MD2-IN-1

MD2-IN-1 is a chalcone derivative and an inhibitor of the interaction between myeloid differentiation 2 (MD-2) and LPS.¹ 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).² 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.¹ It also reduces myeloperoxidase (MPO) activity in isolated neutrophils in the same model.

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1. Zhang, Y., Wu, J., Ying, S., et al. Discovery of new MD2 inhibitor from chalcone derivatives with anti-inflammatory effects in LPS-induced acute lung injury. Sci. Rep. 6, 25130 (2016).

2. Zhang, Y.-L., Li, B.-Y., Yang, R., et al. A class of novel tubulin polymerization inhibitors exert effective anti-tumor activity via mitotic catastrophe. Eur. J. Med. Chem. 163, 896-910 (2019).