bace1 in 1

BACE1-IN-1 is a high brain penetrant BACE1 inhibitor (IC50s: 32 and 47 nM for human BACE1 and BACE2).

BACE1/2-IN-1 (compound 34) is an effective BACE1 and BACE2 inhibitor with IC50 values of 0.01 and 0.0053 μM, respectively. It exhibits a lower Pgp efflux ratio, improved passive permeability, and decreased metabolic stability in liver microsomes.

AChE/BACE1/GSK3β-IN-1 is an orally active, blood-brain barrier-permeable, moderately bioavailable triple inhibitor of AChE, BACE1, and GSK3β, utilized for Alzheimer's disease (AD) research.

Anti-BACE1 Antibody is a humanized monoclonal antibody targeting beta-site amyloid precursor protein cleaving enzyme 1 (BACE1). BACE1 is a transmembrane aspartic protease and the rate-limiting enzyme for the generation of Aβ peptides in Alzheimer's disease (AD). This antibody functions by specifically binding to the extracellular domain of BACE1, neutralizing its enzymatic activity or inducing receptor internalization to block the beta-site cleavage of amyloid precursor protein (APP). This process effectively reduces the production of toxic Aβ40/42 and inhibits the formation and deposition of amyloid plaques, making it a pivotal tool for researching the pathogenesis and immunotherapeutic strategies of neurodegenerative diseases.

BACE1-IN-15 (Compound 72) is a selective β-secretase 1 (BACE-1) inhibitor with oral bioavailability and blood-brain barrier permeability, exhibiting an IC50 value of 121.65 nM, and an IC50 of 480.92 nM for BACE-2. BACE1-IN-15 is applicable for research in the field of Alzheimer's disease.

BACE1-IN-10 is a potent inhibitor of BACE1, demonstrating sub-micromolar activity against recombinant BACE1 (rBACE1) [1].

BACE1-IN-13 (Compound 36), an orally active inhibitor of BACE1, exhibits high potency with an IC50 of 2.9 nM and demonstrates greater efficacy in hAβ42 cells (IC50 = 1.3 nM). It is considered safe for the cardiovascular system and induces a sustained reduction of Aβ42 in both mouse and dog animal models [1].

hAChE/hBACE-1-IN-1 (compounds 5d) is an orally active inhibitor of hAChE that can cross the blood-brain barrier. It effectively inhibits hAChE and hBACE-1, with IC50 values of 0.076 and 0.23 μM, respectively. Additionally, hAChE/hBACE-1-IN-1 prevents Aβ1-42 aggregation and enhances learning and memory in mice. This compound is useful in Alzheimer's disease research.

BACE1-IN-14 (compound 27f) is a BACE1 inhibitor with an EC50 value of 0.7 μM, and it exhibits an EC50 value of 1.6 μM against BACE2. BACE1-IN-14 is applicable in Alzheimer's disease (AD) research.

AChE/BChE/BACE-1-IN-1 (Compound 4k) is an orally active inhibitor that targets acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein cleaving enzyme 1 (BACE-1), with IC50 values of 0.058 μM, 0.082 μM, and 0.115 μM against hAChE, hBChE, and hBACE-1, respectively. It exhibits significant binding affinity with PAS-AChE, excellent blood-brain barrier permeability, potential disassembly of amyloid-beta (Aβ) aggregates, neuroprotective properties against Aβ-induced stress, and remarkable antioxidant capabilities [1].

BACE1-IN-12 is a potent BACE1 inhibitor (IC50: 8.9 μM) that can cross the blood-brain barrier. BACE1-IN-12 selectively inhibits BuChE (butylcholinesterase) activity (IC50: 3.2 μM). BACE1-IN-12 has potential for anti-Alzheimer's disease studies.

Atabecestat (JNJ-54861911) is a potent, brain-penetrant, and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor that achieves robust and high CSF Aβ reduction, is well-tolerated, and displays sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat (JNJ-54861911) has the potential for Alzheimer's Disease treatment[1].

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

(1α,1'S,4β)-Lanabecestat is a Beta site APP Cleaving Enzyme 1 (BACE1) inhibitor with IC50 values of 2.2 nM in the TR-FRET assay and 0.28 nM in the sAPPp release assay.

BACE1-IN-2 is a BACE1 inhibitor (IC50: 22 nM).

BACE1-IN-4 is a potent and highly selective BACE1 inhibitor (IC50: 3.8 nM; Ki: 1.9 nM), exhibiting greater selectivity for BACE1 over BACE2.

BACE1-IN-5 (Compound 15), a potent β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, demonstrates significant efficacy with an IC50 of 9.1 nM for BACE1 inhibition and an impressive IC50 of 0.82 nM against cellular amyloid-β (Aβ) production. Additionally, it is engineered to enhance hERG inhibition and P-gp efflux, indicating its optimized medicinal chemistry profile [1].

PF-06751979 is an inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) (IC50 of 7.3 nM in BACE1 binding assay).

BACE-IN-1 acetate (BACE-IN-1 acetate (350228-37-4,Free base)) has been used as β-site amyloid precursor protein (APP) cleaving enzyme-1 (BACE1) inhibitor in BACE1 inhibitor assay. β-Site amyloid precursor protein (APP) cleaving enzyme-1 (BACE1), an aspartic protease belongs to the protease family of enzymes comprises of six luminal cysteine residues. These residues help in the formation of three intermolecular disulfide bonds and N-linked glycosylation sites.

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)

BACE1-IN-6 is a BACE1 inhibitor with an IC50 value of 1.5 nM.

AChE-IN-11 (compound 5C) is a multifunctional agent used in Alzheimer's disease research, exhibiting neuroprotective and antioxidant activity (ORAC = 2.5 eq). It has IC50 values of 7.9 μM, 9.9 μM, and 8.3 μM against AChE, MAO-B, and BACE1, respectively. AChE-IN-11 demonstrates mixed-type AChE inhibition by binding to both the CAS and PAS of AChE and acts as a selective metal ions chelator [1].

BACE1-IN-8 is a potent inhibitor of BACE1 (β-site APP lyase 1) (IC50: 3.9 μM).

Verubecestat tosylate, also known as MK-8931 or SCH 900931, is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor. Verubecestat tosylate is a promising novel therapeutic drug candidate in Alzheimer's disease. Verubecestat tosylate reduced Aβ cerebral spinal fluids (CSF) levels up to 92% and was well tolerated by patients.