Dacinostat（404951-53-7）

Mechanism of action: treatment of NDHF cells with danoselta will not only lead to the expected growth arrest of G1-S, but also significantly reduce the accumulation of cells in S phase and G2-M checkpoint. Daroselta induces apoptosis and death of human tumor cells. Danoselta increases the acetylation of histones H3 and H4. The IC50 of danoselta inhibiting HDAC1 was 9nM. Danoselta (10 and 20 nM) inhibited the proliferation of 32D cells expressing AML fusion protein. Daroselta can damage the short-term implantation potential of leukemia stem cells. Daroselta will deplete AML1/ETO and PLZF/RAR α The self-renewal potential of positive HSCs in vitro.

Application: Daroselta, R&D code NVP-LAQ824, is an effective HDAC inhibitor and can inhibit the activity of HDAC1, mainly used for cancer research. In vitro, danoselta activated p21 promoter with AC50 of 0.30 μ M。 Daroselta inhibits the growth of tumor cells (H1299, HCT116) with IC50 of 150 and 10nM, respectively. Darnolestat also showed inhibitory activity against two prostate cancer cell lines (DU145 and PC3) and breast cancer cell line (MDA435), with IC50 of 18, 23 and 39 nM respectively.

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