Background
NCI 126224 is a toll-like receptor 4 (TLR4) antagonist.1 NCI 126224 selectively inhibits nitric oxide (NO) production induced by the TLR4 agonist LPS (IC50 = 0.31 μM) over the TLR7/8 agonist R-848 , TLR1/2 agonist Pam3CSK4 , and TLR3 agonist poly(I:C) in RAW 264.7 macrophages but also inhibits NO production induced by the TLR2/6 agonist FSL-1 in the same cells at 0.6 μM. NCI 126224 inhibits LPS-induced NF-κB activity in a reporter assay using BV-2 microglial cells and LPS-induced increases in IL-1β and TNF-α levels in RAW 264.7 macrophages (IC50s = 5.92, 0.42, and 1.54 μM, respectively).
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