PE859

SKU: orb1303187

Description

PE859 is a small molecule research compound that potently inhibits the aggregation of both tau protein and amyloid-beta (Aβ). This dual inhibitory activity makes it a valuable tool for investigating neurodegenerative mechanisms in models of Alzheimer's disease, applicable in both in vitro and in vivo experimental systems.

Research Area

Neuroscience, Protein Biochemistry, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1402727-29-0
• MW: 448.52
• Purity: 99.60% (May vary between batches)
• Formula: C₂₈H₂₄N₄O₂
• SMILES: COc1cc(OCc2ccccn2)ccc1\C=C\c1cc(\C=C\c2ccc3cc[nH]c3c2)[nH]n1
• Target: Microtubule Associated,Beta Amyloid,Gamma-secretase
• Solubility: DMSO:55 mg/mL (122.63 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.46 mM)

Bioactivity

• Target IC50:
  β-Amyloid:1.2 μM|Tau:0.66 μM
• In Vivo:
  PE859 effectively crosses the blood-brain barrier, enabling its distribution within central nervous system tissues. It reaches a peak concentration of 2.005 μg/mL in blood at 3 hours and 1.428 μg/g in the brain by 6 hours. Notably, PE859 postpones the onset and advancement of motor dysfunction in JNPL3 mice by inhibiting the buildup of sarkosyl-insoluble tau.
• In Vitro:
  In an Alzheimer's patient's brain, senile plaques and neurofibrillary tangles, the abnormal aggregates of amyloid β (Aβ) peptide and Tau Protein, are observed as the two major hallmarks of this disease. PE859 inhibits the heparin-induced aggregation of both 3RMBD and full length tau in a concentration-dependent manner. In each assay, the IC50 values calculated at the last measurement periods are 0.81 μM, and 2.23 μM, respectively. PE859 inhibits tau aggregation through the formation of a beta-sheet structure.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

bAmyloid, b Amyloid, Aβ, Beta Amyloid, BetaAmyloid, Inhibitor, Gammasecretase, inhibit, Microtubule Associated, Microtubule/Tubulin, MicrotubuleAssociated, β Amyloid, βAmyloid, PE859, PE-859, PE 859, tau

Compound Identifiers

PubChem CID

66571561