Oct 18, 2017 · FT827 features a vinylsulfonamide moiety that covalently modifies the catalytic Cys223 of USP7 and inhibits the enzyme with an enzyme inactivation rate (kinact) to inhibition constant (Ki)...

One of the inhibitors, FT827, carries vinylsulfonamide moiety, which reaches the catalytic triad and covalently modifies the catalytic cysteine. All other reported USP7 inhibitors are non-covalent.

Oct 26, 2017 · Here we report that two compounds, FT671 and FT827, inhibit USP7 with high affinity and specificity in vitro and within human cells. Co-crystal structures reveal that both compounds target a dynamic pocket near the catalytic centre of the auto-inhibited apo form of USP7, which differs from other USP deubiquitinases.

FT-827: a USP7 inhibitors Drug, Initially developed by FORMA Therapeutics, Inc., Now, its global highest R&D status is Pending, Mechanism: USP7 inhibitors (ubiquitin specific peptidase 7 inhibitors), Therapeutic Areas: Neoplasms.

Use of FT-827 FT827 is a selective and covalent ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 52 nM.

FT827 is a selective and covalent ubiquitin-specific protease 7 (USP7) inhibitor (Ki=4.2 µM). FT827 binds to the USP7 catalytic domain (USP7CD; residues 208-560) with an apparent Kd value of 7.8 µM.

FT827 is a novel potent and selective covalent USP7 inhibitor.