aTAG 2139

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Cat.No. 6970 - aTAG 2139 | C42H38N8O8 | CAS No. 2387510-81-6
Description: Degrader of MTH1 fusion proteins for use within the aTAG system
Alternative Names: CFT 2139
Chemical Name: 6-(6-((4-(2-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamido)butyl)carbamoyl)pyridin-3-yl)-N-methyl-4-(phenylamino)quinoline-3-carboxamide
Purity: ≥98% (HPLC)
Protocols (1)
Literature (2)

Biological Activity

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.

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 our sister brand R&D Systems. Email to enquire.

Licensing Information

Sold under exclusive license from C4 Therapeutics

Mouse DMPK properties are provided in the accompanying supplementary file.

Technical Data

M. Wt 782.81
Formula C42H38N8O8
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2387510-81-6
Smiles O=C(CCC1N2C(C3=C(C(OCC(NCCCCNC(C4=CC=C(C5=CC=C(N=CC(C(NC)=O)=C6NC7=CC=CC=C7)C6=C5)C=N4)=O)=O)=CC=C3)C2=O)=O)NC1=O

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

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 39.14 50

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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

Molarity Calculator

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

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References are publications that support the biological activity of the product.

If you know of a relevant reference for aTAG 2139, please let us know.

Keywords: aTAG 2139, aTAG 2139 supplier, aTAG2139, CFT2139, atag, Achilles, heel, degraders, degradation, MTH1, fusion, protein, PROTAC, proteolysis, targeting, chimeras, targeted, TPD, CFT, 2139, TAG, Degradation, Platform, 6970, Tocris Bioscience

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

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
  • Degrader Building Blocks
  • Custom Degrader Services
  • UPS Proteins and Assays
  • Assays for Protein Degradation
Targeted 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