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Submit ReviewdTAG-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.
Sold under license from Dana-Farber Cancer Institute
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 121.03 | 100 | |
ethanol | 24.21 | 20 |
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.
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 |
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
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
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
Do you know of a great paper that uses dTAG-7 from Tocris? Please let us know.
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
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