FT206 (FT-206, FT3951206, CRT0511973) is a potent, selectivel inhibitor of USP28 with a remarkable USP28/25 selectivity.
FT206 interferes with USP28/25 probe labelling (USP-ABP versus USP) in LSCC H520 cell extracts with EC50 of 0.3-1 uM.
USP28 inhibition causes apoptotic cell death of LSCC tumour cells.
FT206 also resulted in reduced Δp63, c-JUN, and c-MYC protein levels, causes dramatic regression of human LSCC xenograft tumours in vivo.
