BromoTag^® AGB3

Cat. No. 7688 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： Selective Degrader of Brd4^{BD2 L387A} fusion proteins (BromoTag^®)

化学名： (2S,4R)-1-((2S,17R)-2-(tert-Butyl)-17-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,16-dioxo-6,9,12-trioxa-3,15-diazanonadecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

纯度： ≥98% (HPLC)

文献 (3)

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 BromoTag^® AGB3

BromoTag^® ABG3 is a selective "Bump & Hole" TAG Degrader (DC₅₀ 210 - 290 nM, protein degradation t½ = 113 min, D_max = 92%). BromoTag AGB3 comprises a VHL E3 ligase ligand joined by a linker to a (+)-JQ1 (Cat. No. 4499) derivative (the "bump" bearer) that selectively binds the Brd4^{BD2 L387A} variant (the "hole"). In cell lines expressing a fusion of the target protein with the tag, Brd4^{BD2 L387A}, BromoTag AGB3 drives formation of a ternary complex between VHL and the "BromoTagged" protein, leading to ubiquitination of the protein and its subsequent proteasomal degradation.

BromoTag^® is a registered trademark of the University of Dundee and is used under license.

Brd4^{BD2 L387A} can be expressed as a fusion with a target protein of interest using genome engineering techniques via CRISPR-mediated locus-specific knock-in. See protocol for more information.

许可信息

Sold under exclusive licence from the University of Dundee

技术数据 for BromoTag^® AGB3

分子量	1030.7
公式	C₅₁H₆₄ClN₉O₈S₂
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	2776191-07-0
InChI Key	IEUOSJXYLRSZRR-QLMRCLNASA-N
Smiles	ClC1=CC=C(C2=N[C@@H]([C@H](C(NCCOCCOCCOCC(N[C@H](C(N3C[C@@H](C[C@H]3C(NCC4=CC=C(C5=C(N=CS5)C)C=C4)=O)O)=O)C(C)(C)C)=O)=O)CC)C6=NN=C(C)N6C7=C2C(C)=C(S7)C)C=C1

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 BromoTag^® AGB3

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	DMSO	103.07	100

制备储备液 for BromoTag^® AGB3

以下数据基于产品分子量 1030.7。 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.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	0.97 mL	4.85 mL	9.7 mL
5 mM	0.19 mL	0.97 mL	1.94 mL
10 mM	0.1 mL	0.49 mL	0.97 mL
50 mM	0.02 mL	0.1 mL	0.19 mL

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产品说明书 for BromoTag^® AGB3

分析证书/产品说明书

化学品安全技术说明书

参考文献 for BromoTag^® AGB3

参考文献是支持产品生物活性的出版物。

Bond et al (2021) Development of BromoTag: a 'Bump-and-Hole'-PROTAC system to induce potent, rapid, and selective degradation of tagged target proteins. J.Med.Chem. 64 15477 PMID: 34652918

If you know of a relevant reference for BromoTag^® AGB3, please let us know.

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关键词: BromoTag® AGB3, BromoTag® AGB3 supplier, BromoTagAGB3, TAG, Degrades, Degraders, degradation, target, fusion, protein, BromoTag, Brd4BD2, L387A, Degradation, Platform, 7688, 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 GuideUpdated

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

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

Validating Targets for TPD Using dTAG Poster

The dTAG platform offers a generalizable strategy to degrade, in principle, any intracellular protein of interest (POI) and is a useful strategy for exploration and validation of targets. This poster presents a workflow solution for target validation, from custom TAG knock-in cell-lines for your POI, different dTAG Degraders to knockdown you POI, to automated assays for protein degradation using Simple Western^TM instruments. Data are also presented on the use of an antibody that recognizes the TAG domain (FKBP12^F36V) for detection of degradation. Presented at TPD Europe, March 2022, London, UK.