1-甲苯磺酰-1H-吲哚-2-甲酸乙酯

IC50: 5.74 μM (NOD1), 6.45 μM (NOD2)

NOD-IN-1 (compound 4) is potent mixed inhibitor of NOD1 and NOD2, displaying a balanced inhibitory activity on both targets in the low micromolar range. NOD-IN-1 (IC ₅₀ (NOD1)=5.74 μM; IC ₅₀ (NOD2)=6.45 μM) is identified as the best of the series, possessing NOD1- and NOD2-inhibitory activities in the lower micromolar range. These results show that NOD-IN-1 is 7-fold less potent than Noditinib-1 in terms of NOD1 inhibition and completely devoid of selective activity for NOD1 or NOD2 as opposed to Noditinib-1. NOD-IN-1 exhibits balanced dual activities of less than 10 μM on the two targets.