Oxamflatin is an effective inhibitor of HDAC (IC50: 15.7 nM).

HDAC:15.7 nM

Oxamflatin is able to significantly inhibit DNA synthesis and cell proliferation. Oxamflatin can induce E-cadherin expression and also reduce cell viability in the MKN-45 cell line. Oxamflatin causes transcriptional activation of junD and morphological reversion in various NIH3T3-derived transformed cell lines. Oxamflatin induces an elongated cell shape with filamentous protrusions as well as the arrest of the cell cycle at the G1 phase in HeLa cells. Oxamflatin displays antiproliferative activity against various mouse and human tumor cell lines with drastic changes in the cell morphology. Oxamflatin greatly increases the transcriptional activity of the CMV promoter in a dose-dependent manner and inhibits intracellular HDAC activity[1][2][3].

The ILS of the mice treated with Oxamflatin at the dose of 50 mg/kg is calculated to be more than 67% and one mouse survived over 60 days after tumor inoculation. Injection of Oxamflatin, six times at the dose of 20 mg/kg, shows a significant increase in the days of survival (38% of ILS) [1].