XL177A is a highly potent and selective irreversible USP7 inhibitor with an IC50 of 0.34 nM, demonstrating cancer cell killing through a p53-dependent mechanism. It acts as a potent USP7 inhibitor and p53 stabilizer in vitro, effectively suppressing cancer cell growth. The compound selectively labels the catalytic cysteine, C223, of USP7 across the DUBome and human proteome.
- Highly potent and selective irreversible USP7 inhibitor (IC50 of 0.34 nM).
- Elicits cancer cell killing via a p53-dependent mechanism.
- Suppresses cancer cell growth predominantly through p53-dependent pathways.
- Labels USP7's catalytic cysteine (C223) with exquisite selectivity.
- Induces complete G1 arrest in MCF7 cells after 24 hours (at 1 μM).
- Promotes rapid degradation of HDM2, increasing p53 and p21 protein levels in MCF7 cells.