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A Synthetic Chalcone Derivative, 2-hydroxy-3',5,5'-trimethoxychalcone (DK-139), Suppresses the TNFα-induced Invasive Capability of MDA-MB-231 Human Breast Cancer Cells by Inhibiting NF-κB-mediated GROα Expression

Da Young Lee, Da Hyun Lee, Jung You Jung, Dongsoo Koh, Geum-Soog Kim, Young-Sup Ahn, Young Han Lee, Yoongho Lim, Soon Young Shin

Bioorg Med Chem Lett. 2016 Jan 1;26(1):203-8.

PMID: 26602275

Abstract:

2-Hydroxy-3',5,5'-trimenthoxyochalcone (DK-139) is a synthetic chalcone-derived compound. This study evaluated the biological activity of DK-139 on the inhibition of tumor metastasis. Growth-regulated oncogene-alpha (GROα) plays an important role in the progression of tumor development by stimulating angiogenesis and metastasis. In this study, DK-139 inhibited tumor necrosis factor alpha (TNFα)-induced GROα gene promoter activity by inhibiting of IκB kinase (IKK) in MDA-MB231 cells. In addition, DK-139 prevented the TNFα-induced cell migration, F-actin formation, and invasive capability of MDA-MB-231 cells. These findings suggest that DK-139 is a potential drug candidate for the inhibition of tumor cell locomotion and invasion via the suppression of NF-κB-mediated GROα expression.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
IAR4248589 GROα human GROα human Price
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