1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Microtubule/Tubulin
  3. PE859

PE859 

Cat. No.: HY-12662 Purity: 99.84%
Handling Instructions

PE859 is a potent inhibitor of both tau and aggregation with IC50 values of 0.66 and 1.2 μM, respectively.

For research use only. We do not sell to patients.

PE859 Chemical Structure

PE859 Chemical Structure

CAS No. : 1402727-29-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 391 In-stock
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 396 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

PE859 is a potent inhibitor of both tau and aggregation with IC50 values of 0.66 and 1.2 μM, respectively.

IC50 & Target

IC50: 0.66 μM (tau), 1.2 μM (Aβ)[1]

In Vitro

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 formation of beta-sheet structure[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PE859 could cross the blood-brain barrier and that 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]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

448.52

Formula

C₂₈H₂₄N₄O₂

CAS No.

1402727-29-0

SMILES

COC1=CC(OCC2=NC=CC=C2)=CC=C1/C=C/C3=CC(/C=C/C4=CC5=C(C=C4)C=CN5)=NN3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (111.48 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2296 mL 11.1478 mL 22.2956 mL
5 mM 0.4459 mL 2.2296 mL 4.4591 mL
10 mM 0.2230 mL 1.1148 mL 2.2296 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.57 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.57 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[2]

Tau aggregation is monitored using thioflavin T. The test compound (PE859), 10 μM 3RMBD and 10 μM heparin are dissolved in 50 mM Tris-HCl (pH7.6), and incubated at 37°C up to 144 hours. At each point of incubation time, 135 μL of the solutions are removed and mixed with 15 μL of 100 μM ThT solution (final concentration: 10 μM) and the fluorescence intensity with excitation at 440 nm and emission at 486 nm is measured[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice: PE859 is dissolved in 80% PEG400 and 20% water solution at 5 mg/mL, and orally-administered at a dose of 40 mg/kg/day for 6 months (from 9 to 15 months of age). The body weights of the mice are measured once a week during PE859 treatment[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

PE859PE 859PE-859Microtubule/TubulinInhibitorinhibitorinhibit

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Product Name:
PE859
Cat. No.:
HY-12662
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