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 |
|---|---|---|---|---|
|
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. |
|
V4442 | PF-06751979 | 1818339-66-0 | PF-06751979 (PF06751979) is a novel, highly potent, brain penetrant, and selective inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) with the potential to be used for the treatment of Alzheimers disease. |
|
V71458 | RE(EDANS)EVNLDAEFK(DABCYL)R | 310427-94-2 | RE(EDANS)EVNLDAEFK(DABCYL)R is a double-labeled peptide of EDANS and DABCYL, which is the fluorescent substrate of BACE1 (Em=360nm, Ex=528nM). |
|
V71462 | SEVNLDAEFR | 186142-28-9 | SEVNLDAEFR is a substrate of BACE1. |
|
V2792 | Verubecestat (MK-8931) | 1286770-55-5 | Verubecestat (formerly known as MK8931; SCH-900931) is a beta-secretase 1 and BACE1 inhibitor that is in Phase 3 clinical trial for treatment of Alzheimer's disease. |
|
V71461 | β-Secretase inhibitor ([Asn670, Sta671, Val672]-Amyloid β Peptide (662-675)) | 350228-37-4 | β-Secretase inhibitor ([Asn670, Sta671, Val672]-Amyloid β Peptide (662-675)) is a β-secretase and BACE1 inhibitor (IC< sub>50 for β-secretase is 25 nM). |
|
V71450 | β-Secretase Inhibitor I | 1818239-19-8 | β-Secretase Inhibitor I is a very potent β-secretase inhibitor that reduces cardiovascular and hepatotoxicity. |
|
V71455 | β-Secretase Inhibitor II | 263563-09-3 | β-Secretase Inhibitor II is a β-Secretase inhibitor. |
|
V71464 | β-Secretase Inhibitor III | 2760674-85-7 | β-Secretase Inhibitor III is a selective BACE1 inhibitor (Ki = 0.13 nM). |
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