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CAS No.: 913822-46-5

SC75741 Catalog No. CSN19187

Synonyms: SC75741

SC75741 is a novel NF-kappaB inhibitor.

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实验方案

技术信息

生物活性

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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7678 mL
- 8.8391 mL
- 17.6782 mL
- 5 mM
- 0.3536 mL
- 1.7678 mL
- 3.5356 mL
- 10 mM
- 0.1768 mL
- 0.8839 mL
- 1.7678 mL

技术信息

CAS号

913822-46-5

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H23N7O2S2

运输

蓝冰

分子量

565.67

别名

SC75741

溶解度

DMSO	225.0 mg/mL (397.8 mM)
Water	insoluble

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