FT827 is a selective and covalent inhibitor of ubiquitin-specific protease 7 (USP7) (Ki: 4.2 μM). FT827 binds to the USP7 catalytic domain (apparent Kd: 7.8 μM).

FT827 exclusively inhibits USP7 in a panel of 38 deubiquitinases (DUBs) from diverse families. FT827 features a vinyl sulfonamide moiety that covalently modifies the catalytic Cys223 of USP7. FT827 inhibits USP7 probe reactivity (IC50s: 0.1-2 μM), confirming 10 to 100-fold higher potency as compared to P22077 in crude cell extracts or with intact MCF7 breast cancer cells. Followed by incubation with the ubiquitin active site suicide probe haemagglutinin (HA)-tagged ubiquitin bromomethyl (HA-UbC2Br).

1959537-86-0

C27H28N6O5S

548.61

DMSO:125 mg/mL (227.85 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years