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
Biological ActivityFirst generation Degrader/PROTAC for mutant FKBP12F36V fusion proteins. Comprises a ligand selective for F36V single-point mutated FKBP12, a linker and a cereblon-binding ligand. 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-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. Also see dTAG-13.
Plasmid vectors for the lentiviral expression and CRISPR-mediated knock-in of FKBP12F36V are available from Addgene.
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.
A chemoproteomic approach to query the degradable kinome using a multi-kinase degrader.
Huang et al.
Cell Chem.Biol., 2018;25:88
The dTAG system for immediate and target-specific protein degradation.
Nabet et al.
Transcription control by the ENL YEATS domain in acute leukaemia.
Erb et al.
Acute pharmacologic degradation of a stable antigen enhances its direct presentation on MHC class I molecules.
Moser et al.
TAGing for destruction.
Yesbolatova et al.
Targeted degradation of SLC transporters reveals amenability of multi-pass transmembrane proteins to ligand-induced proteolysis.
Bensimon et al.
Cell Chem.Biol., 2020;27
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