2. PROTAC Stem Cell/Wnt PI3K/Akt/mTOR Neuronal Signaling
  3. PROTACs GSK-3 Tau Protein
  4. PT-65

PT-65 is a GSK3α and GSK3β PROTAC degrader with DC50 values of 28.3 nM and 34.2 nM, respectively. PT-65 inhibits excessive tau phosphorylation mediated by GSK3β, Aβ and Okadaic acid (HY-N6785). PT-65 is applicable for the research of Alzheimer's disease.
(Pink: GSK-3α and GSK-3β ligand (HY-15761); Blue: Cereblon ligand (HY-10984); Black: linker).

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

PT-65

PT-65 Chemical Structure

CAS No. : 2721998-87-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

PT-65 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All GSK-3 Isoform Specific Products:

View All Isoforms
GSK-3 GSK-3α GSK-3β

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PT-65 is a GSK3α and GSK3β PROTAC degrader with DC50 values of 28.3 nM and 34.2 nM, respectively. PT-65 inhibits excessive tau phosphorylation mediated by GSK3β, Aβ and Okadaic acid (HY-N6785). PT-65 is applicable for the research of Alzheimer's disease[1]. (Pink: GSK-3α and GSK-3β ligand (HY-15761); Blue: Cereblon ligand (HY-10984); Black: linker).

IC50 & Target[1]

GSK-3α

28.3 nM (DC50)

GSK-3β

34.2 nM (DC50)

In Vitro

PT-65 (62.5-1000 nM; 48 h) dose-dependently reduces GSK3β-mediated tau hyperphosphorylation at serine 396, serine 404, and threonine 205 sites in GSK3β-overexpressing HEK-293T cells by inducing GSK3β degradation, with phosphorylated tau levels recovering fully 12 h after compound washout[1].
PT-65 (0-100 μM; 72 h) protects SH-SY5Y cells from Aβ42-induced neurotoxicity by dose-dependently reducing GSK3 levels and subsequent tau hyperphosphorylation, with no intrinsic cytotoxicity up to 100 μM[1].

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

PT-65 Related Antibodies

Western Blot Analysis[1]

Cell Line: GSK3β-overexpressing HEK-293T cells
Concentration: 62.5, 125, 250, 500 and 1000 nM (24 h dose-dependent); 1 μM (washout recovery)
Incubation Time: 24 h (dose-dependent); 24 h treatment followed by up to 36 h washout recovery
Result: Induced dose-dependent degradation of GSK3β, accompanied by dose-dependent reduction of phosphorylated tau at serine 396, serine 404, and threonine 205 sites; total tau levels remained unchanged.
Recovered GSK3β levels gradually after washout of 1 μM PT-65, and restored phosphorylated tau levels fully by 12 h post-washout.
In Vivo

PT-65 (200-600 μM/5 μL; i.c.v.; two doses: 72 h pre-model establishment and 72 h post-model establishment) dose-dependently ameliorates okadaic acid-induced learning and memory impairments in male Sprague-Dawley rats, while reducing hippocampal GSK3α/β levels and tau hyperphosphorylation[1].

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

Animal Model: Sprague-Dawley (male, 3 months old, 280-300 g, unilateral hippocampal microinjection of okadaic acid to induce AD-like pathology)[1]
Dosage: 200 μM/5 μL; 600 μM/5 μL
Administration: i.c.v.; two doses: 72 h pre-model establishment and 72 h post-model establishment
Result: Reduced escape latency times on day 3, day 4, and day 5 posttreatment (high dose: 600 μM/5 μL) compared to OA-treated rats.
Reduced escape latency compared to OA-treated rats (low dose: 200 μM/5 μL).
Increased time spent in the target quadrant in probe trial compared to OA-treated rats (both doses).
Dose-dependently reduced hippocampal levels of GSK3α, GSK3β, and hyperphosphorylated tau at the S404, S396, and T205 sites compared to OA-treated rats.
Reduced the density of p-T205-tau-positive staining in hippocampal tissue compared to OA-treated rats.
Molecular Weight

1082.19

Formula

C51H63N13O12S
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C(C1=C(N)N=CC(C2=CC=C(S(=O)(N3CCN(CCCCC4=CN(CCOCCOCCOCCOCCOCCNC5=CC=CC(C(N6C7C(NC(CC7)=O)=O)=O)=C5C6=O)N=N4)CC3)=O)C=C2)=N1)NC8=CC=CN=C8
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (92.41 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 0.9241 mL 4.6203 mL 9.2405 mL
5 mM 0.1848 mL 0.9241 mL 1.8481 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
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 (2.31 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 (2.31 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

Purity: 99.48%

SDS (252 KB)

COA (242 KB) HNMR (153 KB) RP-HPLC (171 KB) LCMS (235 KB)

Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9241 mL 4.6203 mL 9.2405 mL 23.1013 mL
5 mM 0.1848 mL 0.9241 mL 1.8481 mL 4.6203 mL
10 mM 0.0924 mL 0.4620 mL 0.9241 mL 2.3101 mL
15 mM 0.0616 mL 0.3080 mL 0.6160 mL 1.5401 mL
20 mM 0.0462 mL 0.2310 mL 0.4620 mL 1.1551 mL
25 mM 0.0370 mL 0.1848 mL 0.3696 mL 0.9241 mL
30 mM 0.0308 mL 0.1540 mL 0.3080 mL 0.7700 mL
40 mM 0.0231 mL 0.1155 mL 0.2310 mL 0.5775 mL
50 mM 0.0185 mL 0.0924 mL 0.1848 mL 0.4620 mL
60 mM 0.0154 mL 0.0770 mL 0.1540 mL 0.3850 mL
80 mM 0.0116 mL 0.0578 mL 0.1155 mL 0.2888 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

PT-65 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:

PT-652721998-87-2PT65PT 65PROTACsGSK-3Tau ProteinGlycogen synthase kinase-3Glycogen synthase kinase 3CRBN E3 ubiquitin ligaseAβGSK3βGSK3αSH-SY5Y cellsproteasometau hyperphosphorylationHEK-293T cellsAlzheimer's diseaseokadaic acidInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PT-65
Cat. No.:
HY-153166
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (252 KB) Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB) Italian - IT (252 KB) Korean - KR (252 KB) Portuguese - PT (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.