GNE-6640 (GNE6640) is a potent, selective and non-covalent USP7 inhibitor with IC50 of 0.75 uM.
GNE-6640 dislpalys selectivity over USP47 and USP5 (IC50>200 uM).
GNE-6640 promotes endogenous MDM2 ubiquitination, stabilized p53 and upregulated p21, induces tumour cell death and enhances cytotoxicity with chemotherapeutic agents and targeted compounds, including PIM kinase inhibitors.
GNE-6640 decreased viability of 108 cancer cell lines with IC50 <10 uM.
