dTAG-7

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Description: First generation Degrader for mutant FKBP12F36V fusion proteins; useful alternative to genetic methods for target validation
Chemical Name: (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
Purity: ≥98% (HPLC)
Datasheet
Citations (2)
Reviews
Literature (3)

Biological Activity 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. Custom knock-in cell lines for the dTAG and aTAG platforms are available from our sister brand R&D Systems. Email TPD@bio-techne.com to enquire.

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

Licensing Information

Sold under license from Dana-Farber Cancer Institute

Technical Data for dTAG-7

TAG Domain FKBP12F36V
Warhead Ortho-AP1867
E3 Ligase Cereblon
M. Wt 1210.32
Formula C63H79N5O19
Storage Store at -20°C
Purity ≥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

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.

Solubility Data for dTAG-7

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 121.03 100
ethanol 24.21 20

Preparing Stock Solutions for dTAG-7

The following data is based on the product molecular weight 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 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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Product Datasheets for dTAG-7

Certificate of Analysis / Product Datasheet
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References for dTAG-7

References are publications that support the biological activity of the product.

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.

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

2 Citations for dTAG-7

Citations are publications that use Tocris products. Selected citations for dTAG-7 include:

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

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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Literature in this Area

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

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Targeted Protein Degradation Research Product Guide

Targeted Protein Degradation Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Ubiquitin-Proteasome System Proteins
  • Assays for Protein Degradation
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.