b-AP15 Chemische Eigenschaften,Einsatz,Produktion Methoden
Enzyminhibitor
This deubiquitinase inhibitor (FW = 421.31 g/mol; CAS 1009817-63-3),
also named 3,5-bis[ (4-nitrophenyl) methylene]-1- (1-oxo-2-propen-1-yl) -
(3E,5E) -4-piperidinone, targets two proteasome-associated ubiquitin
carboxyl-terminal hydrolase-14, or USP14, and Ubiquitin Carboxyl-terminal
Hydrolase isozyme L5 UCHL5, IC50 = 2.1 μM, resulting in a rapid
accumulation of high-molecular-weight ubiquitin conjugates and functional
shutdown of proteasome. Interestingly, b-AP15 displays several differences
with respect to bortezomib including insensitivity to over-expression of the
anti-apoptotic mediator Bcl-2 and anti-tumor activity in solid tumor models.
Inhibition of DUBs blocked the processing and release of interleukin IL-1β
in both mouse and human macrophages. DUB activity was necessary for
inflammasome association as DUB inhibition also impaired ASC
oligomerization and caspase-1 activation without directly blocking caspase-
1 activity. These data reveal the requirement for DUB activity in a key
reaction of the innate immune response and highlight the therapeutic
potential of DUB inhibitors for chronic auto-inflammatory diseases. (See
also Bortezomib, Eeeyarestatin I)
b-AP15 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
