dTAG-13

Name: dTAG-13
Brand: tocris
SKU: 6605
Rating: 5 (3 reviews)

Catalog # 6605

Citations (1)

(3)

Datasheet / COA / SDS

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Bio-Techne Corporation

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Key Product Details

Description:	Degrades mutant FKBP12^F36V fusion proteins; useful alternative to genetic methods for target validation
Chemical Name:	1-[(2S)-1-Oxo-2-(3,4,5-trimethoxyphenyl)butyl]-(2S)-2-piperidinecarboxylate (1R)-3-(3,4-dimethoxyphenyl)-1-[2-[2-[[6-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]hexyl]amino]-2-oxoethoxy]phenyl]propyl ester
Purity:	≥98% (HPLC)
Molecular Weight:	1049.18

View Full Technical Details for dTAG-13

Biological Activity

Degrader targeting 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-13 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.

Negative control (Cat. No. 6916) 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

M. Wt	1049.18
Formula	C₅₇H₆₈N₄O₁₅
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2064175-41-1
PubChem ID	124187630
InChi Key	BJFBRLAWLPZOMJ-QHVFGHLPSA-N
Smiles	CC[C@@H](C1=CC(OC)=C(C(OC)=C1)OC)C(N2CCCC[C@H]2C(O[C@@H](C3=C(C=CC=C3)OCC(NCCCCCCOC4=C5C(N(C(C5=CC=C4)=O)C6CCC(NC6=O)=O)=O)=O)CCC7=CC(OC)=C(C=C7)OC)=O)=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

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	52.46	50
	ethanol	20.98	20

Preparing Stock Solutions

The following data is based on the product molecular weight 1049.18.

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
0.5 mM	1.91 mL	9.53 mL	19.06 mL
2.5 mM	0.38 mL	1.91 mL	3.81 mL
5 mM	0.19 mL	0.95 mL	1.91 mL
25 mM	0.04 mL	0.19 mL	0.38 mL

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References

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

Erb Transcription control by the ENL YEATS domain in acute leukaemia. Nature 2017 PMID: 28241139
Nabet The dTAG system for immediate and target-specific protein degradation. Nat.Chem.Biol. 2018 PMID: 29581585
Bensimon Targeted degradation of SLC transporters reveals amenability of multi-pass transmembrane proteins to ligand-induced proteolysis. Cell Chem.Biol. 2020 PMID: 32386596

Citations (1)

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Citations are publications that use Bio-Techne products. Selected citations for dTAG-13 include:

Kaji et al. (2020) Characterization of cereblon-dependent targeted protein degrader by visualizing the spatiotemporal ternary complex formation in cells Sci.Rep.. 10:3088
PMID: 32080280
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dTAG-13 treatment of FKBP tagged over expressed protein in glioma cell lines

Name: Anonymous

Species: Human

Assay Type: In Vitro

Cell Line/Tissue: Glioma

Assayed the degradation of FKBP-tagged-protein with HA tag in glioma cells using dTAG-13 at 500nM concentration for 0h, 4h, 6h and 24h time intervals. Untransfected cells has no HA signal and in transfected cells with dTAG-13 treatment lead to complete degradation of FKBP-tagged-protein in whole cell lysates
Knockdown of FKBP-tagged Chromatin Protein

Name: Sam Weeks

Species: Mouse

Assay Type: In Vitro

Cell Line/Tissue: mESC

Assayed different dTag concentrations (50nm, 250nm, 500nm) for the knockdown of a FKBP-tagged chromatin-bound protein (180kDa). Whole cell lysate (RIPA) revealed no change to WT cells (150kDa) and considerable knockdown in all conditions after just an hour of treatment.
Works better than expected

Name: Abderhman Abuhashem

Species: Mouse

Assay Type: In Vitro

Cell Line/Tissue: E14 (mouse Embryonic Stem cells)

Used dTAG-13 to degrade a transgene tagged with FKBM12-F36V and HA tags to visualize the protein.

This is a western blot probed for HA tag to track degradation. All samples are treated with 500nM dTAG-13. Lanes are: 1) parental cell line, 2) control (no treatment), 3) 30 mins of treatment, 4) 1hr of treatment, 5) 2hrs of treatment, 6) 4hrs of treatment, 7) 6hrs of treatment. The constructs, as shown by the western, was degraded almost entirely (>98% quantified), within 30 mins. I have tested batch 2 of this product at conc. as low as 50nM and still just as effective. No apparent toxicity to cells. Extremely satisfied.

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dTAG-13

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Citations (1)

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dTAG-13 treatment of FKBP tagged over expressed protein in glioma cell lines

Knockdown of FKBP-tagged Chromatin Protein

Works better than expected

Product Datasheets

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Certificate of Analysis

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