dTAG^V-1

Cat. No. 6914 6 Citations Submit a Review Datasheet / COA / SDS

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Description: Potent and selective degrader of mutant FKBP12^F36V 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% (HPLC)

Datasheet

Citations (6)

Reviews

Literature (3)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for dTAG^V-1

dTAG^V-1 is a degrader targeting mutant FKBP12^F36V 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 FKBP12^F36V fusion proteins in vitro and in vivo. Selectively degrades FKBP12^F36V-EWS/FLI fusion proteins and inhibits cell proliferation in FKBP12^F36V-EWS/FLI-expressing Ewing sarcoma cells.

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

Negative control dTAG^V-1-NEG (Cat. No. 6915) also available.

FKBP12^F36V 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 FKBP12^F36V are available from Addgene.

Licensing Information

Sold under license from Dana-Farber Cancer Institute

Technical Data for dTAG^V-1

M. Wt	1361.58
Formula	C₆₈H₉₀N₆O₁₄S CF₃CO₂H
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2624313-15-9
InChI Key	KSEWNBIDXKMTNT-LNVAYBNASA-N
Smiles	C[C@H](NC([C@@H]1C[C@@H](O)CN1C([C@@H](NC(CCCCCCNC(COC2=CC=CC=C2[C@H](OC([C@@H]3CCCCN3C([C@@H](CC)C4=CC(OC)=C(OC)C(OC)=C4)=O)=O)CCC5=CC(OC)=C(OC)C=C5)=O)=O)C(C)(C)C)=O)=O)C6=CC=C(C=C6)C7=C(N=CS7)C.OC(C(F)(F)F)=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^V-1

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	136.16	100

Preparing Stock Solutions for dTAG^V-1

The following data is based on the product molecular weight 1361.58. 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	0.73 mL	3.67 mL	7.34 mL
5 mM	0.15 mL	0.73 mL	1.47 mL
10 mM	0.07 mL	0.37 mL	0.73 mL
50 mM	0.01 mL	0.07 mL	0.15 mL

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Product Datasheets for dTAG^V-1

Certificate of Analysis / Product Datasheet

Safety Datasheet

References for dTAG^V-1

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

Nabet et al (2020) Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules. Nat.Commun. 11 4687 PMID: 32948771

If you know of a relevant reference for dTAG^V-1, please let us know.

View Related Products by Target

Keywords: dTAGV-1, dTAGV-1 supplier, 2451573-86-5, dTAGVHL1, degraders, degrades, targeted, protein, degradation, FKBP12F36V, fusion, mutant, PROTAC, VHL, von, Hippel, Lindau, TPD, TAG, Degradation, Platform, 6914, Tocris Bioscience

6 Citations for dTAG^V-1

Citations are publications that use Tocris products. Selected citations for dTAG^V-1 include:

Francisca et al (2022) Systematic profiling of conditional degron tag technologies for target validation studies. Nat Commun 13 5495 PMID: 36127368

Tom et al (2022) Control of ribosomal RNA synthesis by hematopoietic transcription factors. Mol Cell 82 3826-3839.e9 PMID: 36113481

Anna-Katerina et al (2022) Generation of knock-in degron tags for endogenous proteins in mice using the dTAG system. STAR Protoc 3 101660 PMID: 36097386

Kristian et al (2021) Generation of locus-specific degradable tag knock-ins in mouse and human cell lines. STAR Protoc 2 100575 PMID: 34151298

Tomek et al (2023) Precise modulation of transcription factor levels identifies features underlying dosage sensitivity. Nat Genet 55 841-851 PMID: 37024583

Cristian et al (2023) MYC regulates CSF-1 expression via microRNA 17/20a to modulate tumor-associated macrophages in osteosarcoma. JCI Insight PMID: 37279073

Do you know of a great paper that uses dTAG^V-1 from Tocris? Please let us know.

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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!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

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

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

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 Western^TM instruments. Data are also presented on the use of an antibody that recognizes the TAG domain (FKBP12^F36V) for detection of degradation. Presented at TPD Europe, March 2022, London, UK.