JavaScript is disabled in your browser. Please enable JavaScript to view this website.
AB223886

LY2886721, BACE-1 inhibitor

Be the first to review this product! Submit a review

|

(1 Publication)

MW 390.4 Da, Purity >98%. Potent and selective BACE-1 inhibitor (IC50 = 20.3 nM for recombinant hBACE-1). Human BACE2 is inhibited with an IC50 of 10.2 nM. Does not inhibit other aspartyl proteases such as cathepsin D, pepsin, and renin. A potential agent to treat Alzheimer's Disease. Inhibits production of Aβ in HEK-293 Swe cells (IC50 values are 18.5 nM and 19.7 nM for Aβ1-40 and Aβ1-42 respectively) and in PDAPP neuronal cells (IC50 ~10 nM). Reduces dose-dependently brain levels of Aβ, C99 and sAPPβ in orally administered mouse model and plasma Aβ in dog model. Ppenetrates the blood-brain barrier.

View Alternative Names

APP beta secretase, Asp 2, Aspartyl protease 2, BACE, BACE1_HUMAN, Beta secretase, Beta site APP cleaving enzyme, Beta site amyloid beta A4 precursor protein cleaving enzyme, Beta site amyloid precursor protein cleaving enzyme, Beta-secretase 1, Beta-site APP cleaving enzyme 1, Beta-site amyloid precursor protein cleaving enzyme 1, FLJ90568, HSPC104, Memapsin-2, Membrane-associated aspartic protease 2, Transmembrane aspartic proteinase Asp2

1 Images
Chemical Structure - LY2886721, BACE-1 inhibitor (AB223886)
  • Chemical Structure

Lab

Chemical Structure - LY2886721, BACE-1 inhibitor (AB223886)

2D chemical structure image of ab223886, LY2886721, BACE-1 inhibitor

Key facts

CAS number

1262036-50-9

Purity

>98%

Form

Solid

form

Molecular weight

390.4 Da

Molecular formula

C<sub>1</sub><sub>8</sub>H<sub>1</sub><sub>6</sub>F<sub>2</sub>N<sub>4</sub>O<sub>2</sub>S

PubChem

49837968

Nature

Synthetic

Solubility

Soluble in DMSO to 20 mM

Soluble in Ethanol < 2 mM

Biochemical name

N-(3-((4aS,7aS)-2-amino-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-fluoropicolinamide

Biological description

Potent and selective BACE-1 inhibitor (IC50 = 20.3 nM for recombinant hBACE-1). Human BACE2 is inhibited with an IC50 of 10.2 nM. Does not inhibit other aspartyl proteases such as cathepsin D, pepsin, and renin. A potential agent to treat Alzheimer's Disease. Inhibits production of Aβ in HEK-293 Swe cells (IC50 values are 18.5 nM and 19.7 nM for Aβ1-40 and Aβ1-42 respectively) and in PDAPP neuronal cells (IC50 ~10 nM). Reduces dose-dependently brain levels of Aβ, C99 and sAPPβ in orally administered mouse model and plasma Aβ in dog model. Ppenetrates the blood-brain barrier.

Canonical smiles

C1C2CSC(=NC2(CO1)C3=C(C=CC(=C3)NC(=O)C4=NC=C(C=C4)F)F)N

Isomeric smiles

C1[C@H]2CSC(=N[C@]2(CO1)C3=C(C=CC(=C3)NC(=O)C4=NC=C(C=C4)F)F)N

InChi

InChI=1S/C18H16F2N4O2S/c19-11-1-4-15(22-6-11)16(25)23-12-2-3-14(20)13(5-12)18-9-26-7-10(18)8-27-17(21)24-18/h1-6,10H,7-9H2,(H2,21,24)(H,23,25)/t10-,18-/m0/s1

InChiKey

NIDRNVHMMDAAIK-YPMLDQLKSA-N

IUPAC Name

N-[3-[(4aS,7aS)-2-amino-4,4a,5,7-tetrahydrofuro[3,4-d][1,3]thiazin-7a-yl]-4-fluorophenyl]-5-fluoropyridine-2-carboxamide

style
left-column

Product details

This product is manufactured by BioVision, an Abcam company and was previously called 2299 LY2886721. 2299-25 is the same size as the 25 mg size of ab223886.
style
left-column

Properties and storage information

Shipped at conditions
Blue Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
Storage information
Store in the dark|Store under desiccating conditions
style
left-column

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

BACE1 also known as beta-site APP cleaving enzyme 1 or beta-secretase plays an important role in the cleavage of amyloid precursor protein (APP). This cleavage results in the production of amyloid-beta peptides which are associated with Alzheimer's disease. BACE1 is a membrane-bound aspartic protease and has a molecular weight of approximately 50100 Da. The enzyme expresses mostly in the brain's neurons and some secretory tissues.
Biological function summary

BACE1 initiates the amyloidogenic pathway of APP processing which involves amyloid-beta generation. BACE1 doesn't function alone but acts as part of a complex that aids in protein substrate recognition and processing. Its activity contributes to physiological processes like myelination and axonal guidance indicating its importance beyond amyloid production.

Pathways

BACE1 is integral to the amyloidogenic pathway which is important in Alzheimer's disease development. It interacts with proteins such as presenilin 1 a part of the gamma-secretase complex that further processes the amyloid-beta precursor. Furthermore BACE1 links to synaptic functions and neural signaling pathways highlighting its multifaceted roles.

BACE1 holds significance in Alzheimer's disease due to its role in amyloid-beta peptide production. This connection has led to the development of BACE1 inhibitors as potential therapeutic agents. Additionally BACE1’s involvement in other neural functions ties it to cognitive impairments. It also relates to APP through its function in Alzheimer's suggesting targeted strategies for treatment could involve modulating BACE1 activity.
style
left-column
style
left-column

Product protocols

style
left-column

Publications (1)

Recent publications for all applications. Explore the full list and refine your search

Nature communications 16:3753 PubMed40307257

2025

Divergent actions of physiological and pathological amyloid-β on synapses in live human brain slice cultures.

Applications

Unspecified application

Species

Unspecified reactive species

Robert I McGeachan,Soraya Meftah,Lewis W Taylor,James H Catterson,Danilo Negro,Calum Bonthron,Kristján Holt,Jane Tulloch,Jamie L Rose,Francesco Gobbo,Ya Yin Chang,Jamie Elliott,Lauren McLay,Declan King,Imran Liaquat,Tara L Spires-Jones,Sam A Booker,Paul M Brennan,Claire S Durrant
View all publications
style
left-column
style
left-column
style
right-column

Complementary Products

Biochemicals

AB142164

Compound E, gamma;-secretase inhibitor

Chemical Structure - Compound E, gamma;-secretase inhibitor (AB142164)

  • 0
  • 0
Biochemicals

AB223883

MK-8931, Beta-sectetase inhibitor

Chemical Structure - MK-8931, Beta-sectetase inhibitor (AB223883)

  • 0
  • 0
Biochemicals

AB141276

Marimastat, Matrix metalloprotease (MMP) inhibitor

Chemical Structure - Marimastat, Matrix metalloprotease (MMP) inhibitor (AB141276)

  • 0
  • 0
Primary Antibodies

AB108394

Anti-BACE1 antibody [EPR3956]

20ul selling size|RabMAb|Recombinant|KO Validated

Western blot - Anti-BACE1 antibody [EPR3956] (AB108394)

  • 5
  • 2

Product promise

We are committed to supporting your work with high-quality reagents, and we're here for you every step of the way. In the unlikely event that one of our products does not perform as expected, you're protected by our Product Promise.
For full details, please see our Terms & Conditions

Please note: All products are 'FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC OR THERAPEUTIC PROCEDURES'.

For licensing inquiries, please contact partnerships@abcam.com