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Biological Activity for aTAG 2139
aTAG 2139 is a degrader of MTH1 fusion proteins for use within the aTAG system. Comprises a ligand selective for MTH1, a linker and the cereblon-binding ligand Thalidomide (Cat. No. 0652). Induces highly potent and selective degradation of fusion proteins after a 4 h incubation (DC50 = 0.27 nM; Dmax = 92.1%). Cell-permeable. Suitable for in vitro and in vivo applications.
Negative control aTAG 2139-NEG (Cat. No. 7575) also available.
Mouse DMPK properties are provided in the supplementary file (see below).
MTH1 can be expressed as a fusion with a target protein of interest using genome engineering techniques via CRISPR-mediated locus-specific knock-in. See protocol for more information.
Custom knock-in cell lines for the dTAG and aTAG platforms are available from Bio-Techne.
Sold under exclusive license from C4 Therapeutics
Supplementary Information for aTAG 2139
Mouse DMPK properties are provided in the accompanying supplementary file.
Technical Data for aTAG 2139
|Storage||Store at -20°C|
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.
Solubility Data for aTAG 2139
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for aTAG 2139
The following data is based on the product molecular weight 782.81. 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.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||2.55 mL||12.77 mL||25.55 mL|
|2.5 mM||0.51 mL||2.55 mL||5.11 mL|
|5 mM||0.26 mL||1.28 mL||2.55 mL|
|25 mM||0.05 mL||0.26 mL||0.51 mL|
References for aTAG 2139
References are publications that support the biological activity of the product.
Veits et al (2021) Development of an AchillesTAG degradation system and its application to control CAR-T activity. Curr.Res.Chem.Biol. 1 100010
If you know of a relevant reference for aTAG 2139, please let us know.
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Citations for aTAG 2139
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Protocols for aTAG 2139
The following protocol features additional information for the use of aTAG 2139 (Cat. No. 6970).
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Targeted Protein Degradation Research Product Guide
This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Ubiquitin-Proteasome System Proteins
- Assays for Protein Degradation
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