KY 05009 是一种 ATP 竞争性 Traf2 和 Nck 相互作用激酶 (TNIK) 抑制剂，Ki 为 100 nM。 KY 05009 药理学抑制人肺腺癌细胞中 TGF-β1 诱导的上皮间质转化 (EMT)。 KY 05009 抑制 TNIK 的蛋白质表达和 Wnt 靶基因的转录活性，并诱导癌细胞凋亡。 KY 05009 具有抗癌活性。
货号:ajcx20392
CAS:1228280-29-2
分子式:C18H16N4O2S
分子量：352.4
溶解度:DMSO: sonicated
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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).