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PT-65

Catalog #: 7651 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
7651/5
PT-65 | CAS No. 2721998-87-2 | Active Degraders
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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%

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Biological Activity

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

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
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2721998-87-2

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.

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