An inhibitor of NOD1 and NOD2
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NOD-IN-1 is an inhibitor of nucleotide-binding oligomerization domain (NOD) receptors and a derivative of nodinitib-1 .1 NOD-IN-1 inhibits C12-iE-DAP-induced NF-?B activation in HEK-Blue cells expressing human recombinant NOD1 or NOD2 (IC50s = 5.74 and 6.45 ?M, respectively).
1.Ke?ek Ple?ec, K., Urban?i?, D., Gobec, M., et al.Identification of indole scaffold-based dual inhibitors of NOD1 and NOD2Bioorg. Med. Chem.24(21)5221-5234(2016)
Cell experiment: | An MTS assay in which the proliferation rates of HEK-Blue NOD1 cells are measured in the presence of Noditinib-1 and of the synthesized potential NOD1 inhibitor NOD-IN-1 is employed to screen these compounds for potential cytotoxicity. Cells are treated for 24 h with the compound of interest at concentrations of up to 25 μM. Comparison of the resulting metabolic activities with that of the untreated control showed that all compounds are well tolerated by HEK-Blue NOD1 cells, since their residual metabolic activities do not fall below 80% at the maximum concentration tested[1]. |
参考文献: [1]. Kecek Plesec K, et al. Identification of indole scaffold-based dual inhibitors of NOD1 and NOD2. Bioorg Med Chem. 2016 Nov 1;24(21):5221-5234. |
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