GNE-PROBE-1977 a chemical probe for TREX1.

The probe and control may be requested here.

overview

overview

Genentech in collaboration with the SGC have discovered the first chemical probe, GNE-PROBE-1977, for human three-prime repair exonuclease 1 (TREX1).

GNE-PROBE-1977 is exquisitely selective against TREX2 as well as DEDDH proteins. Further, the probe has sub-micromolar potency in a THP-1 IFN reporter assay.

We recommend its use in cell assays at a dosage of 500 nM. Please do not exceed a dosage of 2 µM (2000 nM).

*Please note that the probe is not recommended for use in animals. (It is predicted to have high clearance.)

properties

selectivity profile

in vitro potency

cell based assay data

references

pk properties

co-crystal structures

synthetic schemes

materials and methods

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Rafael Junqueira Borges

rjborges@unicamp.br

Av. Cândido Rondon, 400 - Cidade Universitária, Campinas - SP 13083-875

ORCID

Google Scholar

Affiliations

Principal Investigator in the Center For Medicinal Chemistry (CQMED) Researcher in the Center for Molecular Biology and Genetics Engineering (CBMEG) Universidade Estadual de Campinas (UNICAMP)

Group Profile

Biography

Rafael Junqueira Borges, PhD and specialist in Structural Biology, Bioinformatics and Method Development, is a Principal Investigator in the CQMED and the head of LaBEI/CBMEG/UNICAMP. His group integrates experimental and computational methods to understand protein structure and function, focusing on the search for modulators/inhibitors of therapeutic targets in the early phase of drug discovery. His group combines structural biology, biophysical and biochemical assays, mass spectrometry, phylogenetic analysis, structural bioinformatics, chemoinformatics, and artificial intelligence to elucidate structures, complexes, and sequences. We study proteins from natural sources, especially snake venom toxins, and cancer-related targets.