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Oxamflatin is a potent histone deacetylase inhibitor with IC50 value of 15.7 nM [1].

Histone deacetylases (HADC) are a series of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone and make the histones to wrap the DNA more tightly, which prevent transcription.

Oxamflatin is a potent histone deacetylase inhibitor and a novel antitumor compound. In mouse and human tumor cell lines, such as P388, Lewis, Lu-99, HT-29 and HeLa cells, Oxamflatin exhibited antiproliferative activity. In HeLa cells, Oxamflatin changed cell morphology, and significantly reduced the number of the cells in S phase and increased the number of cells in G0/G1 phase [1]. In the HIV-1 latently infected Jurkat T cell line, Oxam?atin increased the acetylation level of histone H3 and histone H4 at the nucleosome 1(nuc-1) site of the HIV-1 LTR and activated HIV-1 gene expression by 2-17 fold, suggesting that Oxam?atin has potential as drug candidates as antilatency therapies [2]. In OVCAR-5 and SKOV-3 ovarian cancer cell lines, oxamflatin decreased cell viability and significantly inhibited DNA synthesis and cell proliferation. Also, oxamflatin reduced the expression of c-Myc, CDK4 and E2F1, and the phosphorylation level of Rb protein, but upregulated p21 [3].

In mice transplanted with B16 murine melanoma, Oxamflatin (20 mg/kg) injected intraperitoneally six times on day 1, 3, 5, 7, 9 and 11 significantly increased the days of survival [1].

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