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| Anti-gastric cancer activity of novel IKKβ inhibitor in vitro |
| BAO Miao1, HUANG Chongxian1, HU Jun1, ZHU Lu2, WEI Tao2, CHEN Xiaoming1 |
| 1.Department of Pediatric Surgery, the First Affiliated Hospital of Wenzhou Medical University, Wenzhou 325015, China; 2.School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, China |
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BAO Miao,HUANG Chongxian,HU Jun, et al. Anti-gastric cancer activity of novel IKKβ inhibitor in vitro[J]. JOURNAL OF WEZHOU MEDICAL UNIVERSITY, 2019, 49(6): 397-400,407.
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Abstract Objective: To investigate the anti-gastric cancer activity of novel IKKβ inhibitor EF24 analog H18 in vitro. Methods: Molecular docking is used to simulate the binding of H18 and IKKβ. MTT assay was used to detect the effect of H18 on the growth of gastric cancer cell line BGC-823. The clonogenicity assay was employed to investigate the role of H18 in the colony formation ability of BGC-823. Cells apoptosis was observed by DAPI staining. The inhibition of the NF-κB signaling pathway was verified by Western blot. Results: H18 binds to the allosteric site of IKKβ. The IC50 of H18 to BGC-823 cells was (1.7±0.3) μmol/L at 72 h. Compared with IKK inhibitor BMS-345541, H18 significantly inhibited cell proliferation, but had no effect on apoptosis. H18 can inhibit significantly NF-κB signaling pathway in gastric cancer cells. Conclusion: H18 is a promising IKKβ inhibitor with good anti-tumor activity in vitro.
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Received: 27 March 2019
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