KY 05009 is an inhibitor of TRAF2- and NCK-interacting kinase (TNIK; Ki = 100 nM).1 It inhibits TGF-β1-induced Wnt, NF-κB, ERK, and JNK signaling and prevents TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in A549 lung cancer cells without inducing cytotoxicity when used at a concentration of 10 μM. KY 05009 inhibits TNF-β1-induced A549 cell migration. It also induces apoptosis in RPMI-8226 multiple myeloma cells in a concentration-dependent manner.2
|1. Kim, J., Moon, S.H., Kim, B.T., et al. A novel aminothiazole KY-05009 with potential to inhibit Traf2- and Nck-interacting kinase (TNIK) attenuates TGF-β1-mediated epithelial-to-mesenchymal transition in human lung adenocarcinoma A549 cells. PLoS One 9(10), e110180 (2014).|2. Lee, Y., Jung, J.I., Park, K.Y., et al. Synergistic inhibition effect of TNIK inhibitor KY-05009 and receptor tyrosine kinase inhibitor dovitinib on IL-6-induced proliferation and Wnt signaling pathway in human multiple myeloma cells. Oncotarget 8(25), 41091-41101 (2017).