dTAG-7

Pricing Availability   Qty
说明: First generation Degrader for mutant FKBP12F36V fusion proteins; useful alternative to genetic methods for target validation
化学名: (1R)-3-(3,4-Dimethoxyphenyl)-1-(2-((19-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)-2,18-dioxo-7,10,13-trioxa-3,17-diazanonadecyl)oxy)phenyl)propyl (2S)-1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate
纯度: ≥98% (HPLC)
说明书
引用文献 (3)
评论
文献 (3)

生物活性 for dTAG-7

dTAG-7 is a first generation Degrader for mutant FKBP12F36V fusion proteins. Comprises a ligand selective for F36V single-point mutated FKBP12, a linker and a cereblon-binding ligand. Application of dTAG-7 induces rapid, reversible and selective degradation of FKBP12F36V fusion proteins in vitro and in vivo. dTAG is generalizable to a range of fusion proteins; useful as an alternative to genetic methods for target validation. See also dTAG-13.

FKBP12F36V can be expressed as a fusion with a target protein of interest using genome engineering techniques, via transgene expression or CRISPR-mediated locus-specific knock-in.

Plasmid vectors for the lentiviral expression and CRISPR-mediated knock-in of FKBP12F36V are available from Addgene.

许可信息

Sold under license from Dana-Farber Cancer Institute

技术数据 for dTAG-7

TAG Domain FKBP12F36V
Warhead Ortho-AP1867
E3 Ligase Cereblon
分子量 1210.32
公式 C63H79N5O19
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2064175-32-0
PubChem ID 131954816
InChI Key IFCAWDLUIZXIPI-FJDAOBEISA-N
Smiles CC[C@H](C(=O)N1CCCC[C@H]1C(=O)O[C@H](CCC1=CC(OC)=C(OC)C=C1)C1=C(OCC(=O)NCCCOCCOCCOCCCNC(=O)COC2=C3C(=O)N(C4CCC(=O)NC4=O)C(=O)C3=CC=C2)C=CC=C1)C1=CC(OC)=C(OC)C(OC)=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 dTAG-7

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 121.03 100
ethanol 24.21 20

制备储备液 for dTAG-7

以下数据基于产品分子量 1210.32。 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 0.83 mL 4.13 mL 8.26 mL
5 mM 0.17 mL 0.83 mL 1.65 mL
10 mM 0.08 mL 0.41 mL 0.83 mL
50 mM 0.02 mL 0.08 mL 0.17 mL

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产品说明书 for dTAG-7

分析证书/产品说明书
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参考文献 for dTAG-7

参考文献是支持产品生物活性的出版物。

Moser et al (2018) Acute pharmacologic degradation of a stable antigen enhances its direct presentation on MHC class I molecules. Front.Immunol. 8 1920 PMID: 29358938

Nabet et al (2018) The dTAG system for immediate and target-specific protein degradation. Nat.Chem.Biol. 14 431 PMID: 29581585

Huang et al (2018) A chemoproteomic approach to query the degradable kinome using a multi-kinase degrader. Cell Chem.Biol. 25 88 PMID: 29129717

Yesbolatova et al (2018) TAGing for destruction. Nat.Chem.Biol. 14 414 PMID: 29581583

Erb et al (2017) Transcription control by the ENL YEATS domain in acute leukaemia. Nature 543 270 PMID: 28241139

Nabet et al (2018) The dTAG system for immediate and target-specific protein degradation. Nat.Chem.Biol. 14 431 PMID: 29581585

Bensimon et al (2020) Targeted degradation of SLC transporters reveals amenability of multi-pass transmembrane proteins to ligand-induced proteolysis. Cell Chem.Biol. 27 728 PMID: 32386596


If you know of a relevant reference for dTAG-7, please let us know.

关键词: dTAG-7, dTAG-7 supplier, dTAG7, dFKBP7, degraders, degrades, degradation, FKBP12F36V, fusion, protein, mutant, PROTACs, proteolysis, targeting, chimera, TAG, Degradation, Platform, 6912, Tocris Bioscience

3 篇 dTAG-7 的引用文献

引用文献是使用了 Tocris 产品的出版物。 dTAG-7 的部分引用包括:

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

David et al (2020) SON and SRRM2 are essential for nuclear speckle formation. Elife 9 PMID: 33095160

Cugusi et al (2022) Heat shock induces premature transcript termination and reconfigures the human transcriptome. Mol.Cell 82 1573 PMID: 35114099


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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

Validating Targets for TPD Using dTAG Poster

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 WesternTM instruments. Data are also presented on the use of an antibody that recognizes the TAG domain (FKBP12F36V) for detection of degradation. Presented at TPD Europe, March 2022, London, UK.