9-ING-41

9-ING-41 is an inhibitor of glycogen synthase kinase 3β (GSK3β; IC₅₀ = 0.71 ?M).¹ It inhibits the growth of MiaPaCa-2, BxPC-3, and HuP-T3 pancreatic cancer cells (IC₅₀s = 5, 1, and 0.6 ?M, respectively). 9-ING-41 (5 ?M) inhibits GSK3β phosphorylation and induces apoptosis in BxPC-3 and HuP-T3 cells. In vivo, 9-ING-41 (40 mg/kg) reduces tumor growth in an SKOV3 mouse xenograft model.² It also reduces pleural thickening and improves lung function in a mouse model of S. pneumoniae-induced empyema.³

1.Gaisina, I.N., Gallier, F., Ougolkov, A.V., et al.From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3β inhibitors that suppress proliferation and survival of pancreatic cancer cellsJ. Med. Chem.52(7)1853-1863(2009) 2.Hilliard, T.S., Gaisina, I.N., Muehlbauer, A.G., et al.Glycogen synthase kinase 3 beta inhibitors induce apoptosis in ovarian cancer cells and inhibit in vivo tumor growthAnticancer Drugs22(10)978-985(2011) 3.Boren, J., Shryock, G., Fergis, A., et al.Inhibition of glycogen synthase kinase 3β blocks mesomesenchymal transition and attenuates Streptococcus pneumonia-mediated pleural injury in miceAm. J. Pathol.187(11)2461-2472(2017)