9-ING-41

9-ING-41 is an inhibitor of glycogen synthase kinase 3β (GSK3β; IC₅₀ = 0.71 µM).¹ It inhibits the growth of MiaPaCa-2, BxPC-3, and HuP-T3 pancreatic cancer cells (IC₅₀s = 5, 1, and 0.6 µM, respectively). 9-ING-41 (5 µM) 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

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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 cells. J. 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 growth. Anticancer Drugs 22(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 mice. Am. J. Pathol. 187(11), 2461-2472 (2017).