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dTAG-13

Cat. No. 6605 21 篇引用文献 4 条评论 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Degrades mutant FKBP12F36V fusion proteins; useful alternative to genetic methods for target validation
化学名： 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
纯度： ≥98% (HPLC)
说明书
引用文献 (21)
评论 (4)
文献 (3)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for dTAG-13

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.

许可信息

Sold under license from Dana-Farber Cancer Institute

技术数据 for dTAG-13

分子量 1049.18
公式 C57H68N4O15
储存 Store at -20°C
纯度 ≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for dTAG-13

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 52.46 50
ethanol 20.98 20

制备储备液 for dTAG-13

以下数据基于产品分子量 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 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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产品说明书 for dTAG-13

分析证书/产品说明书
选择另一批次：
化学品安全技术说明书

参考文献 for dTAG-13

参考文献是支持产品生物活性的出版物。

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

Bensimon et al (2020) Targeted degradation of SLC transporters reveals amenability of multi-pass transmembrane proteins to ligand-induced proteolysis. Cell Chem.Biol. 27 728 PMID: 32386596

Abuhashem et al (2022) Generation of knock-in degron tags for endogenous proteins in mice using the dTAG system. STAR Protoc. 3 101660 PMID: 36097386

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

按标靶查看相关产品

关键词: dTAG-13, dTAG-13 supplier, dTAG13, degraders, degrades, degradation, FKBP12F36V, fusion, protein, mutant, PROTAC, proteolysis, targeting, chimera, cereblon, PROTACs, in, vivo, TAG, Degradation, Platform, 6605, Tocris Bioscience

21 篇 dTAG-13 的引用文献

引用文献是使用了 Tocris 产品的出版物。 dTAG-13 的部分引用包括：

Yuan et al (2022) Effective Menin inhibitor-based combinations against AML with MLL rearrangement or NPM1 mutation (NPM1c). Blood Cancer J 12 5 PMID: 35017466

Daniel A et al (2022) A ubiquitin-independent proteasome pathway controls activation of the CARD8 inflammasome. J Biol Chem 298 102032 PMID: 35580636

Francisca et al (2022) Systematic profiling of conditional degron tag technologies for target validation studies. Nat Commun 13 5495 PMID: 36127368

Rafael et al (2022) BRD2 compartmentalizes the accessible genome. Nat Genet 54 481-491 PMID: 35410381

Fei et al (2022) Regulation of cohesin-mediated chromosome folding by PDS5 in mammals. EMBO Rep 23 e54853 PMID: 36129789

Xin et al (2022) A TET1-PSPC1-Neat1 molecular axis modulates PRC2 functions in controlling stem cell bivalency. Cell Rep 39 110928 PMID: 35675764

Anja et al (2022) NASP maintains histone H3-H4 homeostasis through two distinct H3 binding modes. Nucleic Acids Res 50 5349-5368 PMID: 35489058

Neil et al (2022) Xist-mediated silencing requires additive functions of SPEN and Polycomb together with differentiation-dependent recruitment of SmcHD1. Cell Rep 39 110830 PMID: 35584662

Anna-Katerina et al (2022) Generation of knock-in degron tags for endogenous proteins in mice using the dTAG system. STAR Protoc 3 101660 PMID: 36097386

Tibor et al (2022) The histone methyltransferase SETD2 negatively regulates cell size. J Cell Sci 135 PMID: 36052643

Ma et al (2023) Engineered PROTAC-CID systems for mammalian inducible gene regulation. J Am Chem Soc 145 1593 PMID: 36626587

Orth-He et al (2023) Protein folding stress potentiates NLRP1 and CARD8 inflammasome activation. Cell Rep 42 111965 PMID: 36649711

Rutger A F et al (2023) CasTuner is a degron and CRISPR/Cas-based toolkit for analog tuning of endogenous gene expression. Nat Commun 14 3225 PMID: 37270532

Cristian et al (2023) MYC regulates CSF-1 expression via microRNA 17/20a to modulate tumor-associated macrophages in osteosarcoma. JCI Insight PMID: 37279073

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

Sahillioglu et al (2021) CRASH-IT switch enables reversible and dose-dependent control of TCR and CAR T-cell function. Cancer Immunol.Res. 9 999 PMID: 34193461

Kristian et al (2021) Generation of locus-specific degradable tag knock-ins in mouse and human cell lines. STAR Protoc 2 100575 PMID: 34151298

Hao et al (2021) Dipeptidyl peptidase 9 sets a threshold for CARD8 inflammasome formation by sequestering its active C-terminal fragment. Immunity 54 1392-1404.e10 PMID: 34019797

William P et al (2021) Gene-specific quantification of nascent transcription following targeted degradation of endogenous proteins in cultured cells. STAR Protoc 2 101000 PMID: 34917979

Abuhashem et al (2022) Generation of knock-in degron tags for endogenous proteins in mice using the dTAG system. STAR Protoc. 3 101660 PMID: 36097386

Xavier et al (2019) An efficient auxin-inducible degron system with low basal degradation in human cells. Nat Methods 16 866-869 PMID: 31451765

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Degradation of Myc fusion protein.
By Bikesh Nirala on 06/21/2022
分析类型： In Vitro
种属： Mouse
细胞系/组织： Murine cell lines

I tested this product to degrade FFKBP12-Myc protein. It is working nicely.

review image
dTAG-13 treatment of FKBP tagged over expressed protein in glioma cell lines.
By Anonymous on 07/02/2020
分析类型： In Vitro
种属： Human
细胞系/组织： 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

review image
Knockdown of FKBP-tagged Chromatin Protein.
By Sam Weeks on 01/30/2020
分析类型： In Vitro
种属： Mouse
细胞系/组织： 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.

review image
Works better than expected.
By Abderhman Abuhashem on 10/14/2019
分析类型： In Vitro
种属： Mouse
细胞系/组织： 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.

review image

该领域的文献

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。

TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia

Validating Targets for TPD Using dTAG Poster

Validating Targets for TPD Using dTAG Poster

The dTAG platform offers a generalizable strategy to degrade, in principle, any intracellular protein of interest (POI) and is a useful strategy for exploration and validation of targets. This poster presents a workflow solution for target validation, from custom TAG knock-in cell-lines for your POI, different dTAG Degraders to knockdown you POI, to automated assays for protein degradation using Simple WesternTM instruments. Data are also presented on the use of an antibody that recognizes the TAG domain (FKBP12F36V) for detection of degradation. Presented at TPD Europe, March 2022, London, UK.