产品说明书

SC75741

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Chemical Structure| 913822-46-5 同义名 : -
CAS号 : 913822-46-5
货号 : A448073
分子式 : C29H23N7O2S2
纯度 : 99%+
分子量 : 565.669
MDL号 : MFCD18206785
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 85 mg/mL(150.26 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • NF-κB

    NF-κB, EC50:200 nM
描述 Nuclear Factor-kappa B (NF-κB) is a transcription factor family that regulates a large number of genes that are involved in important physiological processes, including survival, inflammation, and immune responses[3]. SC75741 is a potent inhibitor of NF-κB with an EC50 of 200 nM[2]. SC75741 also acts as a broad and efficient blocker of IV replication in non-toxic concentrations. The underlying molecular mechanism of SC75741 action involves impaired DNA binding of the NF-κB subunit p65, resulting in reduced expression of cytokines, chemokines, and pro-apoptotic factors, subsequent inhibition of caspase activation and block of caspase-mediated nuclear export of viralribonucleoproteins. SC75741 reduces viral replication and H5N1-induced IL-6 and IP-10 expression in the lung of infected mice. Besides its virustatic effect the drug suppresses virus-induced overproduction of cytokines and chemokines, suggesting that it might prevent hypercytokinemia that is discussed to be an important pathogenicity determinant of highly pathogenic IV. Importantly the drug exhibits a high barrier for development of resistant virus variants. Thus, SC75741-derived drugs may serve as broadly non-toxic anti-influenza agents[1].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
A549 cells Function assay 5 h Inhibition of NF-kappaB in A549 cells after 5 hrs by reporter gene assay, EC50=0.2 μM 17869512
PBMC Proliferation assay Antiproliferative activity against human PBMC, IC50=2.2 μM 17869512
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.77mL

0.35mL

0.18mL

8.84mL

1.77mL

0.88mL

17.68mL

3.54mL

1.77mL
参考文献

[1]Ehrhardt C, Rückle A, Hrincius ER, et al. The NF-κB inhibitor SC75741 efficiently blocks influenza virus propagation and confers a high barrier for development of viral resistance. Cell Microbiol. 2013;15(7):1198-1211.

[2]Leban J, Baierl M, Mies J, et al. A novel class of potent NF-kappaB signaling inhibitors. Bioorg Med Chem Lett. 2007;17(21):5858-5862.

[3]NF-kappaB: Two Sides of the Same Coin