USP21-in6 is a potent, specific inhibitor of deubiquitinase ubiquitin-specific peptidase 21 (USP21) with IC50 of 0.61 uM and Kd of 1.3 uM.
USP21-in6 also inhibits USP2, USP5, USP7, and USP15 (IC50 values of 2.48, 3.30, 3.71, and 3.21 uM, respectively), while exhibiting no significant activity against USP3, USP9X, USP14, USP22, USP27, OTUB1 or OTUD5 at 30 uM.
USP21-in6 reduces USP21-mediated cleavage of di-ubiquitin to mono-ubiquitin, potently and selectively inhibits NSCLC cell proliferation.
USP21-in6 inhibits the proliferation, migration, and invasion of NSCLC cells and induces cell apoptosis by targeting USP21.
USP21-in6 inhibits de novo fatty acid synthesis in NSCLC cells in a concentration-dependent manner.
USP21-in6 disrupts SCD1 stability by inhibiting USP21-mediated stabilization.
USP21-in6 (10-20 mg/kg) inhibits NSCLC in LLC tumor-bearing mice, enhances anti-tumor immunity in LLC tumor-bearing mice.