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PT-65

Cat. No. 7651 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent GSK3 Degrader (PROTAC®)
化学名： 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
纯度： ≥98% (HPLC)
说明书
引用文献
评论
文献 (2)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 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.

技术数据 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
分子量 1082.19
公式 C51H63N13O12S
储存 Store at -20°C
纯度 ≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

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

溶解性数据 for PT-65

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 108.22 100

制备储备液 for PT-65

以下数据基于产品分子量 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 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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参考文献 for PT-65

参考文献是支持产品生物活性的出版物。

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.

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关键词: PT-65, PT-65 supplier, potent, bromodomains, GSK3α, GSK3β, active, degraders, degrades, PROTAC, PROTACs, targeted, protein, degradation, tpd, AD, Alzheimer, in, vivo, Glycogen, Synthase, Kinase, 3, Degraders, 7651, Tocris Bioscience

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该领域的文献

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

*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。

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