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Submit ReviewdTAGV-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.
Sold under license from Dana-Farber Cancer Institute
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 136.16 | 100 |
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.
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 |
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
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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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