bace-1

BACE-1 inhibitor 1 (Compound 8a) is a potent BACE-1 inhibitor with an IC50 of 56 nM.

AChE BChE BACE-1-IN-2 (Compound 4o) is an orally active AChE, BACE-1, and BChE inhibitor with IC50 values of 0.069, 0.097, and 0.127 μM against hAChE, hBACE-1, and hBChE, respectively. It exhibits remarkable antioxidant potential, considerable binding capability towards PAS-AChE, potential disassembly of Aβ aggregates, and neuroprotective activity against Aβ-induced stress with excellent brain permeation [1].

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].

BACE-1 Inhibitor 2 is a potent, CNS-permeable inhibitor of BACE-1, exhibiting an IC50 value of 1.5 nM in enzymatic assays [1].

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.

BACE-IN-1 is an imidazo[1,2-a]pyridine derivative that inhibits the β-site amyloid precursor protein cleavage enzyme (BACE) sentence.BACE-IN-1 has the potential to investigate diseases involving BACE, such as Alzheimer's disease.

Compound AK-2, also known as hAChE hBACE-1-IN-4, is a quinazoline derivative that demonstrates significant inhibitory activity against the enzymes hAChE and hBACE-1 (hAChE, IC 50 = 0.283 μM; hBACE-1, IC 50 = 0.231 μM). This compound also shows potential in inhibiting Aβ aggregation and possesses characteristics such as non-neurotoxicity, blood-brain barrier permeability, and oral activity, making it a valuable agent for research in Alzheimer's disease [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

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

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

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

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].

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

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.

β-Secretase Inhibitor IV is a potent, cell-active inhibitor of BACE-1, with IC50 values of 15.6 nM and 16.3 nM at BACE-1 concentrations of 2 nM and 100 pM, respectively.

AChE-IN-82 (compound 49) is an acetylcholinesterase (AChE) inhibitor. It inhibits eeAChE, eqBChE, hMAO-A, hMAO-B, and BACE-1 with IC50 values of 0.072, 9.81, 14.52, 0.024, and 2.42 μM, respectively. Additionally, AChE-IN-82 inhibits COX-1, COX-2, and 5-LOX with IC50 values of 60.41, 0.187, and 0.18 μM, respectively. The compound also demonstrates strong neuroprotective effects by significantly reducing H2O2-induced oxidative stress.

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

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

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

CB1 2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand with Ki values of 3.5 nM and 1.2 nM, respectively. It acts as a full agonist of CB1 and a competitive inverse agonist of CB2. BACE-IN-1 shares these properties, being a complete agonist of CB1 and a competitive inverse agonist of CB2.

NB-216 is a macrocyclic peptidic BACE-1 inhibitor.

NB-533 is a macrocyclic peptidic BACE-1 inhibitor.