SC75741 是NF-Κb抑制剂,对p65的IC50为 200 nM。它可阻断流感病毒复制。它通过损害NF-Κb亚基 p65 的 DNA 结合,导致细胞因子,趋化因子和促凋亡因子的表达降低,抑制 Caspase 活化和阻断 Caspase 介导的病毒核糖核蛋白的核输出。
产品描述
SC75741 is a potent P65 inhibitor with IC50 of 200 nM
体外活性
SC75741 shows immunosuppressive activity by inhibiting human PBMC proliferation with IC50 of 2.2 μM. [1] SC75741 inhibits replication of influenza A and B viruses by inhibiting NF-κB-mediated signalling on a transcriptional level. Moreover, SC75741 shows a high barrier for development of resistant virus variants. [2]
体内活性
SC75741 (15 mg/kg i.p.) reduces virus replication and cytokine expression in mice lungs after H5N1 influenza virus infection. [2]
激酶实验
NF-κB reporter gene assay: The NF-κB reporter gene assay is prepared with A549-NF-κB-SEAP cell line according to manufacturer's instructions. In short, A549 cells stably transfected with pNF-κB-SEAP reporter gene plasmid are plated and allowed to attach overnight. The cells are subsequently incubated for 5 h with described compounds at 100, 30, 10, 3, 1, 0.3, 0.1, and 0 μM and then stimulated with 10 ng/ml TNF-α for 22 h. The supernatant of the cell is analyzed for SEAP activity using a chemiluminescent SEAP reporter gene assay.
细胞实验
Cell viability assay is prepared using a CellTiter-BluTM Cell Viability Assay. For each concentration of the compound four replicates are measured.(Only for Reference)
Cas No.
913822-46-5
分子式
C29H23N7O2S2
分子量
565.67
储存和溶解度
DMSO:33 mg/mL (58.3 mM)
H2O:<1 mgml
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years