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. |
|
V108412 | 2,2′,4,4′-Tetrahydroxychalcone | 123702-96-5 | 2,2′,4,4′-Tetrahydroxychalcone (compound 18) is a highly selective and active BACE1 inhibitor with an IC50 value of 0.62 μM. |
|
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). |
|
V115402 | AZD3839 fumarate | 1421852-78-9 | AZD3839 fumarate is an orally effective, selective, reversible inhibitor of β-amyloid precursor protein lyase BACE1 that can cross the blood-brain barrier. |
|
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. |
|
V117352 | BACE-1/Mpro-IN-1 | BACE-1/Mpro-IN-1 is a dual inhibitor that can simultaneously inhibit BACE-1 (IC50 = 0.26 μM) and SARS-CoV-2 Mpro (IC50 = 0.91 μM) and can easily cross the blood-brain barrier. | |
|
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). |
|
V115512 | CTS-21166 | 1226777-95-2 | CTS-21166 is a BACE1 inhibitor that can cross the blood-brain barrier and is effective when taken orally. |
|
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. |
|
V117104 | GRL-8234 | 913071-81-5 | GRL-8234 is a potent β-secretase (BACE1) inhibitor with blood-brain barrier permeability (Ki = 1.8 nM). |
|
V71452 | JNJ-67569762 | 2380313-26-6 | JNJ-67569762 is a selective BACE1 inhibitor targeting S3 (IC50 = 2.7 nM). |
|
V100297 | K284-6111 | 702668-62-0 | K284-6111 is an oral chitinase 3-like 1 (CHI3L1) inhibitor. |
|
V71457 | Kushenol C | 99119-73-0 | Kushenol C is extracted from Sophora flavescens root and has anti-inflammatory and antioxidant properties. |
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