RNA counterpart.

Verubecestat (MK-8931) (MK-8931) is an effective and specific β-secretase inhibitor and β-site APP-cleaving enzyme 1 inhibitor or BACE1 protein inhibitor.

Leucyl-phenylalanine amide is an intermediate in the synthesis of γ-Secretase Inhibitor, the enzyme complex that catalyzes the cleavage of the amyloid precursor protein (APP) to produce amyloid β-peptide (Aβ) which is the major causative agent in Alzheime

M-2420 is a fluorogenic substrate designed specifically for the β-secretase site found in the Swedish mutation of the amyloid precursor protein (APP).

LY2886721, a BACE inhibitor, is used for the therapy of Alzheimer's Disease.

Semagacestat (LY450139) (LY450139) is a γ-secretase blocker for Aβ42/Aβ40/Aβ38 (IC50: 10.9/12.1/12.0 nM) and also inhibits Notch signaling (IC50: 14.1 nM).

COX-2-IN-22 is a COX-2 inhibitor (IC50: 8.6 μM) that can cross the blood-brain barrier and also exhibits inhibitory effects on AChE (IC50: 2.8 μM), BChE (IC50: 6.3 μM), β-Secretase (IC50: 15.3 μM), LOX-5 (IC50: 13.9 μM) and DPPH ( IC50: 6.8 μM) showed inhibitory effects.

Epiberberine chloride, a natural pro-berberine from Coptis chinensis Franch. is an AChE, BChE, and BACE1 inhibitor with IC50 values of 1.07, 6.03, and 8.55 μM, respectively.Epiberberine chloride has antioxidant effects and inhibits the effects of Ca9-22 and Fa2R. Epiberberine chloride has antioxidant effects, inhibits the motility of Ca9-22 and FaDu cell lines, and can be used to study hyperlipidemia, Alzheimer's disease and diabetes.

Eslicarbazepine Acetate (Zebinix) is an anticonvulsant medication approved for use in Europe, the United States and Canada as an adjunctive therapy for partial-onset seizures that are not adequately controlled with conventional therapy.

Umibecestat is an inhibitor of beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1), 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.

Multitarget AD inhibitor-1 is a reversible and selective inhibitor of butyrylcholinesterase (BuChE) with IC50 values of 7.22 μM and 1.55 μM for human BuChE (hBuChE) and equine serum BuChE (eqBuChE), respectively. Additionally, it exhibits inhibitory activity towards β-secretase (IC50 value of 41.60 μM), amyloid β aggregation (IC50 value of 3.09 μM), and tau aggregation. As a diphenylpropylamine derivative, Multitarget AD inhibitor-1 holds promise for research pertaining to the multifunctional, disease-modifying treatment of Alzheimer's disease.

Elenbecestat (E2609) is an effective oral bioutilization and CNS penetrating ACE-1 inhibitor for the treatment of Alzheimer's disease.

PF-06663195 is a potent inhibitor of β-site amyloid precursor protein (APP) Cleaving Enzyme 1 (BACE1, β-Secretase 1).

E2012 is a γ-secretase modulator (GSM). E2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat.

Aftin-4, an amyloid forty-two inducer, activates γ-secretase, promoting the generation of amyloid-β-1-42 (Aβ1-42) from amyloid-β protein precursor. Aftin-4(Aftin4) increased Aβ-1-42, but not Aβ-1-40 in mouse hipppocampus, accompanied by learning deficits and mitochondrial ultrastructural changes similar to those found in the brains of patients with AD. Aftin-4(Aftin4) can thus be used to induce a rapid, acute Alzheimer's disease-like toxicity in the rodent brain.

Imidazoleacetic acid hydrochloride (I4AA) is an imidazole derivative with potential antituberculosis properties. It also used in the preparation of acyl guanidine inhibitors of β-secretase.