dTAG-47

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Cat.No. 7530 - dTAG-47 | C59H73N5O14 | CAS No. 2265886-81-3
Description: Degrades mutant FKBP12F36V fusion proteins; useful alternative to genetic methods for target validation
Chemical Name: (1R)-3-(3,4-Dimethoxyphenyl)-1-(2-(2-((8-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)amino)octyl)amino)-2-oxoethoxy)phenyl)propyl (2S)-1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate
Purity: ≥97% (HPLC)
Datasheet
Citations
Reviews
Literature (3)

Biological Activity for dTAG-47

dTAG-47 is a degrader targeting mutant FKBP12F36V fusion proteins. Comprises a ligand selective for F36V single-point mutated FKBP12, a linker and a cereblon-binding ligand. Application of dTAG-47 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 and dTAG-7.

Negative control (Cat. No. 7531) also available.

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-47

M. Wt 1076.25
Formula C59H73N5O14
Storage Store at -20°C
Purity ≥97% (HPLC)
CAS Number 2265886-81-3
PubChem ID 153280948
InChI Key OQXAQHQPOQLCAE-ODPQSFPTSA-N
Smiles CC[C@@H](C1=CC(OC)=C(C(OC)=C1)OC)C(N2CCCC[C@H]2C(O[C@@H](C3=C(C=CC=C3)OCC(NCCCCCCCCNC4=CC=C5C(N(C(C5=C4)=O)C6CCC(NC6=O)=O)=O)=O)CCC7=CC(OC)=C(C=C7)OC)=O)=O

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-47

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 107.62 100

Preparing Stock Solutions for dTAG-47

The following data is based on the product molecular weight 1076.25. 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 0.93 mL 4.65 mL 9.29 mL
5 mM 0.19 mL 0.93 mL 1.86 mL
10 mM 0.09 mL 0.46 mL 0.93 mL
50 mM 0.02 mL 0.09 mL 0.19 mL

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References for dTAG-47

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

Popay et al (2021) MYC regulates ribosome biogenesis and mitochondrial gene expression programs through its interaction with host cell factor-1. Elife 10 e60191 PMID: 33416496

Bryan et al (2020) WDR5 is a conserved regulator of protein synthesis gene expression. Nucleic Acids Res. 48 2924 PMID: 31996893

Sreekanth et al (2020) Chemogenetic system demonstrates that Cas9 longevity impacts genome editing outcomes. ACS Cent.Sci. 6 2228 PMID: 33376784

Brunetti et al (2018) Mutant NPM1 maintains the leukemic state through HOX expression. Cancer Cell. 34 499 PMID: 30205049

Weintraub et al (2017) YY1 is a structural regulator of enhancer-promoter loops. Cell 171 1573 PMID: 29224777

Layden et al (2021) A protocol for rapid degradation of endogenous transcription factors in mammalian cells and identification of direct regulatory targets. STAR Protoc. 2 100530 PMID: 34041503


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Keywords: dTAG-47, dTAG-47 supplier, dTAG47, degraders, degrades, degradation, FKBP12F36V, fusion, protein, mutant, PROTAC, proteolysis, targeting, chimera, cereblon, PROTACs, TAG, Degradation, Platform, 7530, Tocris Bioscience

Citations for dTAG-47

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Literature in this Area

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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
  • Custom Degrader Services
  • Ubiquitin-Proteasome System Proteins and Assays
  • 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.