BAY-805 Chemical probe for USP21

This probe is available from Sigma and Tocris, and the control may be requested here.

overview
properties
in vitro potency
cell based assay data
references

overview

Probe		Negative control

BAY-805		BAY-728

Bayer in collaboration with the SGC has developed a first-in-class chemical probe BAY-805 for USP21. BAY-805 inhibits USP21 with IC₅₀ < 10 nM in HTRF and Ub-Rhodamine assays. BAY-728 is a closely related negative control with IC₅₀ > 12 micromolar.

properties

Probe		Negative control

BAY-805		BAY-728

BAY-805 is selective for USP21 in a Ub-Rhodamine assay.

selectivity profile

in vitro potency

cell based assay data

BAY-805 binds USP21 in a HiBiT based target engagement assay with an EC₅₀ = 95 nM.

references

1. Discovery and Characterization of BAY-805, a Potent and Selective Inhibitor of Ubiquitin-Specific Protease USP21. Fabian Göricke, Victoria Vu, Leanna Smith, Ulrike Scheib, Raphael Böhm, Namik Akkilic, Gerd Wohlfahrt, Jörg Weiske, Ulf Bömer, Krzysztof Brzezinka, Niels Lindner, Philip Lienau, Stefan Gradl, Hartmut Beck, Peter J. Brown, Vijayaratnam Santhakumar, Masoud Vedadi, Dalia Barsyte-Lovejoy, Cheryl H. Arrowsmith, Norbert Schmees, and Kirstin Petersen. https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.2c01933

pk properties

co-crystal structures

synthetic schemes

materials and methods