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PT-65

Cat. No. 7651 Submit a Review Datasheet / COA / SDS
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Description: Potent GSK3 Degrader (PROTAC®)
Chemical Name: 3-Amino-6-(4-((4-(4-(1-(17-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-3,6,9,12,15-pentaoxaheptadecyl)-1H-1,2,3-triazol-4-yl)butyl)piperazin-1-yl)sulfonyl)phenyl)-N-(pyridin-3-yl)pyrazine-2-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for PT-65

PT-65 is a potent GSK3 Degrader (PROTAC®) (DC50 = 28.3 nM and 34.2 nM against GSK3α and GSK3β, respectively, in SH-SY5Y cells). It suppresses Okadaic acid (Cat. No. 1136) -induced tau hyperphosphorylation and ameliorates learning and memory impairments in rat models of Alzheimer's disease.

GSK3β antibodies validated for Western Blot also available: Catalog # NBP1-47470 and AF2157.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Technical Data for PT-65

E3 ligase CRBN
DC50 28.3 nM (GSK3α) / 34.2 nM (GSK3β) - Degradation in SH-SY5Y cells after 24 h treatment
Kd (Degrader to Target) 12.41 nM - SPR
Selectivity confirmed by global proteomics Yes
M. Wt 1082.19
Formula C51H63N13O12S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2721998-87-2
InChI Key QJSFLEBIQZMJQF-UHFFFAOYSA-N
Smiles O=C(NC=1C=NC=CC1)C=2N=C(C=NC2N)C3=CC=C(C=C3)S(=O)(=O)N4CCN(CC4)CCCCC=5N=NN(C5)CCOCCOCCOCCOCCOCCNC6=CC=CC=7C(=O)N(C(=O)C67)C8C(=O)NC(=O)CC8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for PT-65

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 108.22 100

Preparing Stock Solutions for PT-65

The following data is based on the product molecular weight 1082.19. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 0.92 mL 4.62 mL 9.24 mL
5 mM 0.18 mL 0.92 mL 1.85 mL
10 mM 0.09 mL 0.46 mL 0.92 mL
50 mM 0.02 mL 0.09 mL 0.18 mL

Molarity Calculator

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Reconstitution Calculator

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Dilution Calculator

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References for PT-65

References are publications that support the biological activity of the product.

Qu et al (2021) Discovery of PT-65 as a highly potent and selective proteolysis-targeting chimera degrader of GSK3 for treating Alzheimer's disease. Eur.J.Med.Chem. 226 113889 PMID: 34649182

If you know of a relevant reference for PT-65, please let us know.

View Related Products by Target

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Citations for PT-65

Citations are publications that use Tocris products.

Currently there are no citations for PT-65. Do you know of a great paper that uses PT-65 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia