2925481-88-3

BAY-805 is a selective inhibitor of ubiquitin-specific protease USP21. BAY-805 has high selectivity for deubiquitinating enzyme (DUB) targets, kinases, proteases and other common target enzymes[1].

Potent and selective dual USP21 deubiquitinase (DUB) inhibitor with anti-cancer efficacy.

BAY-805 is a higly potent and selective USP21 deubiquitinase (DUBs) inhibitor (IC50 (Emax) = 6 nM (95%) by HTRF assay2 nM (87%) by Ub-Rh110 assay; Kd = 2.2 nM by SPR-based competition assay; 50/53% inhibition of USP10/USP22 at 10 μM<31% inhibition against other DUBs) th at effectively upregulates cellular NF-KB activation (7-fold increase at 10 μM 20h post BAY-805 treatment by HEK293T-based reporter assay) with good target engagement (EC50 = 17 nM by USP21 HiBiT CESTA assay).

[1] G?ricke F, et al. Discovery and Characterization of BAY-805, a Potent and Selective Inhibitor of Ubiquitin-Specific Protease USP21. J Med Chem. 2023 Feb 20. DOI:10.1021/acs.jmedchem.2c01933