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    InvivoChem Cat #: V0769
    CAS #: 913822-46-5Purity ≥98%

    Description: SC75741 (SC-75741; SC 75741) is a novel, selective and potent NF-κB inhibitor with potential antiviral and anti-inflammatory activity. It inhibits NF-κB with an EC50 of 200 nM. SC75741 blocks influenza viruses (IV) replication in non-toxic concentrations. 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.  In MDCK cells, inhibitory potential of 5 uM SC75741 on virus replication is highest at later stages of infection. In the human alveolar type II epithelial cell line A549 infected with H5N1 and H7N7 viruses, SC75741 provoked an efficient reduction of virus titers in a dose-dependent way. In the lung of infected mice, SC75741 reduces viral replication and H5N1-induced IL6 and IP-10 expression. In addition, SC75741 also reduced cytokine production in vivo that is involved in hypercytokinemia mediated by influenza virus infection. Importantly, SC75741 exhibits a high barrier for virus variants.

    References: Bioorg Med Chem Lett. 2007 Nov 1;17(21):5858-62; Cell Microbiol. 2013 Jul;15(7):1198-211. 

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    Molecular Weight (MW)565.67
    CAS No.913822-46-5
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 35 mg/mL (61.9 mM)          
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: N-(6-benzoyl-1H-benzimidazol-2-yl)-2-(1-thieno[3,2-d]pyrimidin-4-yl-4-piperidinyl)-4-thiazolecarboxamide


    InChi Code: InChI=1S/C29H23N7O2S2/c37-24(17-4-2-1-3-5-17)19-6-7-20-22(14-19)34-29(33-20)35-27(38)23-15-40-28(32-23)18-8-11-36(12-9-18)26-25-21(10-13-39-25)30-16-31-26/h1-7,10,13-16,18H,8-9,11-12H2,(H2,33,34,35,38)

    SMILES Code: O=C(C1=CSC(C2CCN(C3=C4C(C=CS4)=NC=N3)CC2)=N1)NC5=NC6=CC=C(C(C7=CC=CC=C7)=O)C=C6N5


    SC-75741; SC 75741; SC75741;

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    In Vitro

    In vitro activity: SC75741 shows immunosuppressive activity by inhibiting human PBMC proliferation with IC50 of 2.2 μM. 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.

    Kinase 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. 

    Cell Assay: Cell viability assay is prepared using a CellTiter-BluTM Cell Viability Assay. For each concentration of the compound four replicates are measured.

    In VivoSC75741 (15 mg/kg i.p.) reduces virus replication and cytokine expression in mice lungs after H5N1 influenza virus infection.
    Animal modelC57BL/6 mice infected with H5N1 influenza virus
    Formulation & DosageDissolved in 10% DMSO, 30% Cremophor EL and 60% PBS; 15 mg/kg; i.p. injection

    Bioorg Med Chem Lett. 2007 Nov 1;17(21):5858-62; Cell Microbiol. 2013 Jul;15(7):1198-211. 

    These protocols are for reference only. InvivoChem does not independently validate these methods.

    SC75741 inhibits transcriptional activation of NF-κB-dependent genes. Cell Microbiol. 2013 Jul;15(7):1198-211. 
    SC75741 reduces virus-induced expression of the NF-κB target genes IL-6 and TRAIL but not IFN-β or IRF-3 activity. Cell Microbiol. 2013 Jul;15(7):1198-211. 
    SC75741 treatment influences cytokine expression in mice lungs after H5N1 influenza virus infection. Cell Microbiol. 2013 Jul;15(7):1198-211. 


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