Proteasome-associated deubiquitinases (DUBs) release ubiquitin from proteasome-targeted ubiquitinated proteins, regenerating free ubiquitin.{25593} b-AP15 is an inhibitor of ubiquitin-specific-processing protease 14 (USP14) and ubiquitin carboxyl-terminal hydrolase isozyme L5 (UCHL5), two proteasome-associated DUBs.{20322} It inhibits DUB activity in purified 19S proteasomes with an IC50 value of 2.1 ?M.{20322} It exhibits little or no activity against several other DUBs.{20322} Through its effects on USP14 and UCHL5, b-AP15 blocks tumor progression in vivo in mice and prevents organ infiltration in mouse models of myeloid leukemia.{20322,25591} b-AP15 also renders tumor cells sensitive to TNF-mediated apoptosis by natural killer and T cells.{25592}
产品描述
An inhibitor of USP14 and UCHL5, two proteasome-associated deubiquitinases; inhibits DUB activity in purified 19S proteasomes with an IC50 value of 2.1 ?M; blocks tumor progression in vivo in mice and prevents organ infiltration in mouse models of myeloid leukemia
