| Company Name: |
MedChemexpress LLC
|
| Tel: |
021-58955995 |
| Email: |
sales@medchemexpress.cn |
| Products Intro: |
Product Name:b-AP15
CAS:330450-45-8
|
| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Email: |
eric_feng1954@126.com |
| Products Intro: |
Product Name:NSC-687852
CAS:330450-45-8
Purity:95% -98%HPLC Package:1GR;10GR;50GR;100GR;250GR;500GR;1KG;5KG;10KG;100KG
|
| Company Name: |
Tianjin Kailiqi Biotechnology Co., Ltd.
|
| Tel: |
15076683720 |
| Email: |
klq@cw-bio.com |
| Products Intro: |
Product Name:B-AP15
CAS:330450-45-8
Purity:大于98% Package:1g,5g,10g,25g根据客户需要分装 Remarks:Not For Human Use, Lab Use Only.
|
|
| Product Name: | b-AP15 | | Synonyms: | b-AP15;NSC-687852;(3Z,5E)-1-Acryloyl-3,5-bis(4-nitrobenzylidene)-piperidin-4-one;NSC687852 >=98% (HPLC);4-Piperidinone, 3,5-bis[(4-nitrophenyl)methylene]-1-(1-oxo-2-propen-1-yl)- | | CAS: | 330450-45-8 | | MF: | C22H17N3O6 | | MW: | 419.39 | | EINECS: | | | Product Categories: | | | Mol File: | 330450-45-8.mol |  |
| | b-AP15 Chemical Properties |
| Boiling point | 670.4±55.0 °C(Predicted) | | density | 1.416±0.06 g/cm3(Predicted) | | pka | -1.39±0.20(Predicted) |
| | b-AP15 Usage And Synthesis |
| 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) |
| | b-AP15 Preparation Products And Raw materials |
|