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
Biological ActivityaTAG 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.
Supplementary InformationMouse DMPK properties are provided in the accompanying supplementary file.
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.
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