Biological Activity
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 assay, 2 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).
