Home Tools
Log in
Cart

PE859

Catalog No. T4077   CAS 1402727-29-0

PE859 is a potent inhibitor of both tau and Aβ aggregation.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
PE859 Chemical Structure
PE859, CAS 1402727-29-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 119.00
2 mg In stock $ 168.00
5 mg In stock $ 255.00
10 mg In stock $ 389.00
25 mg In stock $ 652.00
50 mg In stock $ 928.00
100 mg In stock $ 1,260.00
500 mg In stock $ 2,530.00
1 mL * 10 mM (in DMSO) In stock $ 279.00
Bulk Inquiry
Get quote
Select Batch  
Purity: 99.6%
Purity: 98.8%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description PE859 is a potent inhibitor of both tau and Aβ aggregation.
Targets&IC50 Aβ:1.2 μM, tau:0.66 μM
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[2].
In vivo PE859 is able to cross the blood-brain barrier and thus PE859 could be distributed into the tissues of the central nervous system. The maximum concentration of PE859 is 2.005 μg/mL in the blood at 3 h and 1.428 μg/g in the brain at 6 h. PE859 delays onset and progression of the motor dysfunction in JNPL3 mice. PE859 delays progression of the motor dysfunction through the inhibition of accumulation of sarkosyl-insoluble tau. [2]
Kinase Assay PEL cells are incubated in triplicate in a 96-well microculture plate in the presence of different concentrations of methyl-β-cyclodextrin (0-10 mM) in a final volume of 0.1 mL for 24 h at 37°C. Subsequently, MTT (0.5 mg/mL final concentration) is added to each well. After 3 h of additional incubation, 100 μL of a 0.04 N HCl is added to dissolve the crystals. Absorption values at 570 nm are determined.
Molecular Weight 448.52
Formula C28H24N4O2
CAS No. 1402727-29-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL

TargetMolReferences and Literature

1. Okuda, M., Hijikuro, I., Fujita, Y., Teruya, T., Kawakami, H., Takahashi, T., & Sugimoto, H. (2016). Design and synthesis of curcumin derivatives as tau and amyloid β dual aggregation inhibitors. Bioorganic & Medicinal Chemistry Letters, 26(20), 5024-5028. doi: 10.1016/j.bmcl.2016.08.092 2. Okuda M, et al. PE859, a novel tau aggregation inhibitor, reduces aggregated tau and prevents onset and progression of neural dysfunction in vivo. PLoS One. 2015 Feb 6;10(2):e20117511.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Microtubule-Targeted Compound Library Stem Cell Differentiation Compound Library NO PAINS Compound Library Neuronal Signaling Compound Library Target-Focused Phenotypic Screening Library Bioactive Compound Library Protease Inhibitor Library Cytoskeletal Signaling Pathway Compound Library Anti-Alzheimer's Disease Compound Library

Related Products

Related compounds with same targets
β-Amyloid (31-35) γ-Secretase-IN-1 β-Amyloid 15-21 acetate CGP52411 PBD-150 Saikosaponin C β-Amyrin DC-Chol hydrochloride

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PE859 1402727-29-0 Cytoskeletal Signaling Neuroscience Proteases/Proteasome Stem Cells Beta Amyloid Gamma-secretase Microtubule Associated PE 859 Inhibitor PE-859 inhibit Microtubule/Tubulin inhibitor

 

TargetMol