产品描述:
MD2-IN-1 is a chalcone derivative and an inhibitor of the interaction between myeloid differentiation 2 (MD-2) and LPS.{65884} It inhibits the interaction between MD-2 and LPS in a cell-free assay when used at a concentration of 0.1 µM. It inhibits LPS-induced increases in the levels of Tnf-α and Il-6 secreted from isolated and washed mouse peritoneal macrophages (MPMs; IC50s = 4.27 and 2.09 µM, respectively). MD2-IN-1 (5 and 20 µM) inhibits LPS-induced Nf-κB DNA binding in MPMs. It inhibits the growth of HepG2 hepatocellular, A549 lung, HT-29 colon, HeLa cervical, MDA-MB-231 breast, and A2780 ovarian cancer cells (GI50s= 0.19, 0.16, 0.062, 0.019, 0.065, and 0.32 µM, respectively).{65886} MD2-IN-1 (10 mg/kg) reduces tumor volume and weight in a HeLa mouse xenograft model. In vivo, MD2-IN-1 (20 mg/kg per day) prevents LPS-induced increases in bronchoalveolar lavage fluid (BALF) total protein levels and CD68+ macrophage and neutrophil infiltration in a mouse model of LPS-induced acute lung injury.{65884} It also reduces myeloperoxidase (MPO) activity in isolated neutrophils in the same model.