GNE-6776 is a novel potent, specific, non-covalent, orally bioavailable USP7 inhibitor with IC50 of 1.34 uM.
GNE-6776 dislpalys selectivity over USP47 and USP5 (>200 uM).
GNE-6776 promotes endogenous MDM2 ubiquitination, stabilized p53 and upregulated p21, induces tumour cell death and enhances cytotoxicity with chemotherapeutic agents.
GNE-6776 promotes on-target pathway modulation in human xenografts.
