PT-65

Name: PT-65
Brand: Tocris Bioscience
SKU: 7651

Tocris Bioscience, part of Bio-Techne | Catalog # 7651

COA / SDS

Potent GSK3 Degrader (PROTAC®)

Key Product Details

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)
Molecular Weight:	1082.19

View Full Technical Details for PT-65

Technical Data
Citations

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

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
E3 ligase	CRBN
DC₅₀	28.3 nM (GSK3α) / 34.2 nM (GSK3β) - Degradation in SH-SY5Y cells after 24 h treatment
K_d (Degrader to Target)	12.41 nM - SPR
Selectivity confirmed by global proteomics	Yes

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 for PT-65

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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.

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

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References for PT-65

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

Qu 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. 2021 PMID: 34649182