NCI 126224

NCI 126224 is a toll-like receptor 4 (TLR4) antagonist. 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 (Cay-14806), TLR1/2 agonist Pam3CSK4 (Cay-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 (Cay-24220) in the same cells at 0.6 µM. NCI 126224 inhibits LPS-induced NF-kappaB activity in a reporter assay using BV-2 microglial cells and LPS-induced increases in IL-1beta and TNF-alpha levels in RAW 264.7 macrophages (IC50s = 5.92, 0.42, and 1.54 µM, respectively).Formal Name: 2-[(2-nitrophenyl)methylene]-propanedioic acid, 1,3-dimethyl ester. CAS Number: 65974-52-9. Synonyms: NSC 126224. Molecular Formula: C12H11NO6. Formula Weight: 265.2. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Chloroform: Soluble, Methanol: Soluble. SMILES: COC(/C(C(OC)=O)=C/C1=C(C=CC=C1)[N+]([O-])=O)=O. InChi Code: InChI=1S/C12H11NO6/c1-18-11(14)9(12(15)19-2)7-8-5-3-4-6-10(8)13(16)17/h3-7H,1-2H3. InChi Key: LKLMASCOTOBEMT-UHFFFAOYSA-N.