| Identification | Back Directory | [Name]
b-AP15 | [CAS]
330450-45-8 | [Synonyms]
b-AP15
NSC-687852
NSC687852 >=98% (HPLC)
(3Z,5E)-1-Acryloyl-3,5-bis(4-nitrobenzylidene)-piperidin-4-one | [Molecular Formula]
C22H17N3O6 | [MDL Number]
MFCD25976718 | [MOL File]
330450-45-8.mol | [Molecular Weight]
419.39 |
| Hazard Information | Back Directory | [Uses]
(E/Z)-NSC-687852 is a isomer of NSC-687852 (HY-13989). NSC687852 (b-AP15) is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14[1]. | [Enzyme inhibitor]
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) | [References]
[1] Berndtsson M, et al. Induction of the lysosomal apoptosis pathway by inhibitors of the ubiquitin-proteasome system. Int J Cancer. 2009;124(6):1463-1469. DOI:10.1002/ijc.24004 |
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| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
bioleaper
|
| Tel: |
4000880777 17585207275 |
| Website: |
www.bioleaper.com/ |
| Company Name: |
Enzo Biochem Inc
|
| Tel: |
Enzo Biochem Inc. 13797054060 |
| Website: |
www.enzo.com |
|