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dTAGV-1

Catalog #: 6914 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
6914/5
dTAGV-1 | CAS No. 2624313-15-9 | TAG Degradation Platforms
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Description: Potent and selective degrader of mutant FKBP12F36V fusion proteins

Chemical Name: (R)-3-(3,4-Dimethoxyphenyl)-1-(2-(2-((7-(((S)-1-((2S,4R)-4-hydroxy-2-(((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-7-oxoheptyl)amino)-2-oxoethoxy)phenyl)propyl (S)-1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate trifluoroacetate

Purity: ≥98%

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Biological Activity

dTAGV-1 is a degrader targeting mutant FKBP12F36V fusion proteins. Comprises a ligand selective for F36V single-point mutated FKBP12, a linker and a von Hippel-Lindau (VHL)-binding ligand. Induces potent and selective degradation of FKBP12F36V fusion proteins in vitro and in vivo. Selectively degrades FKBP12F36V-EWS/FLI fusion proteins and inhibits cell proliferation in FKBP12F36V-EWS/FLI-expressing Ewing sarcoma cells.

Hydrochloride salt (Cat.No. 7374) available; suitable for in vivo use.

Negative control dTAGV-1-NEG (Cat. No. 6915) 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.

Technical Data

M.Wt:
1361.58
Formula:
C68H90N6O14S CF3CO2H
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2624313-15-9

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.

Complete Your Experiment

dTAG-13
Cat # 6605
dTAGV-1-NEG
Cat # 6915
dTAG-13-NEG
Cat # 6916
dTAGV-1 hydrochloride
Cat # 7374

Additional Information

Licensing Caveats:
Sold under license from Dana-Farber Cancer Institute

Background References

  1. Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules.
    Nabet et al.
    Nat.Commun., 2020;11:4687

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Tocris Small Molecules

dTAGV-1 hydrochloride

7374
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dTAGV-1-NEG

6915
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