ILK-IN-2 is an inhibitor of integrin-linked kinase (ILK; IC50 = 0.6 μM).1 It inhibits the phosphorylation of Akt, glycogen synthase kinase 3β (GSK3β), and myosin light-chain (MLC) in PC3 prostate and MDA-MB-231 breast cancer cells when used at concentrations ranging from 1 to 4 μM. ILK-IN-2 inhibits the proliferation of LNCaP, PC3, MDA-MB-231, MDA-MB-468, SK-BR-3, and MCF-7 cancer cells (IC50s = 1.6, 2, 1, 1.5, 1.8, and 2.5 μM, respectively), as well as induces autophagy and apoptosis in PC3 cells when used at a concentration of 2 μM. It also reduces protein levels of Y-box binding protein (YB-1), HER2, and EGFR in PC3 cells. ILK-IN-2 (25 and 50 mg/kg) reduces tumor growth in a PC3 mouse xenograft model.
1.Lee, S.-L., Hsu, E.-C., Chou, C.-C., et al.Identification and characterization of a novel integrin-linked kinase inhibitorJ. Med. Chem.54(18)6364-6374(2011)