dTAG-7

Name: dTAG-7
Brand: Tocris Bioscience
SKU: 6912

Tocris Bioscience, part of Bio-Techne | Catalog # 6912

COA / SDS

First generation Degrader for mutant FKBP12F36V fusion proteins; useful alternative to genetic methods for target validation

Key Product Details

Description:	First generation Degrader for mutant FKBP12^F36V fusion proteins; useful alternative to genetic methods for target validation
Chemical Name:	(1R)-3-(3,4-Dimethoxyphenyl)-1-(2-((19-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)-2,18-dioxo-7,10,13-trioxa-3,17-diazanonadecyl)oxy)phenyl)propyl (2S)-1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate
Purity:	≥98% (HPLC)
Molecular Weight:	1210.32

View Full Technical Details for dTAG-7

Technical Data
Citations

Biological Activity for dTAG-7

dTAG-7 is a first generation Degrader for mutant FKBP12^F36V 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 FKBP12^F36V 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.

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.

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-7

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
TAG Domain	FKBP12^F36V
Warhead	Ortho-AP1867
E3 Ligase	Cereblon

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 for dTAG-7

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	121.03	100
	ethanol	24.21	20

Preparing Stock Solutions for dTAG-7

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

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References for dTAG-7

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

Bensimon Targeted degradation of SLC transporters reveals amenability of multi-pass transmembrane proteins to ligand-induced proteolysis. Cell Chem.Biol. 2020 PMID: 32386596
Erb Transcription control by the ENL YEATS domain in acute leukaemia. Nature 2017 PMID: 28241139
Yesbolatova TAGing for destruction. Nat.Chem.Biol. 2018 PMID: 29581583
Huang A chemoproteomic approach to query the degradable kinome using a multi-kinase degrader. Cell Chem.Biol. 2018 PMID: 29129717
Nabet The dTAG system for immediate and target-specific protein degradation. Nat.Chem.Biol. 2018 PMID: 29581585
Moser Acute pharmacologic degradation of a stable antigen enhances its direct presentation on MHC class I molecules. Front.Immunol. 2018 PMID: 29358938