USP7-IN-4

(R)-USP-IN-4 is a highly potent, selective, allosteric USP7 inhibitor with IC50 of 6 nM in FP assays; also shows high potency in an alternative assay using the Ub-Rh110 substrate (IC50=1.5 nM) and Kd of 2.0 nM; displays high selectivuty against other DUBs, proteases and kinases; demonstrates highly potent target engagement in cells (EC50=49 nM), with no off-target activity against USP47, causes nongenotoxic stabilization of p53 and decreased levels of MDM2 in HCT116 cells.

References 1. Gavory G, et al. Nat Chem Biol. 2018 Feb;14(2):118-125. View Related Products by Target Deubiquitinase (DUB)