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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.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Technical Data for PT-65
|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|
|Storage||Store at -20°C|
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|
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.
|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|
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!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Targeted Protein Degradation Research Product Guide
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Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Epigenetics in Cancer Poster
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
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