Chemical Structure : Pneumolysin inhibitor PB-3
CAS No.:
330842-49-4
Pneumolysin inhibitor PB-3
(PLY inhibitor PB-3)
货号: PC-22242Not For Human Use, Lab Use Only.
Pneumolysin inhibitor PB-3 is a specific small molecule inhibitor (pore-blocker) of pneumolysin (PLY), binds to Cys428 adjacent to the cholesterol recognition domain of PLY with KD of 256 nM, block the PLY-induced hemoglobin release in sheep erythrocytes with IC50 of 3.1 uM.
大包装，大折扣！
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
纯度 & COA & 质检文件 纯度:
>98% (HPLC)
生物&药学活性
Pneumolysin inhibitor PB-3 is a specific small molecule inhibitor (pore-blocker) of pneumolysin (PLY), binds to Cys428 adjacent to the cholesterol recognition domain of PLY with KD of 256 nM, block the PLY-induced hemoglobin release in sheep erythrocytes with IC50 of 3.1 uM.
PB-3 shows an IC50 value of 0.22 µM against PLY in presence of 2.5% human serum in the hemolysis assay.
PB-3 (6 uM) exhibits significant concentration-dependent inhibition of PLY and prevented more than 95% of cellular damage in PLY-induced cellular damage in human alveolar epithelial cells (A549 cells).
PB-3 does not inhibit cysteine protease SARS-CoV2 main protease and cysteine-containing protein tyrosine phosphatase PTP1B, as well as perforin.
PB-3 protects human lung cells from wild-type PLY during infection with Streptococcus pneumoniae
PB-3 acts as anti-virulence factor preventing human lung epithelial cells from PLY-mediated cytolysis and cell death during infection with Streptococcus pneumoniae and is active against the homologous Cys-containing CDC perfringolysin (PFO) as well.
Pneumolysin (PLY) is a cholesterol-dependent cytolysin (CDC) from Streptococcus pneumoniae, the main cause for bacterial pneumonia.
物理化学性质&存储条件
|
分子量
|
455.29
|
|
分子式
|
C23H16Cl2N2O4
|
|
外观性状
|
Solid
|
|
CAS No.
|
|
|
储存条件
|
- 固体粉末
-
-20°C 12 个月; 4°C 6 个月
|
- 配置液
-
-80°C 6 个月; -20°C 6 个月
|
|
Shipping
|
|
|
Solubility
|
10 mM in DMSO
|
|
Chemical Name/SMILES
|
(E)-5-((5-(2,4-dichlorophenyl)furan-2-yl)methylene)-1-(3,5-dimethylphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione
|
参考文献
1. Aziz UBA, et al. Nat Commun. 2024 Apr 26;15(1):3537.
