FT-671 is a novel potent, specific, non-covalent USP7 inhibitor with Kd of 65 nM (USP7 catalytic domain).
FT-671 inhibits USP7 with IC50 values of 52 nM (USP7 CD) and 69 nM (USP7C-term), display good USP7 selectivity in a panel of 38 deubiquitinases (DUBs).
FT-671 destabilizes USP7 substrates including MDM2, increases levels of p53, and results in the transcription of p53 target genes and induces tumour suppressor p21.
FT-671 blocks the proliferation of MM.1S cells (IC50=33 nM), suppresses tumour growth in mice; orally available.
