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dTAGV-1

Catalog #: 6914
7 Citations Datasheet
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%

Product Details
Citations (7)
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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

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.

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.

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

Product Datasheets

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Citations for dTAGV-1

The citations listed below are publications that use Tocris products. Selected citations for dTAGV-1 include:

7 Citations: Showing 1 - 7

  1. Precise modulation of transcription factor levels identifies features underlying dosage sensitivity.
    Authors: Tomek Et al.
    Nat Genet  2023;55:841-851
  2. MYC regulates CSF-1 expression via microRNA 17/20a to modulate tumor-associated macrophages in osteosarcoma.
    Authors: Cristian Et al.
    JCI Insight  2023;
  3. Control of ribosomal RNA synthesis by hematopoietic transcription factors.
    Authors: Tom Et al.
    Mol Cell  2022;82:3826-3839.e9
  4. Generation of knock-in degron tags for endogenous proteins in mice using the dTAG system.
    Authors: Anna-Katerina Et al.
    STAR Protoc  2022;3:101660
  5. Generation of knock-in degron tags for endogenous proteins in mice using the dTAG system.
    Authors: Abuhashem Et al.
    STAR Protoc.  2022;3:101660
  6. Systematic profiling of conditional degron tag technologies for target validation studies.
    Authors: Francisca Et al.
    Nat Commun  2022;13:5495
  7. Generation of locus-specific degradable tag knock-ins in mouse and human cell lines.
    Authors: Kristian Et al.
    STAR Protoc  2021;2:100575

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