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dTAG-13

Cat. No. 6605 Submit a Review Datasheet / COA / SDS
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Cat.No. 6605 - dTAG-13 | C57H68N4O15 | CAS No. 2064175-41-1
Description: Degrades mutant FKBP12F36V 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)
Datasheet
Citations
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Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Thalidomide-based PROTAC targeting mutant FKBP12F36V fusion proteins. Comprises a ligand selective for F36V single-point mutated FKBP12, a linker and the cereblon-binding ligand, Thalidomide (Cat. No. 0652). 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). Application of dTAG-13 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.

Plasmid vectors for the lentiviral expression and CRISPR-mediated knock-in of FKBP12F36V 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 Data

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 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

If you know of a relevant reference for dTAG-13, please let us know.

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Literature in this Area

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