FKBP12 PROTAC dTAG-7 - CAS 2064175-32-0

FKBP12 PROTAC dTAG-7 is a bifunctional PROTAC® degrader inducing the selective degradation of FKBP12F36V fusion proteins and BET BRD4, consisting of a ligand selective for F36V single-point mutated FKBP12 conjugated to a cereblon ligand by a linker.

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Molecular Formula
Molecular Weight


    • Specification
      • Purity
        Soluble in DMSO, Ethanol
        Off-white Solid
        Store at -20°C
        Room temperature in continental US; may vary elsewhere.
        IUPAC Name
        [(1R)-3-(3,4-dimethoxyphenyl)-1-[2-[2-[3-[2-[2-[3-[[2-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]oxyacetyl]amino]propoxy]ethoxy]ethoxy]propylamino]-2-oxoethoxy]phenyl]propyl] (2S)-1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidine-2-carboxylate
        (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; 2-Piperidinecarboxylic acid, 1-[(2S)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-, (1R)-3-(3,4-dimethoxyphenyl)-1-[2-[[19-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-2,18-dioxo-7,10,13-trioxa-3,17-diazanonadec-1-yl]oxy]phenyl]propyl ester, (2S)-; (1R)-3-(3,4-Dimethoxyphenyl)-1-[2-[[19-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-2,18-dioxo-7,10,13-trioxa-3,17-diazanonadec-1-yl]oxy]phenyl]propyl (2S)-1-[(2S)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-2-piperidinecarboxylate; dTAG-7
    • Properties
      • Boiling Point
        1242.1±65.0°C at 760 Torr
        1.265±0.06 g/cm3
        InChI Key
        Canonical SMILES
        Pub Chem ID
    • Reference Reading
      • 1. The dTAG system for immediate and target-specific protein degradation.
        Nabet, B., Roberts, J.M., Buckley, D.L., Paulk, J., Dastjerdi, S., Yang, A., Leggett, A.L., Erb, M.A., Lawlor, M.A., Souza, A. and Scott, T.G., 2018. Nature chemical biology, 14(5), pp.431-441.
        Dissection of complex biological systems requires target-specific control of the function or abundance of proteins. Genetic perturbations are limited by off-target effects, multicomponent complexity, and irreversibility. Most limiting is the requisite delay between modulation to experimental measurement. To enable the immediate and selective control of single protein abundance, we created a chemical biology system that leverages the potency of cell-permeable heterobifunctional degraders. The dTAG system pairs a novel degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. By transgene expression or CRISPR-mediated locus-specific knock-in, we exemplify a generalizable strategy to study the immediate consequence of protein loss. Using dTAG, we observe an unexpected superior antiproliferative effect of pan-BET bromodomain degradation over selective BRD4 degradation, characterize immediate effects of KRASG12V loss on proteomic signaling, and demonstrate rapid degradation in vivo. This technology platform will confer kinetic resolution to biological investigation and provide target validation in the context of drug discovery.
    • Preparing Stock Solutions
      • ConcentrationVolumeMass1 mg5 mg10 mg
        1 mM0.83 mL4.13 mL8.26 mL
        5 mM0.17 mL0.83 mL1.65 mL
        10 mM0.08 mL0.41 mL0.83 mL
        50 mM0.02 mL0.08 mL0.17 mL
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Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
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