5-Azacytidine (320-67-2) is specific inhibitor of DNA methyltransferase1. Incorporates into DNA and covalently reacts with and inhibits DNA methyltransferases. Induces demethylation and reactivation of silenced genes2. Increases stem cell reprogramming efficiency3. Induces cardiac differentiation of human mesenchymal stem cells by activating ERK4. Induces apoptosis in multiple myeloma cells via ATR-mediated DNA double strand breaks5. Cell permeable.
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2) Brueckner et al. (2005), Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA Methyltransferases; Cancer Res., 65 6305
3) Mikkelsen et al. (2008), Dissecting direct reprogramming through integrative genomic analysis; Nature, 454 49
4) Qian et al. (2011), 5-Azacytidine induces cardiac differentiation of human umbilical cord-derived mesenchymal stem cells by activating extra cellular regulated kinase; Stem Cells Dev., 21 67
5) Kiziltepe et al. (2007), 5-Azacytidine, a DNA Methyltranserase inhibitor, induces ATR-mediated DNA double-strand break responses, apoptosis, and synergistic cytotoxicity with doxorubicin and bortezomib against multiple myeloma cells; Mol. Cancer Ther., 6 1718