XL177A is a highly potent and selective irreversible USP7 inhibitor with an IC50 of 0.34?nM. XL177A elicits cancer cell killing through a p53-dependent mechanism.In Vitro: XL177A is a potent USP7 inhibitor and p53 stabilizer in cyto. XL177A suppresses cancer cell growth predominantly through a p53-dependent mechanism. XL177A labels the catalytic cysteine, C223, of USP7 with exquisite selectivity for USP7 across the DUBome and human proteome.
XL177A (1 μM) induces complete G1 arrest in MCF7 cells after 24?hours.
Treatment of MCF7 cells, which express WT TP53, with XL177A (0.001- 10 μM) induces rapid degradation of HDM2 within 2?hours, followed by increases in p53 and downstream p21 protein levels.