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BAY 87-2243 Sensitizes Hepatocellular Carcinoma Hep3B Cells to Histone Deacetylase Inhibitors Treatment via GSK-3β Activation

BAY 87-2243 Sensitizes Hepatocellular Carcinoma Hep3B Cells to Histone Deacetylase Inhibitors Treatment via GSK-3β Activation

Yang-Ling Li, Ming-Jun Rao, Ning-Yu Zhang, Lin-Wen Wu, Neng-Ming Lin, Chong Zhang

Exp Ther Med. 2019 Jun;17(6):4547-4553.

PMID: 31186678

Abstract:

Hepatocellular carcinoma (HCC) is associated with some of the highest cancer-associated mortality rates. Histone deacetylase (HDAC) inhibitors anti-HCC activities have been shown to promote Snail-induced metastasis. In the present study, it was shown that BAY 87-2243, a hypoxia-inducible transcription factor-1α inhibitor, could enhance the anti-HCC effects of HDAC inhibitors, including trichostatin A and vorinostat. In addition, BAY 87-2243 plus HDAC inhibitors exhibited synergistic cytotoxicity and induced significant cell death in Hep3B cells. Additionally, BAY 87-2243 combined with HDAC inhibitors-treated Hep3B cells formed fewer and smaller colonies as compared with either the control or single agent-treated cells. Furthermore, glycogen synthase kinase-3β might be involved in the enhanced cell death induced by BAY 87-2243 plus HDAC inhibitors. The present data also indicated that BAY 87-2243 combined with HDAC inhibitors could suppress the migration of Hep3B cells, and BAY 87-2243 could reverse the HDAC inhibitor-induced Snail activation in Hep3B cells. In conclusion, BAY 87-2243 combined with HDAC inhibitors might be an attractive chemotherapy strategy for HCC therapy.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1227158851	BAY 87-2243		1227158-85-1	Price

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