Amyloid precursor protein (APP) is broken down by beta-secretase (BACE), a transmembrane aspartic proteinase, to produce the soluble ectodomain (sAPPbeta) and its C-terminal fragment (CTFbeta). Therapeutics for Alzheimer's disease (AD) frequently target BACE. The enzyme comes in two different varieties: BACE1 and BACE2.
The hallmark neuropathology of Alzheimer's disease (AD) is the deposition of amyloid-protein (A) to produce neuritic plaques. By cleavages caused by - and -secretases, A is produced from APP. The -secretase BACE1 causes severe side effects when inhibited, whereas BACE2 suppresses A normally by cleaving APP/A at the -site (Phe20) in the A domain.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V71466 | (1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293; (1α,1'S,4β)-LY3314814) | 1384082-96-5 | (1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) is a less active isomer of Lanabecestat. |
|
V71467 | AM-6494 | 1874232-80-0 | AM-6494 is a potent, oral beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor (IC50=0.4 nM) with in vivo selectivity over BACE2 (IC50=18.6 nM). |
|
V71451 | BACE-1 inhibitor 2 | 2563970-92-1 | BACE-1 inhibitor 2 is a potent, BBB (blood-brain barrier) permeable/penetrable BACE-1 inhibitor (antagonist) with IC50 of 1.5 nM. |
|
V71468 | BACE1-IN-10 | 2799658-44-7 | BACE1-IN-10 is a potent BACE1 inhibitor. |
|
V71449 | BACE1-IN-13 | 1397683-26-9 | BACE1-IN-13 (Compound 36) is an orally bioactive BACE1 inhibitor (antagonist) with IC50 of 2.9 nM. |
|
V87781 | BACE1-IN-14 | BACE1-IN-14 (compound 27f) is a BACE1 inhibitor with an EC50 of 0.7 μM. | |
|
V71463 | BACE1-IN-5 | 2581114-83-0 | BACE1-IN-5 (Compound 15) is a BACE1 inhibitor (antagonist) with IC50 of 9.1 nM and also inhibits cellular Aβ with IC50 of 0.82 nM. |
|
V71459 | BACE1-IN-6 | 2079945-75-6 | BACE1-IN-6 is a BACE1 inhibitor (antagonist) with IC50 of 1.5 nM. |
|
V71465 | BACE1-IN-9 | 2872604-91-4 | BACE1-IN-9 (compound 82b) is a potent BACE1 (beta APP lyase 1) inhibitor (antagonist) with IC50 of 1.2 µM. |
|
V71454 | Cassiaside | 13709-03-0 | Cassiaside is a naphthyl glycoside that displays mixed inhibitory effects on BACE1 (IC50= 4.45 μM; Ki=9.85 μM). |
|
V71446 | Elenbecestat (E2609) | 1388651-30-6 | Elenbecestat (E2609) is a potent, orally bioactive, CNS-penetrating BACE-1 inhibitor. |
|
V71460 | GL189 | 552337-94-7 | GL189 is a beta-secretase inhibitor. |
|
V71452 | JNJ-67569762 | 2380313-26-6 | JNJ-67569762 is a selective BACE1 inhibitor targeting S3 (IC50 = 2.7 nM). |
|
V71457 | Kushenol C | 99119-73-0 | Kushenol C is extracted from Sophora flavescens root and has anti-inflammatory and antioxidant properties. |
|
V3023 | LX2343 | 333745-53-2 | LX2343, discovered by high throughout screening, is a small molecule compound that can effectively reverse the streptozocin (STZ)-induced neuronal apoptosis and tau hyperphosphorylation in vitro and in vivo. |
|
V1313 | LY2811376 | 1194044-20-6 | LY2811376 (LY-2811376; LY 2811376) is a novel, potent, selective and the first orally bioavailable non-peptidic β-secretase (BACE1) inhibitor with the potential for the treatment of Alzheimers Disease (AD). |
|
V71447 | LY2886721 hydrochloride | 1262036-49-6 | LY2886721 HCl is a specific, orally bioactive beta-amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor (antagonist) with IC50 of 20.3 nM against recombinant human BACE1. |
|
V71448 | Mca-SEVNLDAEFK(Dnp) | 1802078-31-4 | 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) beta-secretase cleavage site . |
|
V71403 | Multitarget AD inhibitor-1 | 2205015-77-4 | Multitarget AD inhibitor-1 is a selective and reversible inhibitor of butyrylcholinesterase (BuChE) with IC50s of 7.22 μM and 1.55 μM for human and equine serum hBuChE, respectively. |
|
V71453 | OM99-2 TFA | 2504147-81-1 | OM99-2 TFA, an eight-residue peptidomimetic, is a tight-binding inhibitor of human brain memapsin 2 with a Ki of 9.58 nM. |
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