NCI 126224

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 (Item No. 14806), TLR1/2 agonist Pam₃CSK₄ (Item No. 24126), and TLR3 agonist poly(I:C) in RAW 264.7 macrophages but also inhibits NO production induced by the TLR2/6 agonist FSL-1 (Item No. 24220) 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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1. Zhang, S., Cheng, K., Wang, X., et al. Selection, synthesis, and anti-inflammatory evaluation of the arylidene malonate derivatives as TLR4 signaling inhibitors. Bioorg. Med. Chem. 20(20), 6073-6079 (2012).