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AT 1

Cat. No. 6356 3 篇引用文献 1 条评论 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： (+)-JQ1 based PROTAC® with selectivity for BRD4
化学名： (2S,4R)-1-(2R)-2-Acetamido-3-[[6-[2-[(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetamido]hexyl]thio]-3-methylbutanoyl]-4-hydroxy-N-[4-(4-methylthiazol-5-yl)benzyl)pyrrolidinine-2-carboxamide
纯度： ≥98% (HPLC)
说明书
引用文献 (3)
评论 (1)
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 AT 1

AT 1 is a cell penetrant Proteolysis Targeting Chimera (PROTAC®) compound based on (+)-JQ1 (Cat. No. 4499) conjugated to a von Hippel-Lindau (VHL) ligand. Rationally designed based on a ternary complex crystal structure to improve selectivity for BRD4 degradation compared to MZ1 (Cat. No. 6154). Demonstrates profound and selective degradation of BRD4 in cells at 1-3 μM, with negligible loss of BRD2 and BRD3.

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

许可信息

Sold under licence from the University of Dundee

技术数据 for AT 1

分子量 972.68
公式 C48H58ClN9O5S3
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2098836-45-2
PubChem ID 124201841
InChI Key SQNZDYHMCMIGGV-TZPPCSJFSA-N
Smiles CC1=C(C)SC2=C1C(C3=CC=C(Cl)C=C3)=N[C@@H](CC(NCCCCCCSC(C)(C)[C@H](NC(C)=O)C(N4[C@H](C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@@H](O)C4)=O)=O)C7=NN=C(C)N27

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 AT 1

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 97.27 100
ethanol 97.27 100

制备储备液 for AT 1

以下数据基于产品分子量 972.68。 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 1.03 mL 5.14 mL 10.28 mL
5 mM 0.21 mL 1.03 mL 2.06 mL
10 mM 0.1 mL 0.51 mL 1.03 mL
50 mM 0.02 mL 0.1 mL 0.21 mL

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参考文献 for AT 1

参考文献是支持产品生物活性的出版物。

Gadd (2017) Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat.Chem.Biol. 13 514 PMID: 28288108

If you know of a relevant reference for AT 1, please let us know.

按标靶查看相关产品

关键词: AT 1, AT 1 supplier, PROTAC, Proteolysis, targeted, chimeras, Bromodomain, BRD2, BRD3, BRD4, BET, proteins, JQ1, VHL, E3, ubiquitin, ligase, AT1, PROTACs, active, degraders, degrades, protein, degradation, tpd, Bromodomains, (BRD), Degraders, 6356, Tocris Bioscience

3 篇 AT 1 的引用文献

引用文献是使用了 Tocris 产品的出版物。 AT 1 的部分引用包括：

Ma et al (2023) Engineered PROTAC-CID systems for mammalian inducible gene regulation. J Am Chem Soc 145 1593 PMID: 36626587

Lin et al (2021) Time-dependent effect of 1,6-hexanediol on biomolecular condensates and 3D chromatin organization. Genome Biol 22 230 PMID: 34404453

Eric S et al (2021) Chemo-proteomics exploration of HDAC degradability by small molecule degraders. Cell Chem Biol 28 1514-1527.e4 PMID: 34314730

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AT 1 的评论

平均评分: 5 (Based on 1 Review.)

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AT1 PROTAC.
By Anonymous on 07/24/2020
分析类型： In Vitro
种属： Human
细胞系/组织： glioblastoma

We tested the effect of AT1 PROTAC in degrading the endogenous BRD4 protein in glioblastoma cell lines with varying concentrations of AT1 starting from 100nM, 300nM and 1 uM.

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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