XL177A (XL-177A) is a potent, selective, irreversible USP7 inhibitor with IC50 of 0.34 nM.
XL177A inhibits HA-Ub-VS labeling with IC50s of 85 and 8 nM following 30min and 4hr compound preincubations, respectively。
XL177A is a potent USP7 inhibitor (IC50=39 nM) and p53 stabilizer in cyto.
XL177A binds USP7 in the XL188 binding pocket, XL177A binds to and inhibits USP7 with >10-fold selectivity over closely related DUBs.
XL177A activates p53 signaling transcriptome-wide in MCF7 cells. XL177A exerts p53-dependent growth suppression in individual cell lines.
