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

PE859 is a potent inhibitor of both tau and Aβ 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

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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 USD 198 In-stock
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10 mM * 1 mL in DMSO USD 198 In-stock
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5 mg USD 180 In-stock
10 mg USD 280 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

PE859 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE PE859

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

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

PE859 Related Antibodies
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]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

448.52

Formula

C28H24N4O2
CAS No.
Appearance

Solid

Color

Light yellow to khaki

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (111.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2296 mL 11.1478 mL 22.2956 mL 55.7389 mL
5 mM 0.4459 mL 2.2296 mL 4.4591 mL 11.1478 mL
10 mM 0.2230 mL 1.1148 mL 2.2296 mL 5.5739 mL
15 mM 0.1486 mL 0.7432 mL 1.4864 mL 3.7159 mL
20 mM 0.1115 mL 0.5574 mL 1.1148 mL 2.7869 mL
25 mM 0.0892 mL 0.4459 mL 0.8918 mL 2.2296 mL
30 mM 0.0743 mL 0.3716 mL 0.7432 mL 1.8580 mL
40 mM 0.0557 mL 0.2787 mL 0.5574 mL 1.3935 mL
50 mM 0.0446 mL 0.2230 mL 0.4459 mL 1.1148 mL
60 mM 0.0372 mL 0.1858 mL 0.3716 mL 0.9290 mL
80 mM 0.0279 mL 0.1393 mL 0.2787 mL 0.6967 mL
100 mM 0.0223 mL 0.1115 mL 0.2230 mL 0.5574 mL
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PE859 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PE8591402727-29-0PE 859PE-859Microtubule/TubulinInhibitorinhibitorinhibit

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