dTAGV-1

Pricing Availability   Qty
说明: Potent and selective degrader of mutant FKBP12F36V fusion proteins
化学名: (R)-3-(3,4-Dimethoxyphenyl)-1-(2-(2-((7-(((S)-1-((2S,4R)-4-hydroxy-2-(((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-7-oxoheptyl)amino)-2-oxoethoxy)phenyl)propyl (S)-1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate trifluoroacetate
纯度: ≥98% (HPLC)
说明书
引用文献 (7)
评论 (1)
文献 (3)

生物活性 for dTAGV-1

dTAGV-1 is a degrader targeting mutant FKBP12F36V fusion proteins. Comprises a ligand selective for F36V single-point mutated FKBP12, a linker and a von Hippel-Lindau (VHL)-binding ligand. Induces potent and selective degradation of FKBP12F36V fusion proteins in vitro and in vivo. Selectively degrades FKBP12F36V-EWS/FLI fusion proteins and inhibits cell proliferation in FKBP12F36V-EWS/FLI-expressing Ewing sarcoma cells.

Hydrochloride salt (Cat.No. 7374) available; suitable for in vivo use.

Negative control dTAGV-1-NEG (Cat. No. 6915) 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 dTAGV-1

分子量 1361.58
公式 C68H90N6O14S CF3CO2H
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2624313-15-9
InChI Key KSEWNBIDXKMTNT-LNVAYBNASA-N
Smiles C[C@H](NC([C@@H]1C[C@@H](O)CN1C([C@@H](NC(CCCCCCNC(COC2=CC=CC=C2[C@H](OC([C@@H]3CCCCN3C([C@@H](CC)C4=CC(OC)=C(OC)C(OC)=C4)=O)=O)CCC5=CC(OC)=C(OC)C=C5)=O)=O)C(C)(C)C)=O)=O)C6=CC=C(C=C6)C7=C(N=CS7)C.OC(C(F)(F)F)=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 dTAGV-1

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 136.16 100

制备储备液 for dTAGV-1

以下数据基于产品分子量 1361.58。 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
1 mM 0.73 mL 3.67 mL 7.34 mL
5 mM 0.15 mL 0.73 mL 1.47 mL
10 mM 0.07 mL 0.37 mL 0.73 mL
50 mM 0.01 mL 0.07 mL 0.15 mL

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产品说明书 for dTAGV-1

分析证书/产品说明书
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参考文献 for dTAGV-1

参考文献是支持产品生物活性的出版物。

Nabet et al (2020) Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules. Nat.Commun. 11 4687 PMID: 32948771

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 dTAGV-1, please let us know.

关键词: dTAGV-1, dTAGV-1 supplier, 2451573-86-5, dTAGVHL1, degraders, degrades, targeted, protein, degradation, FKBP12F36V, fusion, mutant, PROTAC, VHL, von, Hippel, Lindau, TPD, in, vivo, TAG, Degradation, Platform, 6914, Tocris Bioscience

7 篇 dTAGV-1 的引用文献

引用文献是使用了 Tocris 产品的出版物。 dTAGV-1 的部分引用包括:

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

Tomek et al (2023) Precise modulation of transcription factor levels identifies features underlying dosage sensitivity. Nat Genet 55 841-851 PMID: 37024583

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

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

Tom et al (2022) Control of ribosomal RNA synthesis by hematopoietic transcription factors. Mol Cell 82 3826-3839.e9 PMID: 36113481

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

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


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dTAGV-1 Treatment.
By Anonymous on 05/28/2024
分析类型: In Vitro
种属: Human

1uM treatment used to knockdown target protein for downstream mechanistic analysis, quick and easy resuspension and treatment works for effective knockdown in as little as 24 hours

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.