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Submit ReviewdTAG-7 is a first generation Degrader for mutant FKBP12F36V fusion proteins. Comprises a ligand selective for F36V single-point mutated FKBP12, a linker and a cereblon-binding ligand. 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. See also dTAG-13.
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.
Sold under license from Dana-Farber Cancer Institute
TAG Domain | FKBP12F36V |
Warhead | Ortho-AP1867 |
E3 Ligase | Cereblon |
分子量 | 1210.32 |
公式 | C63H79N5O19 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 2064175-32-0 |
PubChem ID | 131954816 |
InChI Key | IFCAWDLUIZXIPI-FJDAOBEISA-N |
Smiles | CC[C@H](C(=O)N1CCCC[C@H]1C(=O)O[C@H](CCC1=CC(OC)=C(OC)C=C1)C1=C(OCC(=O)NCCCOCCOCCOCCCNC(=O)COC2=C3C(=O)N(C4CCC(=O)NC4=O)C(=O)C3=CC=C2)C=CC=C1)C1=CC(OC)=C(OC)C(OC)=C1 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 121.03 | 100 | |
ethanol | 24.21 | 20 |
以下数据基于产品分子量 1210.32。 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.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 0.83 mL | 4.13 mL | 8.26 mL |
5 mM | 0.17 mL | 0.83 mL | 1.65 mL |
10 mM | 0.08 mL | 0.41 mL | 0.83 mL |
50 mM | 0.02 mL | 0.08 mL | 0.17 mL |
参考文献是支持产品生物活性的出版物。
Moser et al (2018) Acute pharmacologic degradation of a stable antigen enhances its direct presentation on MHC class I molecules. Front.Immunol. 8 1920 PMID: 29358938
Nabet et al (2018) The dTAG system for immediate and target-specific protein degradation. Nat.Chem.Biol. 14 431 PMID: 29581585
Huang et al (2018) A chemoproteomic approach to query the degradable kinome using a multi-kinase degrader. Cell Chem.Biol. 25 88 PMID: 29129717
Yesbolatova et al (2018) TAGing for destruction. Nat.Chem.Biol. 14 414 PMID: 29581583
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
If you know of a relevant reference for dTAG-7, please let us know.
关键词: dTAG-7, dTAG-7 supplier, dTAG7, dFKBP7, degraders, degrades, degradation, FKBP12F36V, fusion, protein, mutant, PROTACs, proteolysis, targeting, chimera, TAG, Degradation, Platform, 6912, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 dTAG-7 的部分引用包括:
Ma et al (2023) Engineered PROTAC-CID systems for mammalian inducible gene regulation J Am Chem Soc PMID: 36626587
David et al (2020) SON and SRRM2 are essential for nuclear speckle formation. Elife 9 PMID: 33095160
Cugusi et al (2022) Heat shock induces premature transcript termination and reconfigures the human transcriptome. Mol.Cell 82 1573 PMID: 35114099
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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。
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
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