dTAG-13
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%
Biological Activity
dTAG-13 is a degrader targeting mutant FKBP12F36V 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 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.Negative control (Cat. No. 6916) also available.
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.
Plasmid vectors for the lentiviral expression and CRISPR-mediated knock-in of FKBP12F36V are available from Addgene.
Technical Data
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.
Additional Information
Background References
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The dTAG system for immediate and target-specific protein degradation.
Nabet et al.
Nat.Chem.Biol., 2018;14:431 -
Transcription control by the ENL YEATS domain in acute leukaemia.
Erb et al.
Nature., 2017;543:270 -
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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Citations for dTAG-13
The citations listed below are publications that use Tocris products. Selected citations for dTAG-13 include:
22 Citations: Showing 1 - 10
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Protein folding stress potentiates NLRP1 and CARD8 inflammasome activation.
Authors: Orth-He Et al.
Cell Rep 2023;42:111965
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CasTuner is a degron and CRISPR/Cas-based toolkit for analog tuning of endogenous gene expression.
Authors: Rutger A F Et al.
Nat Commun 2023;14:3225
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Engineered PROTAC-CID systems for mammalian inducible gene regulation.
Authors: Ma Et al.
J Am Chem Soc 2023;145:1593
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MYC regulates CSF-1 expression via microRNA 17/20a to modulate tumor-associated macrophages in osteosarcoma.
Authors: Cristian Et al.
JCI Insight 2023;
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BRD2 compartmentalizes the accessible genome.
Authors: Rafael Et al.
Nat Genet 2022;54:481-491
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NASP maintains histone H3-H4 homeostasis through two distinct H3 binding modes.
Authors: Anja Et al.
Nucleic Acids Res 2022;50:5349-5368
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Generation of knock-in degron tags for endogenous proteins in mice using the dTAG system.
Authors: Abuhashem Et al.
STAR Protoc. 2022;3:101660
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Generation of knock-in degron tags for endogenous proteins in mice using the dTAG system.
Authors: Anna-Katerina Et al.
STAR Protoc 2022;3:101660
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A TET1-PSPC1-Neat1 molecular axis modulates PRC2 functions in controlling stem cell bivalency.
Authors: Xin Et al.
Cell Rep 2022;39:110928
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Xist-mediated silencing requires additive functions of SPEN and Polycomb together with differentiation-dependent recruitment of SmcHD1.
Authors: Neil Et al.
Cell Rep 2022;39:110830
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A ubiquitin-independent proteasome pathway controls activation of the CARD8 inflammasome.
Authors: Daniel A Et al.
J Biol Chem 2022;298:102032
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Regulation of cohesin-mediated chromosome folding by PDS5 in mammals.
Authors: Fei Et al.
EMBO Rep 2022;23:e54853
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Systematic profiling of conditional degron tag technologies for target validation studies.
Authors: Francisca Et al.
Nat Commun 2022;13:5495
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The histone methyltransferase SETD2 negatively regulates cell size.
Authors: Tibor Et al.
J Cell Sci 2022;135
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Effective Menin inhibitor-based combinations against AML with MLL rearrangement or NPM1 mutation (NPM1c).
Authors: Yuan Et al.
Blood Cancer J 2022;12:5
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CRASH-IT switch enables reversible and dose-dependent control of TCR and CAR T-cell function.
Authors: Sahillioglu Et al.
Cancer Immunol.Res. 2021;9:999
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Dipeptidyl peptidase 9 sets a threshold for CARD8 inflammasome formation by sequestering its active C-terminal fragment.
Authors: Hao Et al.
Immunity 2021;54:1392-1404.e10
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Gene-specific quantification of nascent transcription following targeted degradation of endogenous proteins in cultured cells.
Authors: William P Et al.
STAR Protoc 2021;2:101000
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Generation of locus-specific degradable tag knock-ins in mouse and human cell lines.
Authors: Kristian Et al.
STAR Protoc 2021;2:100575
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Characterization of cereblon-dependent targeted protein degrader by visualizing the spatiotemporal ternary complex formation in cells
Authors: Kaji Et al.
Sci.Rep. 2020;10:3088
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An efficient auxin-inducible degron system with low basal degradation in human cells.
Authors: Xavier Et al.
Nat Methods 2019;16:866-869
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