| Bioactivity | SC75741 is a broad and efficient NF-κB inhibitor with an IC50 of 200 nM for p65[1]. SC75741 blocks influenza viruses (IV) replication. SC75741 impairs DNA binding of the NF-κB subunit p65, resulting in reduced expression of cytokines, chemokines, and pro-apoptotic factors. SC75741 subsequently inhibits caspase activation and blocks caspase-mediated nuclear export of viral ribonucleoproteins[2]. | ||||||||||||
| Invitro | SC75741 (5 μM; 24-96 hours) inhibits long-term A549 cells proliferation[2].SC75741 (1-10 μM; 5.5-65 hours) reduces A549 cells viability in a concentration-dependent manner indicating a cytostatic effect for A549 cells within a time frame of about 50 and 65 hours[2].SC75741 (5 μM; 24 hours) strongly inhibits cleavage of the effector caspase 3 induced upon H7N7-infection[2]. Cell Proliferation Assay[2] Cell Line: | ||||||||||||
| In Vivo | SC75741 (intraperitoneal injection; 15 mg/kg; for 2 days) leads to a reduced propagation of the H5N1 virus mRNA by 90% in the lungs of infected mice[2].The plasma-levels of SC74751 (intravenously of 5 mg/kg and intraperitoneally of 15 mg/kg; for 3.5 and 6 hours) after i.v. administration decreases mono-exponentially and half-life is roughly 40 min. After i.p. administration, elimination of SC75741 seems to be limited by a slow uptake from the peritoneum and a half-life of 55 min is observed[1]. Animal Model: | ||||||||||||
| Name | SC75741 | ||||||||||||
| CAS | 913822-46-5 | ||||||||||||
| Formula | C29H23N7O2S2 | ||||||||||||
| Molar Mass | 565.67 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Haasbach E, et al. The NF-kappaB inhibitor SC75741 protects mice against highly pathogenic avian influenza A virus. Antiviral Res. 2013 Sep;99(3):336-44. [2]. Ehrhardt C, 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 Jul;15(7):1198-211. |